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Iralukast(CGP 45715A)
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。
Iralukast(CGP 45715A)图片
CAS NO:151581-24-7
包装与价格:
包装价格(元)
250mg电议
500mg电议

产品介绍
Iralukast是白三烯的拮抗剂(CysLT),其对CysLT1的pKi值为7.8。
Cas No.151581-24-7
Canonical SMILESO=C(C1=CC(C2=CC=C(S[C@H]([C@H](O)C3=CC=CC(C(F)(F)F)=C3)/C=C/C=C\CCCCOC4=CC=C(C(C)=O)C(O)=C4CCC)C=C2O1)=O)O
分子式C38H37F3O8S
分子量710.76
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

Iralukast is a cysteinyl-leukotriene antagonist (CysLT) with a pKi of 7.8 for CysLT1.

Both Iralukast and CGP 57698 are able to compete for the two sites labelled by [3H]-LTD4. As in all the G-protein coupled receptors, Iralukast and CGP 57698 do not discriminate between the high and the low affinitystates of the CysLT receptor labelled by LTD4 (Ki1=Ki2=16.6 nM±36% CV and Ki1=Ki2=5.7 nM±19% CV, respectively). Iralukast, displays a slow bindingkinetic, because preincubation (15 min) increases its antagonist potency. Iralukast and CGP 57698 antagonize LTD4-induced contraction of humanbronchi, with pA2 values of 7.77±4.3% CV and 8.51±1.6% CV, respectively, and slopes not significantly different from unity[2].

[1]. Magnus B?ck, et al. Update on leukotriene, lipoxin and oxoeicosanoid receptors: IUPHAR Review 7. Br J Pharmacol. 2014 Aug; 171(15): 3551-3574. [2]. Valérie Capra, et al. Pharmacological characterization of the cysteinyl-leukotrieneantagonists CGP 45715A (iralukast) and CGP 57698 in human airways in vitro.Br J Pharmacol. 1998 Feb; 123(3): 590-598.