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Albiglutide

Alias: Eperzan; Tanzeum; 782500-75-8; Eperzan; tanzeum; GSK-716155; GSK716155; GSK 716155; albugon
Cat No.:V3127 Purity: ≥98%
Albiglutide Fragment (GLP-1 fragment 7-36)is one copy of the 30-amino-acid sequence of modified human glucagon-like peptide-1 (GLP-1, fragment 7-36).
Albiglutide
Albiglutide Chemical Structure CAS No.: 782500-75-8
Product category: Glucagon Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
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250mg
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Other Forms of Albiglutide:

  • Albiglutide fragment (GLP-1-Gly8; GLP-1 (7-36) analog)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Albiglutide Fragment (GLP-1 fragment 7-36) is one copy of the 30-amino-acid sequence of modified human glucagon-like peptide-1 (GLP-1, fragment 7-36). The albumin section, which can be found in the entire sequence of albiglutide (trade names Eperzan, Tanzeum, GSK-716155, GSK716155, albugon), a strong and long-acting GLP-1 agonist licensed for the treatment of type 2 diabetes/T2DM, is absent from Albiglutide Fragment. GSK developed and marketed albiglutide under the trade names Tanzeum and Eperzan in the US and EU, respectively, as an anti-diabetic/anti-hyperglycemic medication. Albiglutide is a peptide made up of 17 disulfide bridges and 645 proteinogenic amino acids. The modified human GLP-1 consists of two copies, amino acids 1–30 and 31–60, where glycine has been substituted for alanine at position 2 to improve resistance to DPP-4. The human albumin sequence is what's left. In the event that metformin therapy is ineffective or intolerable, albiglutide can be used either alone or in conjunction with other antidiabetic medications, such as insulins. Although it is unclear as of 2018 if albiglutide affects a person's risk of dying, GSK has stated that it plans to remove the medication from the global market by July 2018 due to financial concerns.

Biological Activity I Assay Protocols (From Reference)
Targets
GLP-1 receptor
ln Vitro

In vitro activity: Albiglutide is a tiny protein or peptide made up of two copies of a 30-amino-acid sequence of human GLP-1 that has been altered (fragment 7–36). To increase resistance to DPP–4, glycine has been added in place of the naturally occurring alanine at position 8.

