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Medchemexpress LLC VRT-043198 | 244133-31-1 | 98.9% | 480.94 | 100 MG
SDP

Supplier:  Medchemexpress LLC HY112226100MG

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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 and 0.6 nM for ICE/caspase-1 and caspase-4, respectively.

  • 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, but has little effect on the release of several other cytokines, including IL-1α, tumor necrosis factor-, IL-6 and IL-8.
  • Inhibited IL-1β release from both PBMCs and whole blood with IC50 values of 0.67±0.55 and 1.9±0.80 nM, respectively.
  • Lacks potent antiapoptotic activity.

Catalog No. 50-004-36922


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