| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg | |||
| 50mg | |||
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| Other Sizes |
| Targets |
The exact molecular target of Enterostatin is not fully characterized, but it has been shown to bind to the F1-ATPase β subunit. Enterostatin also acts in a CCK-1 receptor-dependent manner. It functions as an endogenous anorexigenic peptide that regulates dietary fat intake and inhibits insulin secretion. The peptide may mediate its effects through both central and peripheral mechanisms, influencing appetite and lipid utilization.
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| ln Vitro |
Enterostatin suppresses the insulin response in the perfused rat pancreas by 70% at 100 mM, 40% at 0.1 mM tolbutamide, and 70% at 5 mM arginine[1].
In vitro, Enterostatin suppresses the insulin response in the perfused rat pancreas. At 100 mM, it suppresses insulin secretion by 70%; at 0.1 mM with tolbutamide, it suppresses by 40%; and at 5 mM with arginine, it suppresses by 70%. The peptide reduces fat intake and modulates metabolic processes. Its effects are mediated through binding to the F1-ATPase β subunit and through CCK-1 receptor-dependent mechanisms. Enterostatin is a highly conserved pentapeptide across mammalian species. |
| ln Vivo |
Enterostatin decreases body weight, body fat, and fat consumption over time. Enterostatin's various metabolic effects, such as decreased insulin secretion, increased sympathetic drive to brown adipose tissue, and stimulated adrenal corticosteroid secretion, may be involved in this response[2]. In a step-through type passive avoidance test in mice, enterostatin improves memory consolidation following central or oral treatment at a level of 10 nmol/mouse or 300 mg/kg, respectively[3]. Enterostatin at 38 nmol significantly reduces the amount of high-fat foods consumed; but, by 76 nmol, the inhibitory effect is no longer there. There is also a minor increase in food intake within the first hour following enterostatin injection[4].
In vivo, Enterostatin decreases body weight, body fat, and fat consumption over time. Its metabolic effects include decreased insulin secretion, increased sympathetic drive to brown adipose tissue, and stimulated adrenal corticosteroid secretion. The peptide acts through both central and peripheral mechanisms to influence appetite and lipid utilization. Chronic administration reduces fat intake and body weight, suggesting potential applications in obesity research. |
| Enzyme Assay |
In vitro receptor binding assays for Enterostatin are performed using membrane preparations or purified proteins. Binding to the F1-ATPase β subunit can be assessed using surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC). The peptide is incubated with the target protein in appropriate buffer systems, and binding affinity (Kd) is determined. For CCK-1 receptor binding, competition binding assays with radiolabeled CCK can be performed using membrane preparations from cells expressing CCK-1 receptors. Nonspecific binding is determined using excess unlabeled ligand.
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| Cell Assay |
Cell-based assays for Enterostatin include evaluation of insulin secretion inhibition using pancreatic islet or perfused pancreas models. Rat pancreas is perfused with buffer containing glucose and test agents. Enterostatin is added at varying concentrations, and insulin secretion is measured by radioimmunoassay or ELISA. The compound suppresses insulin secretion in a concentration-dependent manner. For appetite regulation studies, neuronal cell lines expressing relevant receptors may be used to evaluate downstream signaling pathways. The peptide's effects on cAMP, calcium, or ERK signaling can be measured.
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| Animal Protocol |
In animal studies, Enterostatin is typically administered via intraperitoneal or intracerebroventricular injection to rodents. For feeding studies, rats or mice are injected with Enterostatin (doses ranging from 0.1-10 mg/kg) and food intake is measured over 1-24 hours. For chronic studies, the peptide is administered daily for 1-4 weeks, and body weight, body fat, and food intake are monitored. Insulin levels, glucose tolerance, and metabolic parameters may be assessed. Endpoints include food intake, body weight, body fat composition, insulin secretion, and adrenal corticosteroid levels.
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| ADME/Pharmacokinetics |
Enterostatin is a pentapeptide with a molecular weight of 496.56 and molecular formula C21H36N8O6. As a peptide, it is susceptible to proteolytic degradation in vivo, which may limit its half-life. The compound should be stored as powder at -20°C for up to 3 years. It is soluble in aqueous buffers. For in vivo administration, solutions should be prepared fresh and used immediately. The peptide is stable when stored under appropriate conditions. Further pharmacokinetic studies including plasma half-life, clearance, and tissue distribution would be valuable for in vivo applications.
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| Toxicity/Toxicokinetics |
No specific toxicity data are documented for Enterostatin. As an endogenous peptide derived from procolipase, it is naturally produced in the body and is generally well-tolerated at physiological concentrations. In research settings, standard laboratory safety practices should be followed when handling the peptide. The compound is intended for research use only and is not approved for human therapeutic applications. Toxicity profiling would be required for any therapeutic development.
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| References | |
| Additional Infomation |
APGPR cholestatin is a peptide.
Enterostatin (human, mouse, rat) is a pentapeptide with the sequence Val-Pro-Asp-Pro-Arg. It is derived from the N-terminal region of procolipase, a precursor protein involved in lipid digestion. The peptide is highly conserved across mammalian species. It has been extensively studied for its regulatory role in appetite control and fat metabolism. Enterostatin is an endogenous anorexigenic peptide that regulates dietary fat intake and inhibits insulin secretion. It is commonly used in metabolic and obesity research. The compound is for research use only. |
| Molecular Formula |
C₂₁H₃₆N₈O₆
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|---|---|
| Molecular Weight |
496.56
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| Exact Mass |
496.276
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| CAS # |
117830-79-2
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| PubChem CID |
3082883
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| Appearance |
White to off-white solid powder
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| Density |
1.54g/cm3
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| Index of Refraction |
1.681
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| LogP |
-5
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
35
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| Complexity |
846
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C[C@@H](C(=O)N1CCC[C@H]1C(=O)NCC(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)N
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| InChi Key |
ITZMJCSORYKOSI-AJNGGQMLSA-N
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| InChi Code |
InChI=1S/C21H36N8O6/c1-12(22)19(33)29-10-4-6-14(29)17(31)26-11-16(30)28-9-3-7-15(28)18(32)27-13(20(34)35)5-2-8-25-21(23)24/h12-15H,2-11,22H2,1H3,(H,26,31)(H,27,32)(H,34,35)(H4,23,24,25)/t12-,13-,14-,15-/m0/s1
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| Chemical Name |
(2S)-2-[[(2S)-1-[2-[[(2S)-1-[(2S)-2-aminopropanoyl]pyrrolidine-2-carbonyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic 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) |
DMSO : ~125 mg/mL (~251.73 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.19 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.19 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0139 mL | 10.0693 mL | 20.1386 mL | |
| 5 mM | 0.4028 mL | 2.0139 mL | 4.0277 mL | |
| 10 mM | 0.2014 mL | 1.0069 mL | 2.0139 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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