产品
编 号：F289985
分子式：C22H29ClN4O6
分子量：480.94
分子式：C22H29ClN4O6
分子量：480.94
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 244133-31-1
产品详情
生物活性：
VRT-043198, the agent metabolite of VX-765 (Belnacasan), is a potent, selective and blood-brain barrier permeable inhibitor of interleukin-converting enzyme/caspase-1 subfamily caspases. VRT-043198 exhibits Ki values of 0.8 nM and 0.6 nM for ICE/caspase-1 and caspase-4, respectively.
体内研究：
VX-765 is converted rapidly to VRT-043198 under the action of plasma and liver esterases and also much more slowly in aqueous solution.VX765 reduces disease severity and the expression of inflammatory mediators in models of rheumatoid arthritis and skin inflammation.VX765 (25, 50, 100, or 200 mg/kg) inhibits lipopolysaccharide-induced cytokine secretion.Animal Model:Na?ve male CD-1 mice.
Dosage:25-200 mg/kg.
Administration:Oral gavage 1 h before i.v. injection of 2 mg/kg E. coli LPS (strain 0111:B4).
Result:Reduced serum IL-1β levels.
体外研究：
VRT-043198 exhibits 100- to 10,000-fold selectivity against other caspase-3 and -6 to -9.VRT043198 inhibits the release of interleukin (IL)-1β and IL-18, but it has little effect on the release of several other cytokines, including IL-1α, tumor necrosis factor-, IL-6 and IL-8. VRT-043198 inhibited IL-1β release from both PBMCs (n = 8) and whole blood (n = 4) with IC50 values of 0.67±0.55 and 1.9±0.80 nM, respectively.VRT-043198 lacks potent antiapoptotic activity.
VRT-043198, the agent metabolite of VX-765 (Belnacasan), is a potent, selective and blood-brain barrier permeable inhibitor of interleukin-converting enzyme/caspase-1 subfamily caspases. VRT-043198 exhibits Ki values of 0.8 nM and 0.6 nM for ICE/caspase-1 and caspase-4, respectively.
体内研究：
VX-765 is converted rapidly to VRT-043198 under the action of plasma and liver esterases and also much more slowly in aqueous solution.VX765 reduces disease severity and the expression of inflammatory mediators in models of rheumatoid arthritis and skin inflammation.VX765 (25, 50, 100, or 200 mg/kg) inhibits lipopolysaccharide-induced cytokine secretion.Animal Model:Na?ve male CD-1 mice.
Dosage:25-200 mg/kg.
Administration:Oral gavage 1 h before i.v. injection of 2 mg/kg E. coli LPS (strain 0111:B4).
Result:Reduced serum IL-1β levels.
体外研究：
VRT-043198 exhibits 100- to 10,000-fold selectivity against other caspase-3 and -6 to -9.VRT043198 inhibits the release of interleukin (IL)-1β and IL-18, but it has little effect on the release of several other cytokines, including IL-1α, tumor necrosis factor-, IL-6 and IL-8. VRT-043198 inhibited IL-1β release from both PBMCs (n = 8) and whole blood (n = 4) with IC50 values of 0.67±0.55 and 1.9±0.80 nM, respectively.VRT-043198 lacks potent antiapoptotic activity.
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