Enterostatin, human, mouse, rat is a novel and potent pentapeptide that can reduce the intake of fat. Enterostatin is a pentapeptide generated by trypic digestion of procolipase in the small intestine. Both peripheral and central administration of this peptide to rats has been shown to reduce food intake, this reduction being due to specific suppression of fat intake

Physicochemical Properties

Molecular Formula	C₂₁H₃₆N₈O₆
Molecular Weight	496.56
Exact Mass	496.276
CAS #	117830-79-2
PubChem CID	3082883
Appearance	White to off-white solid powder
Density	1.54g/cm3
Index of Refraction	1.681
LogP	-5
Hydrogen Bond Donor Count	6
Hydrogen Bond Acceptor Count	8
Rotatable Bond Count	11
Heavy Atom Count	35
Complexity	846
Defined Atom Stereocenter Count	4
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
InChi Key	ITZMJCSORYKOSI-AJNGGQMLSA-N
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
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
HS Tariff Code	2934.99.9001
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)

Biological Activity

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].
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].
References	[1]. Effect of enterostatin on insulin, glucagon, and somatostatin secretion in the perfused rat pancreas. Diabetes. 1996 Sep;45(9):1157-60. [2]. Enterostatin--a peptide regulating fat intake. Obes Res. 1997 Jul;5(4):360-72. [3]. Enterostatin (APGPR) enhances memory consolidation in mice. Peptides. 2007 Mar;28(3):719-21. [4]. Enterostatin: a gut-brain peptide regulating fat intake in rat. J Physiol Paris. 1993;87(4):273-5.
Additional Infomation	APGPR Enterostatin is a peptide.

Solubility Data

Solubility (In Vitro)

DMSO : ~125 mg/mL (~251.73 mM)

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.