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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
GLP-1 (9-36) amide targets the GLP-1 receptor, a G protein-coupled receptor that mediates the incretin effects of GLP-1. Unlike the parent peptide GLP-1 (7-36) amide, which is a potent agonist of the GLP-1 receptor, the (9-36) metabolite acts as an antagonist. It binds to the receptor but does not activate downstream signaling, instead blocking the effects of full-length GLP-1. This makes it useful for studying the physiological roles of GLP-1 and its metabolites.
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| ln Vitro |
Hepatic reflux generation (HGP) can be efficiently inhibited by GLP-1 (9-36) amide, a mild insulinotropic medication [2].
In vitro, GLP-1 (9-36) amide is an antagonist of the human pancreatic GLP-1 receptor. It is the major metabolite of GLP-1 (7-36) amide formed by DPP-4 cleavage. The compound is used in research to study GLP-1 receptor pharmacology, glucose metabolism, and the role of GLP-1 metabolites in insulin secretion and appetite regulation. It can be used to block GLP-1 receptor signaling in cell-based assays to confirm the specificity of GLP-1 effects. |
| ln Vivo |
In vivo, GLP-1 (9-36) amide is the naturally occurring major metabolite of GLP-1 (7-36) amide. It circulates in the plasma and may have biological activities distinct from the parent peptide. Some studies suggest that GLP-1 (9-36) amide may have cardiovascular protective effects and may contribute to the overall effects of GLP-1-based therapies. However, as an antagonist of the GLP-1 receptor, it may also modulate the activity of endogenous GLP-1.
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| Enzyme Assay |
For in vitro receptor binding and functional assays, cells expressing the human GLP-1 receptor are treated with GLP-1 (9-36) amide at various concentrations (0.1-1000 nM) alone or in combination with GLP-1 (7-36) amide. Receptor activation is measured by quantifying cAMP accumulation using ELISA or HTRF assays. Antagonism is demonstrated by the compound's ability to inhibit GLP-1 (7-36) amide-induced cAMP production. IC50 values for antagonism can be calculated.
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| Cell Assay |
For cell-based assays, pancreatic beta cells or other GLP-1 receptor-expressing cells are treated with GLP-1 (9-36) amide at concentrations ranging from 0.1-1000 nM. Insulin secretion is measured by ELISA in response to glucose stimulation. The compound's ability to block GLP-1-induced insulin secretion can be assessed. cAMP levels, calcium mobilization, and other downstream signaling events can also be measured.
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| Animal Protocol |
For in vivo studies, animal models of diabetes or obesity would be used. GLP-1 (9-36) amide would be administered via subcutaneous or intraperitoneal injection. Blood glucose levels, insulin levels, and food intake would be measured. The compound can be used to study the physiological role of GLP-1 metabolites and to validate the specificity of GLP-1 receptor-mediated effects. However, specific in vivo protocols for GLP-1 (9-36) amide have not been detailed.
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| ADME/Pharmacokinetics |
GLP-1 (9-36) amide TFA is a peptide with a molecular weight of approximately 3100 Da. It is soluble in water and can be stored at -20°C for long-term stability. The compound is for research use only and is not intended for human or veterinary use. Standard laboratory safety precautions should be followed when handling this compound.
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| Toxicity/Toxicokinetics |
Toxicological data for GLP-1 (9-36) amide have not been extensively reported, as it is a research reagent rather than a therapeutic agent. As a naturally occurring metabolite, it is generally considered to be well-tolerated. Standard laboratory safety precautions should be followed when handling this compound. It is not intended for human use.
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| References |
[1]. Knudsen LB, et al. Glucagon-like peptide-1-(9-36) amide is a major metabolite of glucagon-like peptide-1-(7-36) amide after in vivo administration to dogs, and it acts as an antagonist on the pancreatic receptor. Eur J Pharmacol. 1996;318(2-3):429-435.
[2]. Elahi D, et al. GLP-1 (9-36) amide, cleavage product of GLP-1 (7-36) amide, is a glucoregulatory peptide. Obesity (Silver Spring). 2008;16(7):1501-1509. |
| Additional Infomation |
GLP-1 (9-36) amide TFA is the major metabolite of GLP-1 (7-36) amide generated by DPP-4 cleavage. It is an antagonist of the human GLP-1 receptor. The compound is used in research to study GLP-1 receptor signaling, glucose metabolism, and the physiological role of GLP-1 metabolites. GLP-1 (9-36) amide is a research tool and is not approved for clinical use.
