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REV 5901
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。
REV 5901图片
CAS NO:101910-24-1
包装与价格：
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
REV 5901 是一种竞争性和口服活性的白三烯受体拮抗剂，Ki 为 0.7 μM。
Cas No.101910-24-1
化学名α-pentyl-3-(2-quinolinylmethoxy)-benzenemethanol
Canonical SMILESCCCCCC(O)c1cccc(OCc2ccc3ccccc3n2)c1
分子式C22H25NO2
分子量335.4
溶解度≤100mg/ml in ethanol;100mg/ml in methanol;100mg/ml in acetone;100mg/ml in DMSO;100mg/ml in etonitrile.
储存条件Room temperature
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

Ki: 0.7 μM for cysteinyl-leukotriene receptor of guinea pig lung membranes

REV 5901 is an antagonist of cysteinyl-leukotriene receptors.

Cysteinyl leukotriene receptor 1, a receptor for cysteinyl leukotrienes, contributes to mediating various allergic and hypersensitivity reactions by binding the cysteinyl LTs (CysLTs; viz, LTC4, LTD4, and to a much lesser extent, LTE4) in humans and models of the reactions in other animals.

In vitro: Previous in-vitro showed that REV 5901 had a Ki value of 0.7 μM vs. [3H]leukotriene D4 ([3H]-LTD4) binding to membranes from guinea pig lung. Against LTC4-, LTD4- and LTE4-induced contractions of guinea pig parenchymal strips, REV 5901 had Kb values of ca 3 μM and was relatively ineffective against contractions that was induced by other spasmogens. Moreover, in isolated guinea pig hearts, the peptiodoleukotriene-antagonist activity was also observed against the hemodynamic and vasoconstriction effects of LTD4. In addition, unlike other reported antagonists, REV 5901 was found to be ineffective against the multiple forms of cyclic nucleotide phosphodiesterases [1].

In vivo: Animal study found that the oral antagonist activity had been shown with an LTD4-induced bronchoconstriction model and with an LTD4-induced wheal response model in guinea pigs [1].

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Van Inwegen, R. G.,Khandwala, A.,Gordon, R., et al. REV 5901: An orally effective peptidoleukotriene antagonist, detailed biochemical/pharmacological profile. Journal of Pharmacology and Experimental Therapeutics 241, 117-124 (1987).