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| Targets |
GLP-1(7-37) targets the GLP-1 receptor (GLP-1R), a class B G protein-coupled receptor (GPCR) that is expressed on pancreatic beta cells, as well as on other tissues including the brain, heart, and gastrointestinal tract. By binding to GLP-1R, GLP-1(7-37) activates the Gs protein, which stimulates adenylyl cyclase to produce cAMP. The increase in cAMP activates protein kinase A (PKA) and exchange protein directly activated by cAMP (Epac), which enhances glucose-stimulated insulin secretion from pancreatic beta cells. In addition to its effects on insulin secretion, GLP-1(7-37) also promotes beta cell proliferation and survival, inhibits glucagon secretion from alpha cells, slows gastric emptying, and reduces appetite. These effects make GLP-1(7-37) a key regulator of glucose homeostasis and a target for the treatment of type 2 diabetes and obesity. The peptide's effects are glucose-dependent, meaning that it only stimulates insulin secretion when blood glucose levels are elevated, reducing the risk of hypoglycemia.
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| ln Vitro |
In vitro studies have demonstrated that GLP-1(7-37) is a potent stimulator of insulin secretion in pancreatic beta cell lines (e.g., INS-1, MIN6, or primary human islets). In these assays, treatment with GLP-1(7-37) at concentrations of 0.001-100 nM increases glucose-stimulated insulin secretion in a concentration-dependent manner, with an EC₅₀ of approximately 0.9 nM. The peptide's effects are mediated through the activation of the GLP-1R and the subsequent activation of the cAMP/PKA and Epac pathways. In addition to its effects on insulin secretion, GLP-1(7-37) has been shown to promote beta cell proliferation and to protect beta cells from apoptosis induced by cytokines or glucotoxicity. In neuronal cell cultures, GLP-1(7-37) has been shown to have neuroprotective effects, reducing excitotoxicity and oxidative stress. In cell viability assays, GLP-1(7-37) does not exhibit significant cytotoxicity at concentrations up to 1 µM, indicating a favorable safety profile for in vitro applications.
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| ln Vivo |
GLP-1(7-37) (0.5, 5 or 50 pmol/min/kg) rats exhibit a dose-related enhancement of the glucose-stimulated rise in plasma insulin concentration and an increased rate of glucose infusion when infused during the second hour of a two-hour 11-mM hyperglycemic clamp[2]. Rats infused with GLP-1(7-37) (5 pmol/min/kg) for 1–7 hours experience a sustained increase in plasma insulin concentration compared to rats infused with vehicle, provided that the rats' glucose concentration remains at 11 mM[2].
In vivo studies have demonstrated the insulinotropic effects of GLP-1(7-37) in animal models and in humans. In rodent models of type 2 diabetes, intravenous or subcutaneous administration of GLP-1(7-37) at doses of 1-100 µg/kg significantly reduces blood glucose levels and enhances glucose-stimulated insulin secretion. In clinical studies, infusion of GLP-1(7-37) in patients with type 2 diabetes improves glycemic control, reduces HbA1c, and promotes weight loss. The peptide's effects are dose-dependent, and its short half-life (approximately 1-2 minutes) limits its therapeutic utility, necessitating the development of longer-acting GLP-1 receptor agonists such as exenatide, liraglutide, and semaglutide. GLP-1(7-37) is used as a research tool for studying GLP-1 receptor signaling and for the development of new GLP-1-based therapies. |
| Enzyme Assay |
For in vitro receptor binding and signaling assays, GLP-1(7-37) is typically evaluated for its ability to bind to the GLP-1 receptor and to activate downstream signaling pathways. For receptor binding assays, membrane preparations from cells expressing the human GLP-1R (e.g., HEK293-GLP-1R) are incubated with varying concentrations of GLP-1(7-37) (0.01 nM-10 µM) and a fixed concentration of a radiolabeled GLP-1 analog (e.g., ¹²⁵I-GLP-1) in binding buffer for 1-2 hours at room temperature. Non-specific binding is determined in the presence of a 100- to 1000-fold excess of unlabeled GLP-1. Bound and free ligand are separated by filtration, and the radioactivity is measured. The binding affinity (Ki) is calculated from competition curves. For functional assays, cells expressing the GLP-1R are treated with GLP-1(7-37), and cAMP accumulation is measured using a competitive ELISA or a FRET-based biosensor. The EC₅₀ for cAMP production is determined from dose-response curves. For insulin secretion assays, beta cells or islets are treated with GLP-1(7-37) and glucose, and insulin secretion is measured by ELISA or radioimmunoassay. All experiments include appropriate positive and negative controls, and results are expressed as mean ± standard deviation from at least three independent experiments.
