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PF-4693627 is a potent, selective and orally bioavailable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor (IC50=3 nM) for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA).
| Molecular Weight | 502.43 |
| Formula | C26H29Cl2N3O3 |
| CAS Number | 1312815-93-2 |
| Form | Solid |
| Solubility (25°C) | DMSO 100 mg/mL (ultrasonic) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PGE synthase Products |
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| Vipoglanstat
Vipoglanstat (BI 1029539) is an inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1; IC50 = ≤0.5 nM in isolated human whole blood). Vipoglanstat reduces LPS-induced increases in the influx of neutrophils and levels of cytokines in bronchoalveolar lavage fluid (BALF), as well as the expression of PTGES, the gene encoding mPGES-1, Cox2, and Icam1 in the lung parenchyma, in a human PTGES knock-in mouse model of acute lung injury when administered at a dose of 30 mg/kg. |
| mPGES1-IN-7
mPGES-1-IN-2 is a benzimidazole-based mPGES-1 inhibitor that also inhibits adipophysin PGD synthase (I-PGDS) (5 μM, IR=60 %). |
| (E)-KME-4
(E)-KME-4 is a potent inhibitor of prostaglandin synthetase (PGS) with an IC50 of 0.28 μM; also inhibits 5-lipoxygenase with an IC50 of 1.05 μM. |
| Friluglanstat
Friluglanstat is a prostaglandin E synthase (mPGES-1) inhibitor, with anti-inflammatory activity. |
| UT-11
UT-11 is a potent and brain-permeable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor. |
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