L-Prolinamide, N-(4-amino-3-chlorobenzoyl)-3-methyl-L-valyl-N-[(2R,3S)-2-ethoxytetrahydro-5-oxo-3-furanyl]-
VX-765
CAS: 273404-37-8
Molecular Formula: C24H33ClN4O6
L-Prolinamide, N-(4-amino-3-chlorobenzoyl)-3-methyl-L-valyl-N-[(2R,3S)-2-ethoxytetrahydro-5-oxo-3-furanyl]- - Names and Identifiers
L-Prolinamide, N-(4-amino-3-chlorobenzoyl)-3-methyl-L-valyl-N-[(2R,3S)-2-ethoxytetrahydro-5-oxo-3-furanyl]- - Physico-chemical Properties
| Molecular Formula | C24H33ClN4O6 |
| Molar Mass | 508.99 |
| Density | 1.32 |
| Boling Point | 779.0±60.0 °C(Predicted) |
| Solubility | Soluble in DMSO (>25 mg/ml) |
| Appearance | solid |
| Color | Off-white to white |
| pKa | 12.60±0.40(Predicted) |
| Storage Condition | -20°C |
| Stability | Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| In vitro study | VX-765 is an Orly-associated drecrug of VRT-043198, which has shown potential inhibition against ICE/caspase-1 and caspase-4 with Ki of 0.8 nM and less than 0.6 nM. And VRT-043198 also inhibitors IL-1β release from both PBMCs and whole blood with IC50 of 0.67 μm and 1.9 μm, review. VX-765 is an orally absorbable VRT-043198 prodrug that exhibits potent inhibition of ICE/caspase-1 and caspase-4 with a Ki of 0.8 nM and <0.6 nM, respectively. VRT-043198 also inhibited IL-1β release from PBMCs and whole blood with an IC50 of 0.67 μm and 1.9 μm, respectively. |
| In vivo study | In collagen-induced arthritis mouse model, VX-765 (200 mg/kg) inhibits LPS-induced IL-1β production by about 60%, and results in a dose-dependent, statistically significant reduction in the inflammation scores and effective protection from joint changes. In vivo VX-765 blocks kindling epileptogenesis in rats by preventing IL-1β increase in forebrain astrocytes without significant effect on afterdischarge duration. In the mouse model of acute seizures, VX-765 (50 mg/kg-200 mg/kg) produces the anticonvulsant effect by delaying the time to onset of the first seizure and decreasing the number of seizures as well as their total duration by average 50% and 64%. In adult rats with genetic absence epilepsy (GAERS), VX-765, after the 3rd drug injection, significantly reduces the cumulative duration and number of spike-and-wave discharges (SWDs) by 55% on average by selective blocking IL-1β biosynthesis. In a mouse model of collagen-induced arthritis, VX-765 (200 mg/kg) inhibited LPS-induced IL-1β production by 60% and resulted in a dose-dependent, the joint lesions can also produce effective protective effect. In vivo, VX-765 blocked epileptogenesis in rats by preventing an increase in IL-1β in forebrain astrocytes without significant effect on post-discharge duration. In a mouse model of acute epilepsy, VX-765 (50 mg/kg-200 mg/kg) delays the onset of the first seizure, and reduce the average 50% of the number of seizures and 64% of the total duration, resulting in anti spasmodic effect. In adult rats with hereditary absence epilepsy, the cumulative duration and average 55% spike slow wave discharges (SWDs) were significantly reduced by selectively blocking IL-1β biosynthesis 3 days after VX-765 drug injection. |
L-Prolinamide, N-(4-amino-3-chlorobenzoyl)-3-methyl-L-valyl-N-[(2R,3S)-2-ethoxytetrahydro-5-oxo-3-furanyl]- - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.965 ml | 9.823 ml | 19.646 ml |
| 5 mM | 0.393 ml | 1.965 ml | 3.929 ml |
| 10 mM | 0.196 ml | 0.982 ml | 1.965 ml |
| 5 mM | 0.039 ml | 0.196 ml | 0.393 ml |
Last Update：2024-01-02 23:10:35
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Spot supply
Product Name: VX-765 Visit Supplier Webpage Request for quotationCAS: 273404-37-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History
L-Prolinamide, N-(4-amino-3-chlorobenzoyl)-3-methyl-L-valyl-N-[(2R,3S)-2-ethoxytetrahydro-5-oxo-3-furanyl]-
27762-64-7
27762-64-7