ln Vivo
Albiglutide lowers blood sugar levels after a single dosage in less than 24 hours due to the molecule's binding to the GLP-1 receptor. It is dose-related that both postprandial and fasting glucose levels decrease. Less powerful than GLP-1 is albiglutide. Increased β-cell mass is stimulated by albiglutide administration in animal models of diabetes. Patients with type 2 diabetes experience a maximum concentration in 3-5 days and a half-life of 3.6–6.8 days after receiving a single 30-mg dose SC. 8.2-18.5 L was the apparent volume of distribution following an albiglutide dose. In the bloodstream, albiglutide eventually breaks down into discrete amino acids and small peptides. Albiglutide did not appear to have any effect on respiratory function, heart rate, electrocardiographic intervals, cardiovascular function, or any indication of arrhythmias or abnormalities in the electrocardiograms of male cynomolgus monkeys. Additionally, no effects of albiglutide were observed on neurobehavioral functional assessments. Albiglutide is unable to enter the brain's satiety centers through the blood–brain barrier. After myocardial I/R injury, albiglutide decreased the size of the myocardial infarct and improved cardiac function and energetics. These effects are linked to increased myocardial glucose uptake and a change toward a more energetically favorable substrate metabolism by raising both glucose and lactate oxidation.
Animal Protocol
1, 3 or 10 mg/kg/day; s.c.
Male Sprague-Dawley rats
ADME/Pharmacokinetics
Absorption, Distribution and Excretion
Maximum concentrations of albiglutide were reached at 3 to 5 days post-dosing following a single 30mg dose. The mean peak concentration (Cmax) and mean area under the time-concentration curve (AUC) of albiglutide were 1.74 mcg/mL and 465 mcg.h/mL, respectively
11 L.
67 mL/h.
/MILK/ It is not known whether albiglutide is distributed into milk in humans ... .
Albiglutide is a glucagon-like peptide-1 analogue composed of tandem copies of modified human glucagon-like peptide-1 (7-36) coupled to recombinant human albumin that is approved in adults for the treatment of type 2 diabetes mellitus. After subcutaneous administration, albiglutide is likely primarily absorbed via the lymphatic circulation, with maximum concentrations being reached in 3 to 5 days; steady-state exposures are achieved following approximately 4 to 5 weeks of once-weekly administration. The elimination half-life of albiglutide is approximately 5 days. Clearance of albiglutide is 67 mL/h with between-subject variability of 34.9%; no covariates have been identified that would require dose adjustment of albiglutide. Albiglutide lowers the fasting plasma glucose and reduces postprandial glucose excursions. In addition, beta-cell secretion is enhanced by albiglutide during hyperglycemia, whereas secretion is suppressed during hypoglycemia; alpha-cell response to hypoglycemia is not impaired by albiglutide. Albiglutide does not prolong the corrected QT interval but has a modest effect on heart rate in patients with type 2 diabetes mellitus. Dose adjustment is not suggested in patients with renal impairment, but experience in patients with severe renal impairment is very limited, and it is recommended that albiglutide be used with care in such patients due to an increased frequency of diarrhea, nausea, and vomiting. No clinically relevant drug interactions have been observed in clinical trials.
Following SC administration of a single 30-mg dose to subjects with type 2 diabetes mellitus, maximum concentrations of albiglutide were reached at 3 to 5 days post-dosing. The mean peak concentration (C max) and mean area under the time-concentration curve (AUC) of albiglutide were 1.74 mcg/mL and 465 mcg.h/mL, respectively, following a single dose of 30 mg albiglutide in type 2 diabetes mellitus subjects. Steady-state exposures are achieved following 4 to 5 weeks of once-weekly administration. Exposures at the 30-mg and 50-mg dose levels were consistent with a dose-proportional increase. Similar exposure is achieved with SC administration of albiglutide in the abdomen, thigh, or upper arm. The absolute bioavailability of albiglutide following SC administration has not been evaluated. The mean estimate of apparent volume of distribution of albiglutide following SC administration is 11 L. As albiglutide is an albumin fusion molecule, plasma protein binding has not been assessed. The mean apparent clearance of albiglutide is 67 mL/hr with an elimination half-life of approximately 5 days, making albiglutide suitable for once-weekly administration.
Metabolism / Metabolites
Biotransformation studies have not been performed. Because albiglutide is an albumin fusion protein, it likely follows a metabolic pathway similar to native human serum albumin, which is catabolized primarily in the vascular endothelium.
