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AAT-008
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。
AAT-008图片
CAS NO:847727-81-5
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
AAT-008 是一种有效、选择性和口服活性的前列腺素 EP4 受体拮抗剂,对重组人 EP4 和重组大鼠 EP4 的 Kis 分别为 0.97 和 6.1 nM。
Cas No.847727-81-5
Canonical SMILESC[C@H](NC(C1=CC(Cl)=CN=C1OC2=CC=CC(F)=C2)=O)C3=CC=C(C(O)=O)C=C3
分子式C21H16ClFN2O4
分子量414.8
溶解度DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 0.5 mg/ml
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

AAT-008 is an orally bioavailable and potent antagonist of the prostaglandin E2 (PGE2) receptor subtype 4 (EP4; IC50 = 16.3 nM in a human EP4 functional assay). It is selective for EP4 with IC50 values of 2.4, 1,890, >20,000, and >20,000 nM for binding to human recombinant EP4, EP2, EP1, and EP3, respectively. AAT-008 has potent binding affinity for human, rat, and dog EP4 (Kis = 0.97, 6.1, and 38 nM, respectively) and suppresses PGE2-induced elevation of intracellular cAMP with an antagonistic potency (pA2) of 1.1 nM in vitro. Oral administration of AAT-008 reduces carrageenan-induced mechanical hyperalgesia in rats in a dose-dependent manner.