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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]- manufacturers
- Vipoglanstat
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- $2580.00
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2026-07-15
- CAS:1360622-01-0
- Purity:
- Supply Ability: 10g
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| | 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]- Basic information |
| | 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]- Chemical Properties |
| density | 1.43±0.1 g/cm3(Predicted) | | solubility | Acetonitrile: Slightly soluble: 0.1-1 mg/ml
DMSO: Sparingly soluble: 1-10 mg/ml | | form | Solid | | pka | 12.25±0.40(Predicted) | | color | White to off-white |
| | 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]- Usage And Synthesis |
| 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 LPSchallenged 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 CLPinduced 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
[4] GÖRAN TORNLING. A phase 2 trial investigating the efficacy and safety of the mPGES-1 inhibitor vipoglanstat in systemic sclerosis-related Raynaud’s.[J]. Rheumatology, 2025: 704-713. DOI: 10.1093/rheumatology/keae049
[5] EMMA L. B. SOLDNER. Inhibition of human microsomal PGE2 synthase-1 reduces seizure-induced increases of P-glycoprotein expression and activity at the blood-brain barrier[J]. FASEB Journal, 2019, 33 12: 13966-13981. DOI: 10.1096/fj.201901460rr |
| | 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]- Preparation Products And Raw materials |
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