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VX-765

Chemical Structure : VX-765

CAS No.: 273404-37-8

VX-765 (Belnacasan;VX765;VX 765)

Catalog No.: PC-43391Not For Human Use, Lab Use Only.

VX-765 (Belnacasan) is an orally absorbed prodrug of VRT-043198, which is a potent and selective inhibitor of interleukin-converting enzyme/caspase-1 with Ki of 0.8 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

VX-765 (Belnacasan) is an orally absorbed prodrug of VRT-043198, which is a potent and selective inhibitor of interleukin-converting enzyme/caspase-1 with Ki of 0.8 nM; VRT-043198 exhibits 100- to 10,000-fold selectivity against other caspase-3 and -6 to -9, VX-765 is converted rapidly to VRT-043198 under the action of plasma and liver esterases; inhibits LPS-induced IL-1β production, reduces disease severity and the expression of inflammatory mediators in models of rheumatoid arthritis and skin inflammation.

Epilepsy

Phase 2 Discontinued

Physicochemical Properties

M.Wt 508.995
Formula C24H33ClN4O6
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 27 mg/mL

Chemical Name/SMILES

L-Prolinamide, N-(4-amino-3-chlorobenzoyl)-3-methyl-L-valyl-N-[(2R,3S)-2-ethoxytetrahydro-5-oxo-3-furanyl]-

References

1. Stack JH, et al. J Immunol. 2005 Aug 15;175(4):2630-4.

2. Wannamaker W, et al. J Pharmacol Exp Ther. 2007 May;321(2):509-16.

3. Bialer M, et al. Epilepsy Res. 2013 Jan;103(1):2-30.

4. Wang W, et al. Proc Natl Acad Sci U S A. 2016 Aug 23;113(34):9587-92.

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