| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
GLP-1 receptor (GLP-1R) and Glucagon receptor (GCGR). As an Exendin-4 derivative, it primarily targets the GLP-1 receptor, and its structural modifications suggest potential dual agonism on both GLP-1R and GCGR.
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| ln Vitro |
Pure GLP-1 receptor agonists include exendin-4. Structurally derived from exendin-4, exendin-4 peptide derivatives may have a connection to dual GLP-1/glucagon receptor agonists. Their use in medicine, for instance, includes reducing excessive food intake and treating metabolic syndrome disorders like diabetes and obesity. In order to lower the risk of hypoglycemia, these dual GLP-1/glucagon receptor agonists exhibit decreased activity on the GIP receptor[1].
Not reported. As an Exendin-4 peptide derivative, exendin-4 is known to be a pure GLP-1 receptor agonist. This peptide derivative shows reduced activity on the GIP receptor to lower the risk of hypoglycemia. |
| ln Vivo |
Not reported. The medical use of similar dual GLP-1/glucagon receptor agonists includes treatment of metabolic syndrome disorders like diabetes and obesity, as well as reduction of excess food intake.
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| Enzyme Assay |
A typical cell-free assay for binding to GLP-1R uses radiolabeled ligand displacement. Membranes expressing human GLP-1R are incubated with a fixed concentration of [125I]GLP-1 and varying concentrations of the test compound. After incubation, bound and free ligands are separated by filtration, and radioactivity is measured to calculate inhibition constant (Ki).
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| Cell Assay |
For in vitro cell-based assays, HEK293 cells stably expressing human GLP-1R are seeded in multi-well plates. After overnight culture, cells are incubated with various compound concentrations, and receptor activation is measured by quantifying intracellular cAMP accumulation using a homogeneous time-resolved fluorescence (HTRF) or chemiluminescence-based detection kit.
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| Animal Protocol |
In vivo animal models, such as diet-induced obese (DIO) mice or db/db diabetic mice, are used. Compounds are administered subcutaneously or orally. Endpoints include blood glucose levels (measured via tail vein), cumulative food intake, body weight change, and glucose tolerance via an intraperitoneal glucose tolerance test (IPGTT).
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| ADME/Pharmacokinetics |
Not reported. Similar GLP-1 receptor agonists typically have short half-lives due to rapid renal clearance and enzymatic degradation, requiring modification for extended duration.
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| Toxicity/Toxicokinetics |
Not reported. As a research-grade peptide, no standardized toxicity data is available. GLP-1 receptor agonists are generally well-tolerated with common side effects including nausea, vomiting, and gastrointestinal distress.
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| References |
[1]. US20150315260 A1
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| Additional Infomation |
Exendin-4 is a pure GLP-1 agonist. Exendin-4 peptide derivatives are structurally derived and may relate to dual GLP-1/glucagon receptor agonists. Exendin-4, as Exenatide, has been approved for the treatment of type 2 diabetes and obesity since 2005, serving as a reference for this research compound.
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| Exact Mass |
3054.531
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|---|---|
| CAS # |
1263874-37-8
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| PubChem CID |
171397204
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
40
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| Hydrogen Bond Acceptor Count |
47
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| Rotatable Bond Count |
98
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| Heavy Atom Count |
215
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| Complexity |
7130
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| Defined Atom Stereocenter Count |
26
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| SMILES |
CC[C@H](C)[C@@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC1=CNC2=CC=CC=C21)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)N)C(=O)NCC(=O)NCC(=O)N3CCC[C@H]3C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N4CCC[C@H]4C(=O)N5CCC[C@H]5C(=O)N6CCC[C@H]6C(=O)N[C@@H](CO)C(=O)O)NC(=O)[C@H](CC7=CC=CC=C7)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CCCCN)N
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| InChi Key |
LRIWXAFEWYKFON-UZUWXZSJSA-N
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| InChi Code |
InChI=1S/C136H212N36O42S/c1-12-72(8)110(168-126(204)90(59-75-27-14-13-15-28-75)161-124(202)89(58-70(4)5)159-117(195)81(33-22-51-144-136(142)143)157-130(208)109(71(6)7)167-111(189)73(9)150-115(193)83(39-44-105(181)182)153-119(197)84(40-45-106(183)184)154-120(198)85(41-46-107(185)186)155-122(200)87(48-56-215-11)156-118(196)82(38-43-100(140)176)151-112(190)78(139)30-18-20-49-137)131(209)158-86(42-47-108(187)188)121(199)162-91(60-76-62-145-79-31-17-16-29-77(76)79)125(203)160-88(57-69(2)3)123(201)152-80(32-19-21-50-138)116(194)163-92(61-101(141)177)113(191)147-63-102(178)146-65-104(180)169-52-23-34-96(169)128(206)165-94(67-174)127(205)164-93(66-173)114(192)148-64-103(179)149-74(10)132(210)171-54-25-36-98(171)134(212)172-55-26-37-99(172)133(211)170-53-24-35-97(170)129(207)166-95(68-175)135(213)214/h13-17,27-29,31,62,69-74,78,80-99,109-110,145,173-175H,12,18-26,30,32-61,63-68,137-139H2,1-11H3,(H2,140,176)(H2,141,177)(H,146,178)(H,147,191)(H,148,192)(H,149,179)(H,150,193)(H,151,190)(H,152,201)(H,153,197)(H,154,198)(H,155,200)(H,156,196)(H,157,208)(H,158,209)(H,159,195)(H,160,203)(H,161,202)(H,162,199)(H,163,194)(H,164,205)(H,165,206)(H,166,207)(H,167,189)(H,168,204)(H,181,182)(H,183,184)(H,185,186)(H,187,188)(H,213,214)(H4,142,143,144)/t72-,73-,74-,78-,80-,81-,82-,83-,84-,85-,86-,87-,88-,89-,90-,91-,92-,93-,94-,95-,96-,97-,98-,99-,109-,110-/m0/s1
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| Chemical Name |
(4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-4-amino-1-[[2-[[2-[(2S)-2-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[(2S)-2-[(2S)-2-[(2S)-2-[[(1S)-1-carboxy-2-hydroxyethyl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-2-oxoethyl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2,6-diaminohexanoyl]amino]-5-oxopentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-4-carboxybutanoyl]amino]-4-carboxybutanoyl]amino]-5-oxopentanoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O: 50 mg/mL (16.36 mM)
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| Solubility (In Vivo) |
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
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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 : PEG300 ：Tween 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). View More
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)] 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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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.
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