REV 5901
目录号 : GC14939
An antagonist of cysteinyl-leukotriene receptors
Cas No.:101910-24-1
Sample solution is provided at 25 µL, 10mM.
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- Purity: >98.00%
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- SDS (Safety Data Sheet)
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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).
Cas No. | 101910-24-1 | SDF | |
化学名 | α-pentyl-3-(2-quinolinylmethoxy)-benzenemethanol | ||
Canonical SMILES | CCCCCC(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 |
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1 mg | 5 mg | 10 mg |
1 mM | 2.9815 mL | 14.9076 mL | 29.8151 mL |
5 mM | 0.5963 mL | 2.9815 mL | 5.963 mL |
10 mM | 0.2982 mL | 1.4908 mL | 2.9815 mL |
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