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MK-8318
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。
MK-8318图片
CAS NO:1416581-40-2
包装与价格:
包装价格(元)
250mg电议
500mg电议

产品介绍
MK-8318是一种有效的选择性CRTh2受体拮抗剂,Ki为5.0nM。
Cas No.1416581-40-2
Canonical SMILESFC1=CC=C(N(C(C2=CC=C(OC(F)(F)F)C=C2)=O)[C@@H](CCC3)[C@@H]3[C@H]4N(C(CCC(O)=O)=O)C5CC5)C4=C1
分子式C27H26F4N2O5
分子量534.5
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

MK-8318 is a potent and selective CRTh2 receptor antagonist with a Ki of 5.0 nM.

MK-8318 also inhibits β-arrestin, cAMP, CYP3A4, CYP2C9, and CYP2D6 with IC50s of 3.5±2.1 nM, 8.0±6.8 nM, 50 µM, 50 µM and 50 µM[1].

In a sheep model, MK-8318 blocks late airway response (LAR) and airway hyperresponsiveness (AHR) after i.v. infusion at 1 mg/kg. MK-8318 shows 76% LAR efficacy and 114% AHR efficacy. MK-8318 also displays good efficacy on BAL cells/pulmonary function from ovalbumin sensitized and challenged Brown Norway rats at 3, 10, and 30 mg/kg oral dosing[1].

[1]. Huang X, et al. Discovery of MK-8318, a Potent and Selective CRTh2 Receptor Antagonist for the Treatment of Asthma. ACS Med Chem Lett. 2018 Jun 23;9(7):679-684.