Albiglutide Fragment

Alias: 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 Fragment 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
100mg
250mg
Other Sizes

Other Forms of Albiglutide Fragment:

  • 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
References

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

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C148H224N40O45
Molecular Weight
3283.6
CAS #
782500-75-8
Related CAS #
Albiglutide fragment TFA; Albiglutide fragment; 224638-84-0
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
Synonyms
Eperzan; Tanzeum; GSK-716155; GSK716155; GSK 716155; albugon
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)
NA
 (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.

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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.
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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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