Albiglutide is a protein for which the expected metabolic pathway is degradation to small peptides and individual amino acids by ubiquitous proteolytic enzymes. Classical biotransformation studies have not been performed. Because albiglutide is an albumin fusion protein, it likely follows a metabolic pathway similar to native human serum albumin which is catabolized primarily in the vascular endothelium.
Biological Half-Life
4-7 days.
The elimination half-life of albiglutide following subcutaneous administration is 5 days, making the drug suitable for once-weekly administration.
Toxicity/Toxicokinetics
Toxicity Summary
IDENTIFICATION AND USE: Albiglutide (trade name: Tanzeum) is a prescription medication approved to improve glycemic control in adults with type 2 diabetes mellitus. HUMAN EXPOSURE AND TOXICITY: In epidemiological meta-analyses, pancreatitis and thyroid cancer were observed, but it was not clear if they were related to the treatment. Additional adverse events included gastrointestinal symptoms (nausea, vomiting, and diarrhea), and hypoglycemia. In patients treated with GLP-1 receptor agonists, there have been post marketing reports of acute renal failure and worsening of chronic renal failure, which may sometimes require hemodialysis. Some of these events were reported in patients without known underlying renal disease. The risk of hypoglycemia is increased when albiglutide is used in combination with insulin secretagogues (e.g., sulfonylureas) or insulin. In clinical trials, acute pancreatitis has been reported in association with albiglutide. There may be an increased risk of thyroid C-cell tumors in patients treated with albiglutide. Albiglutide is an agonist of the GLP-1 receptor and augments glucose-dependent insulin secretion. Albiglutide also slows gastric emptying. ANIMAL STUDIES: Carcinogenicity of albiglutide could not be assessed in rodents, but other glucagon-like peptide-1 (GLP-1) receptor agonists have caused thyroid C-cell tumors in rodents at clinically relevant exposures. Human relevance of GLP-1 receptor agonist induced C-cell tumors in rodents has not been determined. In pregnant mice given subcutaneous doses from gestation Day 6 through 15 (organogenesis), embryo-fetal lethality (post-implantation loss) and bent (wavy) ribs were observed, in addition to maternal toxicity (body weight loss and reduced food consumption). Offspring exhibited reduced body weight pre-weaning, dehydration and coldness, and a delay in balanopreputial separation. Increased mortality and morbidity were seen at all doses in lactating females. Reduced weight gain in the pups was also observed during the treatment period. In a mouse fertility study, reductions in estrous cycles were observed at 50 mg/kg/day, a dose associated with maternal toxicity (body weight loss and reduced food consumption). Females were treated with SC doses for 7 days prior to cohabitation with males, and continuing through mating. Reductions in estrous cycles were observed.
Hepatotoxicity
In large clinical trials, serum enzyme elevations were no more common with albiglutide therapy than with placebo or comparator agents, and no instances of clinically apparent liver injury were reported. Since licensure, there have been no published case reports of hepatotoxicity due to albiglutide and the product label does not list liver injury as an adverse event. Thus, liver injury due to albiglutide must be rare, if it occurs at all.
Likelihood score: E (unlikely cause of clinically apparent liver injury).
Interactions
Potential pharmacokinetic interactions (altered absorption because of albiglutide-induced slowing of gastric emptying). In clinical trials, albiglutide did not affect the absorption of concomitantly administered oral drugs to any clinically relevant degree. However, caution should be exercised when albiglutide is administered concomitantly with oral drugs.
To review drug interaction studies of glucagon-like peptide-1 receptor agonists (GLP-1RAs) and concurrent oral medications. PubMed was searched (to December 5, 2011) using the terms exenatide, liraglutide, albiglutide, and lixisenatide. The AUCs of acetaminophen and lovastatin were decreased after exenatide administration and those of lisinopril and digoxin were decreased after liraglutide administration. In 10 studies, GLP-1RAs decreased the C(max) and, in 14 studies, prolonged the t(max) of study drug. Pharmacokinetic properties of drugs and differences in study design can explain differences in interaction potential. GLP-1RAs may produce clinically significant interactions with drugs that require achievement of target peak concentrations or a rapid onset of action. Studies in patients with type 2 diabetes are needed to further assess and allow comparison of several GLP-1RA agents' impact on steady-state pharmacokinetics and pharmacodynamics of concomitant oral medications.
References

