Description
A RIPK1 inhibitor (IC50s = 16 and 2,500 nM for the human and mouse enzymes, respectively); >10,000-fold selective for RIPK1 over a panel of 339 kinases at 10 µM; inhibits necrotic cell death induced by a combination of TNF-α and the caspase inhibitor QVD-OPh in U937 human monocytic and L929 murine fibrosarcoma cells (IC50s = 6.3 and 1,300 nM, respectively); decreases IL-1β and IL-6 levels in intestinal mucosa tissue isolated from patients with ulcerative colitis at 3-300 nM; increases survival in a mouse model of TNF-α-induced lethal shock at 3, 10, and 50 mg/kg
Formal name: 3-(phenylmethyl)-N-[(3S)-2,3,4,5-tetrahydro-5-methyl-4-oxo-1,5-benzoxazepin-3-yl]-1H-1,2,4-triazole-5-carboxamide
Synonyms:
Molecular weight: 377.4
CAS: 1622848-92-3
Purity: ≥98%
Formulation: A solid
