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- 详细信息
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
244133-31-1
- 规格：
10 mM * 1 mL/5 mg/10 mg/25 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥1650.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥1500.0 |
| 规格： | 10 mg | 产品价格： | ￥2500.0 |
| 规格： | 25 mg | 产品价格： | ￥4500.0 |
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VRT-043198
CAS No. : 244133-31-1
MCE 国际站：VRT-043198
产品活性：VRT-043198 是 VX-765 (Belnacasan) 的活性代谢物，是有效的、选择性的、能透过血脑屏障的 caspase-1 的抑制剂。VRT-043198 对 caspase-1 和 caspase-4 的 Ki 值分别为 0.8 nM 和 0.6 nM。
研究领域：Apoptosis | Metabolic Enzyme/Protease
作用靶点：Caspase | Drug Metabolite
In Vitro: 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.
In Vivo: 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.
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