VRT-043198

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. VRT-043198 exhibits Ki values of 0.8 nM and 0.6 nM for ICE/caspase-1 and caspase-4, respectively[1].

Product Specifications

CAS Number

[244133-31-1]

UNSPSC

12352005

Target

Caspase; Drug Metabolite

Type

Reference compound

Related Pathways

Apoptosis; Metabolic Enzyme/Protease

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/vrt-043198.html

Purity

98.89

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(N[C@H](C=O)CC(O)=O)[C@H]1N(C([C@H](C(C)(C)C)NC(C2=CC=C(N)C(Cl)=C2)=O)=O)CCC1

Molecular Formula

C22H29ClN4O6

Molecular Weight

480.94

References & Citations

[1]Woods Wannamaker, et al. (S) -1- ((S) -2-{[1- (4-amino-3-chloro-phenyl) -methanoyl]-amino}-3,3-dimethyl-butanoyl) -pyrrolidine-2-carboxylic acid ((2R,3S) -2-ethoxy-5-oxo-tetrahydro-furan-3-yl) -amide (VX-765), an orally available selective interleukin (IL) -converting enzyme/caspase-1 inhibitor, exhibits potent anti-inflammatory activities by inhibiting the release of IL-1beta and IL-18. J Pharmacol Exp Ther. 2007 May;321 (2) :509-16.