您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Win 58237
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Win 58237
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 58237图片
CAS NO:158001-76-4
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
20mg电议

产品介绍
Win58237是一种phosphodiesterase(PDE)抑制剂,对PDEV有很强的亲和力,Ki值为170nM,具有舒张血管的作用。
Cas No.158001-76-4
Canonical SMILESO=C1C2=C(N(C3CCCC3)N=C2C)NC(C4=CC=NC=C4)=N1
分子式C16H17N5O
分子量295.34
溶解度Soluble in DMSO
储存条件Store at -20°C
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 58237 is a cyclic nucleotide phosphodiesterase (PDE) inhibitor, with Ki of 170 nM for PDE V, possessing vasorelaxant activity.

Win 58237 is a competitive inhibitor of cGMP PDE V from canine aorta, with a Ki value of 170 nM. Win 58237 is a potent inhibitor of PDE V isolated from vascular tissue with an IC50 value of 240 nM. It is a relatively less potent inhibitor of calmodulin-sensitive PDE I and cGMP-inhibitable cyclic AMP PDE III; but does inhibit cyclic AMP PDE IV with an IC50 value of approximately 300 nM. Win 58237 possesses vasorelaxant activity in the presence of an intact endothelium or nitric oxide[1].

Win 58237 (0.3-3.0 mg/kg i.v.) decreases mean arterial pressure in conscious spontaneously hypertensive rats with an associated increase in vascular (aortic) cGMP content in vivo. Win 58237 (10 mg/kg i.v.) increases plasma cGMP levels, from basal levels of 6.7 ± 1.0 to 31.4 ± 3.5 fmol/μL[1].

[1]. Silver PJ, et al. Cyclic GMP potentiation by WIN 58237, a novel cyclic nucleotide phosphodiesterase inhibitor. J Pharmacol Exp Ther. 1994 Dec;271(3):1143-9.