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PF-4693627 is an effective and selective microsomal prostaglandin E synthase-1 inhibitor (IC50=3 nM). It is used for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA).
PF-4693627 is an effective and selective microsomal prostaglandin E synthase-1 inhibitor (IC50=3 nM). It is used for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA).
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
500 μg | ¥ 647 | 35日内发货 | |
1 mg | ¥ 1,190 | 35日内发货 | |
5 mg | ¥ 5,580 | 35日内发货 | |
10 mg | ¥ 9,870 | 35日内发货 |
产品描述 | PF-4693627 is an effective and selective microsomal prostaglandin E synthase-1 inhibitor (IC50=3 nM). It is used for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA). |
靶点活性 | mPGES-1:3 nM |
体外活性 | PF-4693627 displays high activity in lipopolysaccharide (LPS) stimulated human whole blood (HWB) cell assay (IC50=109 nM). PF-4693627 also inhibits mPGES-1 (IC50s: 180 and 6 nM in HWB-1483 and human fetal fibroblast, respectively). |
体内活性 | PF-4693627 (1.0 mg/kg; i.v.) displays good bioavailability (59%) and modest half-life (t1/2=3.7 h) in Sprague-Dawley rats. PF-4693627 (10 mg/kg; orally) suppresses 63% of PGE2 production relative to vehicle control in the Guinea pig carrageenan stimulated air pouch model[1]. |
分子量 | 502.43 |
分子式 | C26H29Cl2N3O3 |
CAS No. | 1312815-93-2 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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