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CAY10471 Racemate
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。
CAY10471 Racemate图片
CAS NO:844639-57-2

CAY10471 Racemate (TM30089 Racemate) 是一种有效、高度选择性的前列腺素 D2 受体 (CRTH2) 拮抗剂,对 hCRTH2 的 Ki 值为 0.6 nM,对其选择性远高于人血栓素 A2 受体 TP (Ki,>10000 nM) 或 PGD2 受体 DP (Ki,1200 nM)。CAY10471 Racemate 对小鼠和大鼠的同源 CRTH2 也具有拮抗作用。
Cas No.844639-57-2
别名3-[[(4-氟苯基)磺酰基]甲基氨基]-1,2,3,4-四氢-9H-咔唑-9-乙酸,TM30089 Racemate
Canonical SMILESO=C(O)CN1C2=C(C3=C1C=CC=C3)CC(N(S(=O)(C4=CC=C(F)C=C4)=O)C)CC2
分子式C21H21FN2O4S
分子量416.47
溶解度DMSO: 150 mg/mL (360.17 mM)
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

CAY10471 Racemate (TM30089 Racemate) is a potent and highly selective prostaglandin D2 receptor CRTH2 antagonist, with a Ki of 0.6 nM for hCRTH2, selective over human thromboxane A2 receptor TP (Ki, >10000 nM) or PGD2 receptor DP (Ki, 1200 nM). CAY10471 Racemate also has effect on mouse and rat orthologs of CRTH2[1]. Ki: 0.6 nM (CRTH2), 1200 nM (DP)[1]

CAY10471 Racemate (Compound 13) inhibits PGD2-induced inositol phosphate or cAMP formation, suppresses β-arrestin translocation with IC50s of 12 and 3 nM, respectively[1].

[1]. Ulven T, et al. Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist. J Med Chem. 2005 Feb 24;48(4):897-900.

 
 
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