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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 |
| Related PGE synthase Products |
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(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. |
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| CAY10526
CAY10526 is a specific microsomal PGE2 synthase-1 (mPGES1) inhibitor. CAY10526 inhibits PGE2 production through the selective modulation of mPGES1 expression but does not affect COX-2. CAY10526 significantly suppresses tumor growth and increases apoptosis in melanoma xenografts. CAY10526 reduces BCL-2 and BCL-XL (anti-apoptotic) protein levels and increases BAX and BAK (pro-apoptotic) as well as cleaved caspase 3 levels. CAY10526 inhibits cell viability (IC50<5 μM) in three melanoma cell lines expressing mPGES1. |
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