ベルナカサン 化学特性,用途語,生産方法
効能
抗てんかん薬, カスパーゼ1阻害薬
使用
VX-765 shows anti-convulsant activity by inhibiting interlukin-1β biosynthesis.
一般的な説明
The cell-permeable prodrug of the caspase-1/4-selective inhibitor VRT-43198 (
Ki in nM = <0.6/Caspase-4, 0.8/Caspase-1, 100/Caspase-8, 560/Caspase-6, 1,030/Caspase-9, 9,000/Granzyme B, 16,000/Caspase-7, 21,500/Caspase-3; IC
50 >100 μM against Cathepsin B & Trypsin). In addition to inhibiting LPS-induced IL-1β production in primary human PBMC cultures (IC
50 ~1 μM), VX-765 is also effective in preventing HIV infection-induced IL-1β production and pyroptosis of CD4 T cells in human lymphoid aggregate cultures (HLAC; CD4 population = 29.2% in non-infected control cultures, 8.3% vs. 30.2% in infected cultures with or without 5 μM VX-765). VX-765 is orally available in mice (Blood
Cmax = 0.78 μg/mL = 1.53 μM;
Tmax = 1.0 h; AUC
last = 2.06 μg · h/mL; 84 mg/kg, p.o.) and shown to display
in vivo anti-inflammatory efficacy against LPS-induced plasma IL-1β production (ED
max = 100 mg/kg, p.o.), Oxazolone-induced delayed-type hypersensitivity (ED
max = 50 mg/kg, p.o.), collagen-induced arthritis (ED
max = 100 mg/kg, p.o.). When administered via intraperitoneal injection, VX-765 is also demonstrated to suppress the severity of seizure induction (ED
max = 50 mg/kg i.p.) among rats receiving kainic acid via intracerebroventricular injection.
Biochem/physiol Actions
Cell permeable: yes
ベルナカサン 上流と下流の製品情報
原材料
準備製品