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| Cell Assay |
For in vitro cell-based assays, GLP-1(7-37) is evaluated for its effects on insulin secretion, cell proliferation, and apoptosis in beta cell lines. Cells (e.g., INS-1, MIN6) are seeded in 24- or 96-well plates and treated with the peptide at concentrations of 0.001-100 nM in the presence of glucose (5-20 mM) for 1-4 hours. Insulin secretion is measured by ELISA. For cell proliferation assays, cells are treated with the peptide for 24-72 hours, and cell proliferation is measured using BrdU incorporation or MTT assays. For apoptosis assays, cells are treated with cytokines (IL-1β, TNF-α, IFN-γ) or glucotoxic conditions (high glucose, palmitate) in the presence or absence of GLP-1(7-37), and apoptosis is assessed by flow cytometry using Annexin V-FITC/PI staining or by measuring caspase-3/7 activity. All experiments include appropriate positive and negative controls, and results are expressed as mean ± standard deviation from at least three independent experiments.
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| Animal Protocol |
Male Sprague-Dawley rats weighing 300 to 350 g with maintained plasma glucose concentration at 11 mM
0.5, 5 or 50 pmol/min/kg IV during the second hour of a 2-hour 11-mmol/L hyperglycemic clamp. For in vivo animal experiments, GLP-1(7-37) is typically administered intravenously or subcutaneously to mice or rats. For glucose tolerance tests, animals are fasted overnight and then administered the peptide (1-100 µg/kg) 30-60 minutes prior to an oral or intraperitoneal glucose challenge (1-2 g/kg). Blood glucose levels are measured at various time points (0, 15, 30, 60, 90, 120 minutes), and insulin levels are measured in plasma samples. For chronic studies, the peptide is administered via continuous infusion using osmotic minipumps, and glycemic control, body weight, and food intake are monitored. For pharmacokinetic studies, blood samples are collected at various time points, and plasma concentrations of GLP-1(7-37) are measured by ELISA or LC-MS. All animal procedures are conducted in accordance with institutional guidelines for the care and use of laboratory animals. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for GLP-1(7-37) indicate that the peptide has a very short half-life in circulation. The compound has a molecular weight of 3355.67 g/mol and a molecular formula of C₁₅₁H₂₂₈N₄₀O₄₇. Following intravenous administration, GLP-1(7-37) is rapidly cleared from the circulation, with a half-life of approximately 1-2 minutes, due to degradation by the enzyme dipeptidyl peptidase-4 (DPP-4) and renal clearance. The peptide's short half-life limits its therapeutic utility, and longer-acting GLP-1 receptor agonists have been developed to overcome this limitation. The peptide is stable when stored as a powder at -20°C, protected from light and moisture. For in vivo administration, GLP-1(7-37) can be formulated in saline or other suitable vehicles.
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| Toxicity/Toxicokinetics |
GLP-1(7-37) is generally well-tolerated at the concentrations used in research applications. In animal studies, the peptide does not exhibit significant toxicity at doses up to 100 µg/kg. However, higher doses may cause gastrointestinal side effects, including nausea and vomiting, which are consistent with the known effects of GLP-1 receptor agonists. As with all research chemicals, appropriate safety precautions should be taken when handling GLP-1(7-37), including the use of personal protective equipment and working in a well-ventilated area. The peptide is for research use only and is not intended for human therapeutic use.
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| References |
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| Additional Infomation |
During pancreatic perfusion, it is a potent stimulant for insulin release; it is co-encoded by the glucagon gene.
