| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
GLP-1(7-36) Acetate targets the GLP-1 receptor (GLP-1R), a G protein-coupled receptor expressed on pancreatic β-cells, as well as on other tissues including brain, heart, and gastrointestinal tract. When GLP-1 binds to its receptors on β-cells, it initiates a signaling cascade that increases intracellular cAMP, leading to enhanced insulin exocytosis. The peptide also inhibits glucagon secretion from pancreatic α-cells when glucose levels are high, contributing to glucose homeostasis.
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| ln Vitro |
The contents of amide acetate and active GLP-1(7-36) in the culture medium were significantly greater in the cells treated with phorbol 12-myristate 13-acetate for two hours than in the control group. Additionally, a dose-dependent increase in active GLP-1 production from cells was seen upon glucose administration. GLP-1 is actively secreted by cells in response to dose-dependent stimulation by palmitic acid, oleic acid, linoleic acid, or linolenic acid. Unsaturated fatty acids like oleic, linoleic, and linolenic acid secreted substantially more GLP-1 when active than palmitic acid. The amount of active GLP-1 in the culture media rose dose-dependently when CPE was added to NCI-H716 cells. These cells secreted 37 percent more active GLP-1 at a dose of 0.1% CPE [1].
In vitro, cells treated with phorbol 12-myristate 13-acetate for 2 hours show significantly higher active GLP-1(7-36) concentrations in the media compared to controls. The peptide activates the GLP-1 receptor, promoting insulin secretion and inhibiting glucagon secretion. It has been shown to stimulate glucose-induced insulin secretion from β-cells in various cell culture models. The compound's ability to activate GLP-1R and increase cAMP levels has been extensively characterized. |
| ln Vivo |
Gastric administration of glucose increased active GLP-1(7-36) amide levels in portal blood 10 minutes later, followed by a significant decrease at 30 minutes. When TO was administered gastrically, active GLP-1 levels rose after 10 minutes and fell to basal levels after 60 minutes. Individually, glucose and TO increased GLP-1 secretion in a dose-dependent manner. Furthermore, co-administration of glucose and TO further increased peak GLP-1 levels. Mice given CPE had higher levels of active GLP-1 in portal blood at 10 and 30 minutes compared with control mice. When glucose was administered with CPE, the levels of active GLP-1 and insulin in the portal blood of mice administered CPE were slightly higher than those of control mice. C57BL/6J mice fed a high-fat diet develop hyperglycemia and impaired glucose tolerance [1].
In vivo, GLP-1(7-36) Acetate is the active form of GLP-1 that regulates glucose metabolism. It lowers blood glucose after meals by stimulating insulin secretion and inhibiting glucagon secretion. The peptide has a very short half-life due to rapid degradation by dipeptidyl peptidase-4 (DPP-4). It has shown potential for treating type 2 diabetes mellitus and obesity. GLP-1 receptor agonists based on this peptide are approved for diabetes treatment. |
| Enzyme Assay |
For non-cell enzyme/receptor binding assays, GLP-1(7-36) Acetate binding to GLP-1 receptor can be assessed using membrane preparations from cells expressing the receptor. Radioligand binding assays using [¹²⁵I]-labeled GLP-1 or fluorescently labeled GLP-1 analogues are employed. Membrane fractions are incubated with the labeled ligand and varying concentrations of unlabeled peptide. Bound and free ligand are separated by filtration, and binding affinity (Kd) is calculated from saturation and competition binding experiments.
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| Cell Assay |
For in vitro cell-based assays, GLP-1(7-36) Acetate is tested in pancreatic β-cell lines or primary islet cells. Cells are treated with the peptide, and insulin secretion is measured by ELISA or RIA. cAMP accumulation is measured using immunoassays. The peptide's effects on cell proliferation and survival can also be assessed. The compound is extensively used in studies of glucose metabolism and insulin signaling. Cells treated with phorbol 12-myristate 13-acetate show increased GLP-1(7-36) levels.
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| Animal Protocol |
For in vivo animal experiments, GLP-1(7-36) Acetate is typically administered intravenously or subcutaneously to rodent models. Blood glucose levels and insulin concentrations are measured at various time points following administration. Glucose tolerance tests are performed to assess the peptide's effects on glucose homeostasis. The peptide's effects on food intake and body weight can also be studied in obesity models. Due to its short half-life, continuous infusion or DPP-4 inhibitors may be used.
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| ADME/Pharmacokinetics |
GLP-1(7-36) Acetate has a molecular weight of approximately 3357.73 g/mol and molecular formula C₁₅₁H₂₃₀N₄₀O₄₇. It is a peptide consisting of 30 amino acids (positions 7-36 of full-length GLP-1). The compound is supplied as a lyophilized powder with purity ≥95% for research purposes. It should be stored at -20°C for long-term stability. The peptide is soluble in water and other aqueous buffers.
