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Background Information:
VX-765 is a novel Caspase-1 inhibitor being investigated for the treatment of epilepsy, currently being developed by Vertex. VX-765 is an orally-absorbed pro-drug of VRT-043198, a potent and selective inhibitor of ICE/caspase-1 sub-family caspases. VRT-043198 exhibits 100-10,000-fold selectivity against other caspase-3 and -6-9. In cultures of peripheral blood mononuclear cells and whole blood from healthy subjects stimulated with bacterial products, VRT-043198 inhibited the release of Interleukin (IL)-1beta and IL-18, but had little effect on the release of several other cytokines, including IL-1alpha, tumor necrosis factor-alpha, IL-6 and IL-8.
Reference:
1. Boxer, Matthew B.; Quinn, Amy M.; Shen, Min; Jadhav, Ajit; Leister, William; Simeonov, Anton; Auld, Douglas S.; Thomas, Craig J. A Highly Potent and Selective Caspase 1 Inhibitor that Utilizes a Key 3-Cyanopropanoic Acid Moiety. ChemMedChem (2010), 5(5), 730-738.
2. Eda, Hiroyuki. Therapeutic potential for caspase inhibitors: Present and future. Design of Caspase Inhibitors as Potential Clinical Agents (2009), 251-287.
APIM050366: VX-765
CAS No.: 273404-37-8.
Molecular Formula: C24H33ClN4O6.
Molecular Weight: 508.99.
Purity: 99% chem. and stereomeric purity (HPLC and Chiral HPLC).
QC: HPLC-MS, 1HNMR, Chiral HPLC, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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