VX-765是VRT-043198的口服前药,是一种有效,选择性的 caspase-1 抑制剂,Ki为0.8 nM。
Description | VX-765 is an oral prodrug of VRT-043198, a potent and selective caspase-1 inhibitor with a Ki of 0.8 nM. | ||||||||||||||||
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IC50 & Target |
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In Vivo | VX-765 doses 50, 100, and 200 mg/kg significantly (p<0.05) reduces serum IL-1β levels by as much as 60%, whereas 25 mg/kg has a smaller effect (~35% inhibition) that is not statistically significant. It is noteworthy that the effect of VX-765 on the release of IL-1β induced by LPS reached a plateau at 100 mg/kg. VX-765 (25, 50, and 100 mg/kg × 2) significantly reduces ear edema. VX-765 also dose-dependently reduces the concentrations of cytokines, chemokines, and inflammatory mediators in the ear biopsy samples[2]. VX-765 at doses of 25, 50, and 200 mg/kg significantly delays the time to seizure onset by 1.5- to twofold (p<0.01), reduces the number of seizures by 40% (p<0.01) and the total time spent in EEG seizure activity by 30 to 50% (p<0.01)[3]. | ||||||||||||||||
Solvent & Solubility | In Vitro: DMSO : ≥ 27 mg/mL (53.05 mM) * "≥" means soluble, but saturation unknown. Preparing Stock Solutions
* Please refer to the solubility information to select the appropriate solvent. In Vivo:
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References | |
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