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| Toxicity/Toxicokinetics |
GLP-1(7-36) Acetate is a peptide for research use only and is not approved for human therapeutic use in its synthetic form. However, GLP-1 receptor agonists based on this peptide (e.g., exenatide, liraglutide, semaglutide) are approved for the treatment of type 2 diabetes and obesity. The native peptide has a very short half-life due to DPP-4 degradation, limiting its therapeutic utility. Standard safety precautions for handling peptides should be followed.
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| References | |
| Additional Infomation |
GLP-1(7-36) Acetate is the active form of the incretin hormone GLP-1, which is secreted by intestinal L-cells in response to nutrient intake. It plays a crucial role in glucose homeostasis by stimulating insulin secretion and inhibiting glucagon secretion. GLP-1 receptor agonists are a major class of drugs for type 2 diabetes and obesity. The peptide is extensively used in research on metabolic pathways and receptor interactions. No clinical trials are ongoing for the synthetic acetate form as it has been superseded by stabilized analogues.
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| Molecular Formula |
C149H226N40O45(C2H4O2)N
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| Exact Mass |
3356.687
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| CAS # |
1119517-19-9
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| Related CAS # |
GLP-1(7-36), amide TFA;GLP-1(7-36), amide;107444-51-9
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| PubChem CID |
166638343
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
50
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| Hydrogen Bond Acceptor Count |
52
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| Rotatable Bond Count |
109
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| Heavy Atom Count |
238
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| Complexity |
7690
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| Defined Atom Stereocenter Count |
30
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| SMILES |
CC[C@H](C)[C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CC1=CNC2=CC=CC=C21)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)N)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC4=CC=C(C=C4)O)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC5=CC=CC=C5)NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CC6=CN=CN6)N.CC(=O)O
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| InChi Key |
BCNDXSMWLGNKFT-AMEUXXCWSA-N
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| InChi Code |
InChI=1S/C149H226N40O45.C2H4O2/c1-17-76(10)119(146(232)167-80(14)126(212)175-104(60-86-63-159-91-36-25-24-35-89(86)91)136(222)177-100(56-73(4)5)137(223)186-117(74(6)7)144(230)174-93(37-26-28-52-150)128(214)160-65-110(197)168-92(122(154)208)39-30-54-158-149(155)156)188-138(224)102(57-83-31-20-18-21-32-83)178-133(219)98(47-51-115(204)205)173-132(218)94(38-27-29-53-151)170-124(210)78(12)164-123(209)77(11)166-131(217)97(44-48-109(153)196)169-111(198)66-161-130(216)96(46-50-114(202)203)172-134(220)99(55-72(2)3)176-135(221)101(59-85-40-42-88(195)43-41-85)179-141(227)106(68-190)182-143(229)108(70-192)183-145(231)118(75(8)9)187-140(226)105(62-116(206)207)180-142(228)107(69-191)184-148(234)121(82(16)194)189-139(225)103(58-84-33-22-19-23-34-84)181-147(233)120(81(15)193)185-112(199)67-162-129(215)95(45-49-113(200)201)171-125(211)79(13)165-127(213)90(152)61-87-64-157-71-163-87;1-2(3)4/h18-25,31-36,40-43,63-64,71-82,90,92-108,117-121,159,190-195H,17,26-30,37-39,44-62,65-70,150-152H2,1-16H3,(H2,153,196)(H2,154,208)(H,157,163)(H,160,214)(H,161,216)(H,162,215)(H,164,209)(H,165,213)(H,166,217)(H,167,232)(H,168,197)(H,169,198)(H,170,210)(H,171,211)(H,172,220)(H,173,218)(H,174,230)(H,175,212)(H,176,221)(H,177,222)(H,178,219)(H,179,227)(H,180,228)(H,181,233)(H,182,229)(H,183,231)(H,184,234)(H,185,199)(H,186,223)(H,187,226)(H,188,224)(H,189,225)(H,200,201)(H,202,203)(H,204,205)(H,206,207)(H4,155,156,158);1H3,(H,3,4)/t76-,77-,78-,79-,80-,81+,82+,90-,92-,93-,94-,95-,96-,97-,98-,99-,100-,101-,102-,103-,104-,105-,106-,107-,108-,117-,118-,119-,120-,121-;/m0./s1
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| Chemical Name |
acetic acid;(4S)-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]-4-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]propanoyl]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 : ≥ 100 mg/mL
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| Solubility (In Vivo) |
Solubility in Formulation 1: 25 mg/mL (Infinity mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(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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