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Spinorphin
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Spinorphin图片
CAS NO:137201-62-8
包装:1mg
市场价:1985元

产品介绍
Spinorphin 是脑啡肽降解酶的抑制剂。
Cas No.137201-62-8
别名LVV-hemorphin-4
化学名2-(2-(1-(2-(2-(2-(2-amino-4-methylpentanamido)-3-methylbutanamido)-3-methylbutanamido)-3-(4-hydroxyphenyl)propanoyl)pyrrolidine-2-carboxamido)-3-(1H-indol-3-yl)propanamido)-3-hydroxybutanoic acid
Canonical SMILESCC(C)CC(C(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NC(CC1=CC=C(C=C1)O)C(=O)N2CCCC2C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NC(C(C)O)C(=O)O)N
分子式C45H64N8O10
分子量877.05
溶解度DMF: 30 mg/ml,DMSO: 30 mg/ml
储存条件Desiccate at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Spinorphin is an endogenous inhibitor of enkephalin-degrading enzymes (aminopeptidase, dipeptidyl aminopeptidase III, angiotensin-converting enzyme and enkephalinase) [1]. Also, it is a potent antagonist of human P2X3 receptor and the N-formylpeptide receptor subtype FPR with IC50 value of 8.3 pM for P2X3 receptor[2][3].

Enkephalin degrading enzymes are a series of enzymes that hydrolyze enkephalins, which play an important role in management of blood pressure, pain, hypertension and cardiovascular diseases.

In human embryonic kidney (HEK) 293 cells transfected with mouse FPR, spinorphin induced a typical rise in the intracellular Ca2+ concentration with EC50 of 128 μM. Also, in normal mouse neutrophils, Spinorphin induced calcium flux in a dose-dependent way. While the neutrophils from mice deficient in the fMLF receptor subtype FPR didn’t response [3].

In mice, intrathecal administration of spinorphin inhibited the allodynia induced by intrathecal nociceptin in a dose-dependent way. Furthermore, spinorphin enhanced the inhibitory effect of enkephalin on allodynia induced by nociceptin [4].

References:
[1].  Nishimura K, Hazato T. Isolation and identification of an endogenous inhibitor of enkephalin-degrading enzymes from bovine spinal cord. Biochem Biophys Res Commun, 1993, 194(2): 713-719.
[2].  Jung KY, Moon HD, Lee GE, et al. Structure-activity relationship studies of spinorphin as a potent and selective human P2X(3) receptor antagonist. J Med Chem, 2007, 50(18): 4543-4547.
[3].  Liang TS, Gao JL, Fatemi O, et al. The endogenous opioid spinorphin blocks fMet-Leu-Phe-induced neutrophil chemotaxis by acting as a specific antagonist at the N-formylpeptide receptor subtype FPR. J Immunol, 2001, 167(11): 6609-6614.
[4].  Honda M, Okutsu H, Matsuura T, et al. Spinorphin, an endogenous inhibitor of enkephalin-degrading enzymes, potentiates leu-enkephalin-induced anti-allodynic and antinociceptive effects in mice. Jpn J Pharmacol, 2001, 87(4): 261-267.