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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. Vipoglanstat (30 mg/kg) also reduces the lung injury score and expression of PTGES and Nos2, the gene encoding inducible nitric oxide synthase (iNOS), as well as increases survival, in a human PTGES knock-in mouse model of sepsis induced by cecal ligation and puncture. Vipoglanstat reduces status epilepticus-induced increases in brain capillary mPGES-1 and P-glycoprotein levels in a human PTGES knock-in mouse model of kainic acid-induced status epilepticus when administered at doses of 10, 30, and 100 mg/kg.
| Molecular Weight | 678.52 |
| Formula | C30H34Cl2F5N5O3 |
| CAS Number | 1360622-01-0 |
| Form | Solid |
| Solubility (25°C) | DMSO 75 mg/mL |
| Storage | -20°C, sealed |
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