GLP-1(7-37) is a research-use only compound and has not been approved for clinical applications as a therapeutic agent, although GLP-1 receptor agonists derived from it are FDA-approved for the treatment of type 2 diabetes and obesity. It is also known as glucagon-like peptide-1 (7-37). The compound has a molecular formula of C₁₅₁H₂₂₈N₄₀O₄₇ and a molecular weight of 3355.67 g/mol. GLP-1(7-37) is a 31-amino acid peptide hormone that is an endogenous GLP-1 receptor ligand and a potent insulinotropic hormone. The compound is used for the study of GLP-1 receptor signaling, glucose metabolism, and the development of therapies for type 2 diabetes and obesity. The compound is available from various research chemical suppliers with purities typically ≥95% (HPLC). Storage recommendations include keeping the peptide in a tightly sealed container, protected from light and moisture, at -20°C. |
| Molecular Formula |
C₁₅₁H₂₂₈N₄₀O₄₇
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|---|---|
| Molecular Weight |
3355.67
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| Exact Mass |
3353.667
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| CAS # |
106612-94-6
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| Related CAS # |
GLP-1(7-37) acetate; 1450806-98-0
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| PubChem CID |
16133830
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.660
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| LogP |
-3.86
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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 |
111
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| Heavy Atom Count |
238
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| Complexity |
7820
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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)NCC(=O)O)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=CNC=N6)N
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| InChi Key |
GCYXWQUSHADNBF-AAEALURTSA-N
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| InChi Code |
InChI=1S/C151H228N40O47/c1-17-77(10)121(148(236)169-81(14)127(215)177-105(60-87-63-160-92-36-25-24-35-90(87)92)138(226)179-101(56-74(4)5)139(227)188-119(75(6)7)146(234)176-94(37-26-28-52-152)130(218)161-65-111(199)170-93(39-30-54-159-151(156)157)129(217)164-68-118(210)211)190-140(228)103(57-84-31-20-18-21-32-84)180-135(223)99(47-51-116(206)207)175-134(222)95(38-27-29-53-153)172-125(213)79(12)166-124(212)78(11)168-133(221)98(44-48-110(155)198)171-112(200)66-162-132(220)97(46-50-115(204)205)174-136(224)100(55-73(2)3)178-137(225)102(59-86-40-42-89(197)43-41-86)181-143(231)107(69-192)184-145(233)109(71-194)185-147(235)120(76(8)9)189-142(230)106(62-117(208)209)182-144(232)108(70-193)186-150(238)123(83(16)196)191-141(229)104(58-85-33-22-19-23-34-85)183-149(237)122(82(15)195)187-113(201)67-163-131(219)96(45-49-114(202)203)173-126(214)80(13)167-128(216)91(154)61-88-64-158-72-165-88/h18-25,31-36,40-43,63-64,72-83,91,93-109,119-123,160,192-197H,17,26-30,37-39,44-62,65-71,152-154H2,1-16H3,(H2,155,198)(H,158,165)(H,161,218)(H,162,220)(H,163,219)(H,164,217)(H,166,212)(H,167,216)(H,168,221)(H,169,236)(H,170,199)(H,171,200)(H,172,213)(H,173,214)(H,174,224)(H,175,222)(H,176,234)(H,177,215)(H,178,225)(H,179,226)(H,180,223)(H,181,231)(H,182,232)(H,183,237)(H,184,233)(H,185,235)(H,186,238)(H,187,201)(H,188,227)(H,189,230)(H,190,228)(H,191,229)(H,202,203)(H,204,205)(H,206,207)(H,208,209)(H,210,211)(H4,156,157,159)/t77-,78-,79-,80-,81-,82+,83+,91-,93-,94-,95-,96-,97-,98-,99-,100-,101-,102-,103-,104-,105-,106-,107-,108-,109-,119-,120-,121-,122-,123-/m0/s1
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| Chemical Name |
(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)-5-carbamimidamido-1-(carboxymethylamino)-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-4-yl)propanoyl]amino]propanoyl]amino]-5-oxopentanoic acid
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| Synonyms |
InsulinotropinTglp-1 GLP-1 (7-37); peptide Glucagon like Peptide-1 (7-37) Acetate
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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) |
0.1 M HCL: ≥ 50 mg/mL (~14.9 mM)
80% Acetic acid/water: ≥ 10 mg/mL (~3 mM) H2O: < 0.1 mg/mL |
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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 | 0.2980 mL | 1.4900 mL | 2.9800 mL | |
| 5 mM | 0.0596 mL | 0.2980 mL | 0.5960 mL | |
| 10 mM | 0.0298 mL | 0.1490 mL | 0.2980 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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