[1]. Expert Opin Biol Ther . 2016 Dec;16(12):1557-1569.

Additional Infomation
Albiglutide is a glucagon-like peptide-1 agonist (GLP-1) biologic drug indicated in the treatment of type 2 diabetes. It is marketed under the brands Eperzan and Tanzeum by GSK (GlaxoSmithKline). It is a dipeptidyl peptidase-4-resistant glucagon-like peptide-1 dimer fused to human albumin. Albiglutide was approved on April 15, 2014 by the FDA.
Albiglutide is a recombinant DNA produced polypeptide analogue of human glucagon-like peptide-1 (GLP-1) which is used in combination with diet and exercise in the therapy of type 2 diabetes, either alone or in combination with other antidiabetic agents. There have been no published reports of hepatotoxicity attributed to albiglutide therapy.
Albiglutide is a long-acting glucagon-like peptide-1 (GLP-1) receptor agonist, with antihyperglycemic activity. Albiglutide is composed of a GLP-1 (7-36) dimer fused to recombinant human albumin. Upon subcutaneous administration, this agent has a half-life of 4-7 days and resists degradation by dipeptidyl peptidase-4 (DPP-4).
See also: Albiglutide (annotation moved to).
Drug Indication
Indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
Eperzan is indicated for the treatment of type 2 diabetes mellitus in adults to improve glycaemic control as: MonotherapyWhen diet and exercise alone do not provide adequate glycaemic control in patients for whom use of metformin is considered inappropriate due to contraindications or intolerance. Add-on combination therapyIn combination with other glucose-lowering medicinal products including basal insulin, when these, together with diet and exercise, do not provide adequate glycaemic control (see section 4. 4 and 5. 1 for available data on different combinations).
Treatment of type II diabetes mellitus
Mechanism of Action
Albiglutide is an agonist of the GLP-1 (glucagon-like peptide 1) receptor and augments glucose-dependent insulin secretion. Albiglutide also slows gastric emptying.
Tanzeum is an agonist of the GLP-1 receptor and augments glucose-dependent insulin secretion. Tanzeum also slows gastric emptying.
Therapeutic Uses
Incretins; Antidiabetic
/CLINICAL TRIALS/ ClinicalTrials.gov is a registry and results database of publicly and privately supported clinical studies of human participants conducted around the world. The Web site is maintained by the National Library of Medicine (NLM) and the National Institutes of Health (NIH). Each ClinicalTrials.gov record presents summary information about a study protocol and includes the following: Disease or condition; Intervention (for example, the medical product, behavior, or procedure being studied); Title, description, and design of the study; Requirements for participation (eligibility criteria); Locations where the study is being conducted; Contact information for the study locations; and Links to relevant information on other health Web sites, such as NLM's MedlinePlus for patient health information and PubMed for citations and abstracts for scholarly articles in the field of medicine. Albiglutide is included in the database.
Tanzeum is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. /Included in US product label/
EXPL THER Rats were treated with albiglutide and subjected to 30 min myocardial ischemia followed by 24 hr reperfusion. Left ventricle infarct size, hemodynamics, function and energetics were determined. In addition, cardiac glucose disposal, carbohydrate metabolism and metabolic gene expression were assessed. Albiglutide significantly reduced infarct size and concomitantly improved post-ischemic hemodynamics, cardiac function and energetic parameters. Albiglutide markedly increased both in vivo and ex vivo cardiac glucose uptake while reducing lactate efflux. Analysis of metabolic substrate utilization directly in the heart showed that albiglutide increased the relative carbohydrate versus fat oxidation which in part was due to an increase in both glucose and lactate oxidation. Metabolic gene expression analysis indicated upregulation of key glucose metabolism genes in the non-ischemic myocardium by albiglutide. Albiglutide reduced myocardial infarct size and improved cardiac function and energetics following myocardial I/R injury.
Drug Warnings
/BOX WARNING/ Tanzeum is contraindicated in patients with a personal or family history of medullary thyroid carcinoma (MTC) or in patients with Multiple Endocrine Neoplasia syndrome type 2 (MEN 2). Counsel patients regarding the potential risk of MTC with the use of Tanzeum and inform them of the symptoms of thyroid tumors (e.g., mass in the neck, dysphagia, dyspnea, persistent hoarseness). Routine monitoring of serum calcitonin or using thyroid ultrasound monitoring is of uncertain value for early detection of MTC in patients treated with Tanzeum.
/BOX WARNING/ Carcinogenicity of albiglutide could not be assessed in rodents, but other glucagon-like peptide-1 (GLP-1) receptor agonists have caused thyroid C-cell tumors in rodents at clinically relevant exposures. Human relevance of GLP-1 receptor agonist induced C-cell tumors in rodents has not been determined. It is unknown whether Tanzeum causes thyroid C-cell tumors, including medullary thyroid carcinoma (MTC), in humans.
