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BV165183

VRT 043198 NEW

An inhibitor of caspase-1 and active metabolite of VX-765. Blocks lipopolysaccharide-mediated release of cytokines. Suppresses release of interleukins IL-1β and IL-18. Reduced inflammatory cytokines, such as IL-1α, tumor necrosis factor-α, IL-6 and IL-8, observed in in vivo models of rheumatoid arthritis and skin inflammation.

Technical Data

CAS No: 244133-31-1
Product Code: BV165183
Chemical Formula: C22H29ClN4O6
Molecular Weight: 480.94

Literature

References
  • Wannamaker W et al (2007). (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 321 (2): 509-16.
  • Boxer MB et al (2010). A highly potent and selective caspase 1 inhibitor that utilizes a key 3-cyanopropanoic acid moiety. Chem Med Chem 5(5):730-8.
  • Adriaenssens Y et al (2017). Carboxylate isosteres for caspase inhibitors: the acylsulfonamide case revisited. Org Biomol Chem 15(35):7456-7473.

Solubility

Stability

Datasheets

Specification: View
MSDS: View

VRT 043198

CAS No:
244133-31-1
Chemical Formula:
Molecular Weight:
480.94
Product Structure
References:
1. Wannamaker W et al (2007). (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 321 (2): 509-16.
2. Boxer MB et al (2010). A highly potent and selective caspase 1 inhibitor that utilizes a key 3-cyanopropanoic acid moiety. Chem Med Chem 5(5):730-8.
3. Adriaenssens Y et al (2017). Carboxylate isosteres for caspase inhibitors: the acylsulfonamide case revisited. Org Biomol Chem 15(35):7456-7473.
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