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WIN 64338 hydrochloride
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。
WIN 64338 hydrochloride图片
CAS NO:163727-74-0
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
WIN 64338 hydrochloride 是一种有效的、选择性的、非肽竞争性缓激肽 B2 受体拮抗剂。
Cas No.163727-74-0
化学名(S,E)-(N,N'-dicyclohexylcarbamimidoyl)(3-(naphthalen-2-yl)-1-oxo-1-((4-((tributylphosphonio)methyl)phenyl)amino)propan-2-yl)amide dihydrochloride
Canonical SMILESCCCC[P+](CCCC)(CC1=CC=C(NC([C@]([N-]/C(NC2CCCCC2)=N\C3CCCCC3)([H])CC4=CC5=CC=CC=C5C=C4)=O)C=C1)CCCC.Cl.Cl
分子式C45H68ClN4OP.HCl
分子量783.95
溶解度<58.8mg/ml in DMSO
储存条件Store 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

WIN 64338 hydrochloride is a potent and competitive antagonist of bradykinin B2 receptor [1].

Bradykinin B2 receptor is a G-protein coupled receptor for bradykinin. Bradykinin is an inflammatory nonapeptide and plays a critical role in edema, vasodilation, pain fiber stimulation and smooth muscle spasm.

WIN 64338 hydrochloride is a potent and competitive bradykinin B2 receptor antagonist. In human IMR-90 cells, WIN 64338 inhibited bradykinin binding to the bradykinin B2 receptor with Ki value of 64 nM and inhibited Ca2+ efflux stimulated by bradykinin with pA2 value of 7.1 in a competitive way. WIN 64338 inhibited guinea pig ileum contractility induced by bradykinin with pA2 value of 8.2 and also inhibited acetyicholine-induced contractility [1]. In iris sphincter isolated from rabbit, WIN 64338 (1-10 μM) inhibited contractile responses evoked by bradykinin with pKB value of 6.6 [2]. In guinea-pig tracheal smooth muscle cells, WIN 64338 inhibited inositol phosphate formation induced by bradykinin [3].

In guinea-pigs, WIN 64338 (30 nM) significantly inhibited the increases in plasma extravasation induced by bradykinin via the release of tachykinins from the trigeminal nerve [2].

References:
[1].  Sawutz DG, Salvino JM, Dolle RE, et al. The nonpeptide WIN 64338 is a bradykinin B2 receptor antagonist. Proc Natl Acad Sci U S A, 1994, 91(11): 4693-4697.
[2].  Hall JM, Figini M, Butt SK, et al. Inhibition of bradykinin-evoked trigeminal nerve stimulation by the non-peptide bradykinin B2 receptor antagonist WIN 64338 in vivo and in vitro. Br J Pharmacol, 1995, 116(8): 3164-3168.
[3].  Scherrer D, Schmidlin F, Lach E, et al. Effect of WIN 64338, a B2 bradykinin receptor antagonist on guinea-pig tracheal smooth muscle cells in culture. Fundam Clin Pharmacol, 1998, 12(2): 188-193.