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| Molecular Formula |
C140H214N36O43
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|---|---|
| Molecular Weight |
3089.41000
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| Exact Mass |
3087.57
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| CAS # |
161748-29-4
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| Related CAS # |
GLP-1(9-36)amide TFA
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| PubChem CID |
90488821
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
2.291
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| Hydrogen Bond Donor Count |
46
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| Hydrogen Bond Acceptor Count |
47
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| Rotatable Bond Count |
103
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| Heavy Atom Count |
219
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| Complexity |
7080
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| Defined Atom Stereocenter Count |
28
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| SMILES |
CCC(C)C(C(=O)NC(C)C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC(CC(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NCC(=O)NC(CCCNC(=N)N)C(=O)N)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CCC(=O)O)NC(=O)C(CCCCN)NC(=O)C(C)NC(=O)C(C)NC(=O)C(CCC(=O)N)NC(=O)CNC(=O)C(CCC(=O)O)NC(=O)C(CC(C)C)NC(=O)C(CC4=CC=C(C=C4)O)NC(=O)C(CO)NC(=O)C(CO)NC(=O)C(C(C)C)NC(=O)C(CC(=O)O)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C(CC5=CC=CC=C5)NC(=O)C(C(C)O)NC(=O)CNC(=O)C(CCC(=O)O)N
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| InChi Key |
WPNGPBPCQMDAAD-WRFZDFFOSA-N
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| InChi Code |
InChI=1S/C140H214N36O43/c1-16-72(10)112(137(217)155-75(13)118(198)162-97(59-81-61-149-85-35-24-23-34-83(81)85)127(207)164-93(55-69(4)5)128(208)173-110(70(6)7)135(215)161-87(36-25-27-51-141)120(200)151-62-103(184)156-86(115(145)195)38-29-53-148-140(146)147)175-129(209)95(56-78-30-19-17-20-31-78)165-124(204)91(46-50-108(191)192)160-123(203)88(37-26-28-52-142)158-117(197)74(12)153-116(196)73(11)154-122(202)90(44-47-102(144)183)157-104(185)63-152-121(201)89(45-49-107(189)190)159-125(205)92(54-68(2)3)163-126(206)94(58-80-39-41-82(182)42-40-80)166-132(212)99(65-177)169-134(214)101(67-179)170-136(216)111(71(8)9)174-131(211)98(60-109(193)194)167-133(213)100(66-178)171-139(219)114(77(15)181)176-130(210)96(57-79-32-21-18-22-33-79)168-138(218)113(76(14)180)172-105(186)64-150-119(199)84(143)43-48-106(187)188/h17-24,30-35,39-42,61,68-77,84,86-101,110-114,149,177-182H,16,25-29,36-38,43-60,62-67,141-143H2,1-15H3,(H2,144,183)(H2,145,195)(H,150,199)(H,151,200)(H,152,201)(H,153,196)(H,154,202)(H,155,217)(H,156,184)(H,157,185)(H,158,197)(H,159,205)(H,160,203)(H,161,215)(H,162,198)(H,163,206)(H,164,207)(H,165,204)(H,166,212)(H,167,213)(H,168,218)(H,169,214)(H,170,216)(H,171,219)(H,172,186)(H,173,208)(H,174,211)(H,175,209)(H,176,210)(H,187,188)(H,189,190)(H,191,192)(H,193,194)(H4,146,147,148)/t72-,73-,74-,75-,76+,77+,84-,86-,87-,88-,89-,90-,91-,92-,93-,94-,95-,96-,97-,98-,99-,100-,101-,110-,111-,112-,113-,114-/m0/s1
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| Chemical Name |
(4S)-4-amino-5-[[2-[[(2S,3R)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-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]-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, avoid exposure to moisture. |
| 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 : ≥ 25 mg/mL (~8.09 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.3237 mL | 1.6184 mL | 3.2369 mL | |
| 5 mM | 0.0647 mL | 0.3237 mL | 0.6474 mL | |
| 10 mM | 0.0324 mL | 0.1618 mL | 0.3237 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.
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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