In patients treated with GLP-1 receptor agonists, there have been postmarketing reports of acute renal failure and worsening of chronic renal failure, which may sometimes require hemodialysis. Some of these events were reported in patients without known underlying renal disease. Use caution when initiating or escalating doses of Tanzeum in patients with renal impairment.
Serious hypersensitivity reactions (pruritus, rash, dyspnea) have been reported in patients receiving albiglutide.1 If a hypersensitivity reaction occurs, albiglutide should be discontinued and the patient should be treated according to the standard of care and monitored until manifestations resolve.
For more Drug Warnings (Complete) data for Albiglutide (14 total), please visit the HSDB record page.
Albiglutide has a chemical structure quite distinct from that of other marketed GLP-1 RAs. The agent has less gastrointestinal side effects than other comparable GLP-1 RAs and is safe in patients with renal failure. As a sole treatment for diabetes and used with other hypoglycemic agents, it achieves a lowering of HbA1c of up to 1%, less than several competitor GLP-1 RAs. The benefit on weight reduction is minimal compared to other GLP-1 RAs. There exists concern about an imbalance of pancreatitis cases in the approval program as well as injection site reactions which led to discontinuance of therapy in up to 2% of participants. A large long term study now underway will determine if albiglutide, with its lower level of GI intolerance, has a place in the treatment of patients with increased risk of cardiovascular events.[1]
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C148H224N40O45
Molecular Weight
3283.6
Exact Mass
3281.646
CAS #
782500-75-8
Related CAS #
Albiglutide fragment TFA; Albiglutide fragment; 224638-84-0
PubChem CID
145994868
Sequence
H-His-Gly-Glu-Gly-aThr-Phe-aThr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-D-Ala-D-Ala-Lys-Glu-Phe-aIle-D-Ala-Trp-Leu-Val-Lys-Gly-Arg-NH2; L-histidyl-glycyl-L-alpha-glutamyl-glycyl-L-allothreonyl-L-phenylalanyl-L-allothreonyl-L-seryl-L-alpha-aspartyl-L-valyl-L-seryl-L-seryl-L-tyrosyl-L-leucyl-L-alpha-glutamyl-glycyl-L-glutaminyl-D-alanyl-D-alanyl-L-lysyl-L-alpha-glutamyl-L-phenylalanyl-L-alloisoleucyl-D-alanyl-L-tryptophyl-L-leucyl-L-valyl-L-lysyl-glycyl-L-argininamide
SequenceShortening
HGEGXFXSDVSSYLEGQAAKEFXAWLVKGR
Appearance
White to yellow powder
Density
1.5±0.1 g/cm3
Index of Refraction
1.661
LogP
-5.2
Hydrogen Bond Donor Count
49
Hydrogen Bond Acceptor Count
50
Rotatable Bond Count
109
Heavy Atom Count
233
Complexity
7620
Defined Atom Stereocenter Count
29
SMILES
O=C([C@H](CC(C)C)NC([C@H](CC1=CNC2C=CC=CC1=2)NC([C@@H](C)NC([C@H]([C@H](C)CC)NC([C@H](CC1C=CC=CC=1)NC([C@H](CCC(=O)O)NC([C@H](CCCCN)NC([C@@H](C)NC([C@@H](C)NC([C@H](CCC(N)=O)NC(CNC([C@H](CCC(=O)O)NC([C@H](CC(C)C)NC([C@H](CC1C=CC(=CC=1)O)NC([C@H](CO)NC([C@H](CO)NC([C@H](C(C)C)NC([C@H](CC(=O)O)NC([C@H](CO)NC([C@H]([C@H](C)O)NC([C@H](CC1C=CC=CC=1)NC([C@@H]([C@H](C)O)NC(CNC([C@H](CCC(=O)O)NC(CNC([C@H](CC1=CN=CN1)N)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)N[C@H](C(N[C@H](C(NCC(N[C@H](C(N)=O)CCCNC(=N)N)=O)=O)CCCCN)=O)C(C)C
InChi Key
JYDZPPZAYQTOIV-OTSUTHPESA-N
InChi Code
InChI=1S/C148H224N40O45/c1-16-76(10)119(145(231)166-79(13)125(211)174-103(59-85-62-158-90-35-24-23-34-88(85)90)135(221)176-99(55-73(4)5)136(222)185-117(74(6)7)143(229)173-92(36-25-27-51-149)127(213)160-65-109(196)167-91(122(153)208)38-29-53-157-148(154)155)187-137(223)101(56-82-30-19-17-20-31-82)177-132(218)97(46-50-115(204)205)172-131(217)93(37-26-28-52-150)170-124(210)78(12)164-123(209)77(11)165-130(216)96(43-47-108(152)195)169-111(198)66-161-129(215)95(45-49-114(202)203)171-133(219)98(54-72(2)3)175-134(220)100(58-84-39-41-87(194)42-40-84)178-140(226)105(68-189)181-142(228)107(70-191)182-144(230)118(75(8)9)186-139(225)104(61-116(206)207)179-141(227)106(69-190)183-147(233)121(81(15)193)188-138(224)102(57-83-32-21-18-22-33-83)180-146(232)120(80(14)192)184-112(199)67-162-128(214)94(44-48-113(200)201)168-110(197)64-159-126(212)89(151)60-86-63-156-71-163-86/h17-24,30-35,39-42,62-63,71-81,89,91-107,117-121,158,189-194H,16,25-29,36-38,43-61,64-70,149-151H2,1-15H3,(H2,152,195)(H2,153,208)(H,156,163)(H,159,212)(H,160,213)(H,161,215)(H,162,214)(H,164,209)(H,165,216)(H,166,231)(H,167,196)(H,168,197)(H,169,198)(H,170,210)(H,171,219)(H,172,217)(H,173,229)(H,174,211)(H,175,220)(H,176,221)(H,177,218)(H,178,226)(H,179,227)(H,180,232)(H,181,228)(H,182,230)(H,183,233)(H,184,199)(H,185,222)(H,186,225)(H,187,223)(H,188,224)(H,200,201)(H,202,203)(H,204,205)(H,206,207)(H4,154,155,157)/t76-,77-,78-,79-,80+,81+,89+,91+,92+,93+,94+,95+,96+,97+,98+,99+,100+,101+,102+,103+,104+,105+,106+,107+,117+,118+,119+,120+,121+/m1/s1
Chemical Name
(4S)-5-[[2-[[(2S,3S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-5-amino-1-[[(2R)-1-[[(2R)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[2-[[(2S)-1-amino-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-2-oxoethyl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-4-[[2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]acetyl]amino]-5-oxopentanoic acid
Synonyms
Eperzan; Tanzeum; 782500-75-8; Eperzan; tanzeum; GSK-716155; GSK716155; GSK 716155; albugon
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: N/A
Water: ~100 mg/mL (~30.5 mM)
Ethanol: N/A
Solubility (In Vivo)

