PF-4693627 是一种有效的、选择性的和口服生物可利用的微粒体前列腺素 E 合成酶-1 (mPGES-1) 抑制剂 (IC50=3 nM)，用于治疗由骨关节炎 (OA) 和类风湿性关节炎 (RA) 引起的炎症。
| Cas No. |
1312815-93-2 |
| 化学名 |
1-[5-chloro-6-(4-chlorophenyl)-2-benzoxazolyl]-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]-4-piperidinecarboxamide |
| Canonical SMILES |
ClC1=CC=C(C2=CC(OC(N3CCC(C(N[C@@H]4C[C@@H](CO)CCC4)=O)CC3)=N5)=C5C=C2Cl)C=C1 |
| 分子式 |
C26H29Cl2N3O3 |
| 分子量 |
502.4 |
| 溶解度 |
DMF: 10 mg/ml,DMSO: 10 mg/ml,DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml,Ethanol: 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 |
| 半岛bd体育手机客户端 描述 |
PF-4693627 is an orally bioavailable inhibitor of microsomal prostaglandin E (PGE) synthase-1 (mPGES-1; IC50 = 3 nM). It is selective for mPGES-1 over PGDS, TXAS, and 5-LO in HWB-1483 cells, which have IC50 values greater than 50 μM, as well as COX-2 in fetal fibroblasts (IC50 = >10 μM). PF-4693627 inhibits LPS-stimulated synthesis of PGE2 in human whole blood (IC50 = 109 nM). In vivo, PF-4693627 (10 mg/kg) inhibits PGE2 production in a guinea pig model of carrageenan-induced air pouch inflammation. |
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