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 SMILES | C[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 tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation 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. |
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