Note: Please refer to the "Guidelines for Dissolving Peptides" section in the 4th page of the "Instructions for use" file (upper-right section of this webpage) for how to dissolve peptides.
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

Injection Formulations
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO 400 μLPEG300 50 μL Tween 80 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).
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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL Saline)


Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 0.3045 mL 1.5227 mL 3.0454 mL
5 mM 0.0609 mL 0.3045 mL 0.6091 mL
10 mM 0.0305 mL 0.1523 mL 0.3045 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
Efficacy and Safety of the Insulin Glargine/Lixisenatide Fixed Ratio Combination (FRC) Versus GLP-1 Receptor Agonist in Patients With Type 2 Diabetes, With a FRC Extension Period
CTID: NCT02787551
Phase: Phase 3
Status: Completed
Date: 2022-03-25
Safety and Efficacy of Albiglutide + Insulin Glargine Versus Insulin Lispro + Insulin Glargine Subjects With Type 2 Diabetes Mellitus
CTID: NCT02229227
Phase: Phase 3
Status: Completed
Date: 2020-11-27
A Study Comparing the Effect of Albiglutide With Exenatide on Regional Brain Activity Related to Nausea in Healthy Subjects
CTID: NCT02802514
Phase: Phase 4
Status: Terminated
Date: 2020-10-30
An Exploratory Study on the Effects of Repeat Doses of Albiglutide Compared to Exenatide on Gastric Myoelectrical Activity and Gastric Emptying in Type 2 Diabetes Mellitus Subjects
CTID: NCT02793154
Phase: Phase 4
Status: Terminated
Date: 2020-10-30
Extension to Study 200952 to Evaluate the Long-term Safety, Tolerability and Pharmacodynamics of Albiglutide Liquid Drug Product in Type 2 Diabetes Mellitus Subjects
CTID: NCT02750930
Phase: Phase 4
Status: Terminated
Date: 2019-07-12
Biological Data
  • farct size following myocardial ischemia/reperfusion injury.. 2011; 6(8): e23570.
  • AlbiglutideCardiac glucose metabolismin vivoandex vivo.
    AlbiglutideIn vivointermediary glucose metabolism in normal rat hearts.. 2011; 6(8): e23570.
  • Albiglutide

    . 2011; 6(8): e23570.
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