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REV 5901

Catalog No.
C5416
antagonist of cysteinyl-leukotriene receptors
Grouped product items
SizePriceStock Qty
10mg
$90.00
Ship with 5-10 days
50mg
$370.00
Ship with 5-10 days
100mg
$647.00
Ship with 5-10 days
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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).

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at RT
M.Wt335.4
Cas No.101910-24-1
FormulaC22H25NO2
Solubility≤100mg/ml in ethanol;100mg/ml in methanol;100mg/ml in acetone;100mg/ml in DMSO;100mg/ml in etonitrile.
Chemical Nameα-pentyl-3-(2-quinolinylmethoxy)-benzenemethanol
Canonical SMILESCCCCCC(c1cccc(OCc2nc(cccc3)c3cc2)c1)O
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

REV 5901
 

User Guide

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