Desks and Tables
Medchemexpress LLC VRT-043198 | 244133-31-1 | 98.89% | 480.94 | 50 MG
VRT-043198 is a potent, selective, and blood-brain barrier permeable inhibitor of interleukin-converting enzyme/caspase-1 subfamily caspases. It is the agent metabolite of VX-765 (Belnacasan). This inhibitor exhibits Ki values of 0.8 nM for ICE/caspase-1 and 0.6 nM for caspase-4.
- Potent, selective, and blood-brain barrier permeable inhibitor of interleukin-converting enzyme/caspase-1 subfamily caspases.
- Exhibits Ki values of 0.8 nM for ICE/caspase-1 and 0.6 nM for caspase-4.
- Exhibits 100- to 10,000-fold selectivity against other caspase-3 and -6 to -9.
- Inhibits the release of interleukin (IL)-1β and IL-18.
- Has little effect on IL-1α, tumor necrosis factor-, IL-6, and IL-8.
- Lacks potent antiapoptotic activity.
Medchemexpress LLC L-Prolinamide, N-(4-amino-3-chlorobenzoyl)-3-methyl-L-valyl-N-[(1S)-2-carboxy-1-formyleth | 244133-31-1 | 98.9% | 480.94 | 10 MG
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. It exhibits Ki values of 0.8 nM for ICE/caspase-1 and 0.6 nM for caspase-4.
- Potent, selective, and blood-brain barrier permeable inhibitor of interleukin-converting enzyme/caspase-1 subfamily caspases.
- Exhibits Ki values of 0.8 nM for ICE/caspase-1 and 0.6 nM for caspase-4.
- Exhibits 100- to 10,000-fold selectivity against other caspases (caspase-3 and -6 to -9).
- Inhibits the release of interleukin (IL)-1β and IL-18.
- Little effect on the release of other cytokines, including IL-1α, tumor necrosis factor-, IL-6, and IL-8.
- Inhibited IL-1β release from PBMCs (n = 8) and whole blood (n = 4) with IC50 values of 0.67±0.55 and 1.9±0.80 nM, respectively.
- Lacks potent antiapoptotic activity.
- For research use only.
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