![Insulinotropin acetate [GLP-1 (7-37)]](/upload/1124/V16459.png)
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| 1mg |
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| 2mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| Other Sizes |
| Targets |
Insulinotropin acetate targets the glucagon-like peptide-1 (GLP-1) receptor, a G protein-coupled receptor expressed on pancreatic beta cells. By binding to and activating this receptor, it stimulates insulin secretion in a glucose-dependent manner. This mechanism enhances glucose-induced insulin release, making it a potential therapeutic agent for type 2 diabetes. It is an intestinal insulinotropic hormone.
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| ln Vitro |
Insulinotropin acetate augments glucose-induced insulin secretion. It is an intestinal insulinotropic hormone. Its in vitro activity is characterized by its ability to stimulate insulin release from pancreatic beta cells in a glucose-dependent manner. It is a potent stimulator of insulin secretion.
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| ln Vivo |
GLP-1(7-37) (0.5, 5 or 50 pmol/min/kg) administered to rats during the second hour of a two-hour 11-mM hyperglycemic clamp results in an increased rate of glucose infusion and a dose-related enhancement of the glucose-stimulated increase in plasma insulin concentration[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, Insulinotropin acetate has been shown to augment glucose-induced insulin secretion. It has potential anti-diabetic effects. In animal studies, GLP-1(7-37) has been administered at doses of 0.5, 5, or 50 pmol/min/kg to evaluate its effects on insulin secretion and glucose metabolism. Its efficacy in improving glycemic control has been demonstrated in preclinical models. |
| Enzyme Assay |
In vitro receptor binding assays for Insulinotropin acetate measure its affinity for the GLP-1 receptor. The receptor is incubated with a radiolabeled ligand and varying concentrations of the compound, and displacement is measured to determine binding affinity (Ki). Functional assays assess its agonist activity by measuring cAMP accumulation or insulin secretion in cells expressing the receptor.
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| Cell Assay |
In vitro cellular assays for Insulinotropin acetate involve treating pancreatic beta cell lines (e.g., INS-1, MIN6) or isolated pancreatic islets with the compound and measuring insulin secretion by ELISA or radioimmunoassay. Its effects on cell signaling, such as cAMP production and calcium mobilization, are also assessed. Its effects on cell proliferation and survival can be studied.
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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. In vivo animal models for Insulinotropin acetate include rodent models of type 2 diabetes to evaluate its effects on glucose tolerance and insulin secretion. Animals are treated with the compound, and blood glucose and insulin levels are measured during glucose tolerance tests. Its effects on pancreatic islet function and beta cell mass can be assessed histologically. |
| ADME/Pharmacokinetics |
Insulinotropin acetate is a peptide and is typically administered by injection. It has a short half-life due to rapid degradation by dipeptidyl peptidase-4 (DPP-4) and other proteases. Its pharmacokinetics are characterized by rapid clearance. It is not orally bioavailable and requires parenteral administration for therapeutic use.
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| Toxicity/Toxicokinetics |
The toxicological profile of Insulinotropin acetate is characteristic of GLP-1 receptor agonists. Common side effects may include gastrointestinal disturbances, such as nausea and vomiting. It may also cause hypoglycemia when used in combination with other anti-diabetic agents. Its safety has been evaluated in preclinical and clinical studies.
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| References |
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| Additional Infomation |
Insulinotropin acetate is the acetate salt of GLP-1 (7-37), an intestinal insulinotropic hormone. It stimulates insulin secretion and augments glucose-induced insulin release. It has potential anti-diabetic effects. It is a research compound used to study glucose metabolism and insulin secretion. It is also known as Tglp-1.
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| Exact Mass |
3354.671
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| CAS # |
1450806-98-0
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| Related CAS # |
GLP-1(7-37); 106612-94-6
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| PubChem CID |
16133830
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
-14.2
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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 |
Insulinotropin 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) |
H2O: ~50 mg/mL (~14.6 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 12.5 mg/mL (3.66 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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