CAS NO: | 101910-24-1 |
包装 | 价格(元) |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
Physical Appearance | A crystalline solid |
Storage | Store at RT |
M.Wt | 335.4 |
Cas No. | 101910-24-1 |
Formula | C22H25NO2 |
Solubility | ≤100mg/ml in ethanol;100mg/ml in methanol;100mg/ml in acetone;100mg/ml in DMSO;100mg/ml in etonitrile. |
Chemical Name | α-pentyl-3-(2-quinolinylmethoxy)-benzenemethanol |
Canonical SMILES | CCCCCC(O)c1cccc(OCc2ccc3ccccc3n2)c1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
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).