| Identification | Back Directory | [Name]
1H-Benzimidazole-5-carboxamide, 2-[[2,6-dichloro-3-[[(2,2-dimethyl-1-oxopropyl)amino]methyl]phenyl]amino]-6-(2,2-difluoroethoxy)-1-methyl-N-[trans-4-(trifluoromethyl)cyclohexyl]- | [CAS]
1360622-01-0 | [Synonyms]
Vipoglanstat
1H-Benzimidazole-5-carboxamide, 2-[[2,6-dichloro-3-[[(2,2-dimethyl-1-oxopropyl)amino]methyl]phenyl]amino]-6-(2,2-difluoroethoxy)-1-methyl-N-[trans-4-(trifluoromethyl)cyclohexyl]- | [Molecular Formula]
C30H34Cl2F5N5O3 | [MOL File]
1360622-01-0.mol | [Molecular Weight]
678.52 |
| Hazard Information | Back Directory | [Uses]
Vipoglanstat (BI 1029539), a carboxamide, is a potent and selective, non-peptide and orally active small molecular inhibitor of human prostaglandin E synthase 1 (mPGES-1). Vipoglanstat also has anti-inflammatory activity[1][2]. | [in vivo]
Vipoglanstat (30 mg/kg; i.p.) can reduce LPS-induced lung injury, with reduction in neutrophil influx, protein content, TNF-ɑ, IL-1β and PGE2 levels in bronchoalveolar lavage (BAL), myeloperoxidase activity, expression of mPGES-1, cyclooxygenase (COX)-2 and intracellular adhesion molecule in lung tissue[2].
Vipoglanstat (30 mg/kg; p.o.; 2 h, 8 h and 22 h) significantly reduces sepsis-induced BAL inflammatory cell recruitment, lung injury score and lung expression of mPGES-1 and inducible nitric oxide synthase[2].
Vipoglanstat (30 mg/kg; p.o.; QD) also significantly prolongs survival of mice with severe sepsis[2]. | Animal Model: | LPS-induced acute lung injury models[2] | | Dosage: | 30 mg/kg | | Administration: | 30 mg/kg, i.p. | | Result: | Preserved lung architecture and reduced immune cell influx into the lungs of LPS?challenged mice. |
| Animal Model: | CLP-induced sepsis models[2] | | Dosage: | 30 mg/kg | | Administration: | 30 mg/kg, p.o., 2 hrs, 8 hrs and 22 hrs; 30 mg/kg, p.o., QD | | Result: | Attenuated CLP?induced lung injury and prolongs survival. |
| [References]
[1] International Nonproprietary Names for Pharmaceutical Substances (INN). WHO Drug Information, Vol. 36, No. 2, 2022.
[2] Malarvizhi Gurusamy, et al. Inhibition of microsomal prostaglandin E synthase-1 ameliorates acute lung injury in mice. DOI:10.1186/s12967-021-03016-9
[3] Yan-Yu Zhang, et al. Microsomal prostaglandin E 2 synthase-1 and its inhibitors: Molecular mechanisms and therapeutic significance. Pharmacol Res. 2022 Jan;175:105977. DOI:10.1016/j.phrs.2021.105977 |
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