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About This Item
Empirical Formula (Hill Notation):
C22H29ClN4O6
CAS Number:
Molecular Weight:
480.94
MDL number:
NACRES:
NA.28
SMILES string
O=C([C@H]1N(CCC1)C([C@@H](NC(C2=CC=C(C(Cl)=C2)N)=O)C(C)(C)C)=O)N[C@H](C=O)CC(O)=O
assay
≥94% (HPLC)
form
(Powder or Lyophilized powder or film)
color
white to off-white
storage temp.
-10 to -25°C
Quality Level
Biochem/physiol Actions
Orally available, highly potent and selective caspase-1 (ICE) inhibitor in vitro and in vivo.
VRT-043198, the active metabolite of VX-765 ( Belnacasan), is an orally available, highly potent and selective caspase-1 (ICE; Interleukin-1 converting enzyme) inhibitor (IC50/caspase- = 204 pM/1, 3.3 nM/8, 5.07 nM/9, 10.6 nM/5, 14.5 nM/4, 58.5 nM/14, 66.5 nM/10, >10 μM/3, 6 or 7). VRT-043198 inhibits IL-1β release from human PBMCs in cultures (IC50 = 0.67 μM) without affecting caspase-8/9-meidated apoptosis in Jurkat & NT2 cells. When administered orally in mice in vivo (25-100 mg/kg), VRT-043198 alleviates LPS-induced IL-1β production (50-100 mg/kg p.o. 1h prior to LPS i.v.) and is efficacious in a oxazolone-induced DTH dermatitis and a collagen-induced arthritis (CIA) model.
VRT-043198, the active metabolite of VX-765 ( Belnacasan), is an orally available, highly potent and selective caspase-1 (ICE; Interleukin-1 converting enzyme) inhibitor (IC50/caspase- = 204 pM/1, 3.3 nM/8, 5.07 nM/9, 10.6 nM/5, 14.5 nM/4, 58.5 nM/14, 66.5 nM/10, >10 μM/3, 6 or 7). VRT-043198 inhibits IL-1β release from human PBMCs in cultures (IC50 = 0.67 μM) without affecting caspase-8/9-meidated apoptosis in Jurkat & NT2 cells. When administered orally in mice in vivo (25-100 mg/kg), VRT-043198 alleviates LPS-induced IL-1β production (50-100 mg/kg p.o. 1h prior to LPS i.v.) and is efficacious in a oxazolone-induced DTH dermatitis and a collagen-induced arthritis (CIA) model.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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