Formulation: A crystalline solid
Formal Name: N-[5-[[2-[[[4-[(ethylsulfonyl)amino]cyclohexyl]carbonyl]amino]-5-fluoro-6-benzothiazolyl]oxy]-2-fluorophenyl]-3-(trifluoromethyl)-benzeneacetamide
Purity: ≥98%
Formula Markup: C31H29F5N4O5S2
Formula Weight: 696,7
Shelf life (days): 730
CAS Number: 2919801-86-6
Notes: SZM-1209 is an inhibitor of receptor-interacting serine/threonine kinase 1 (RIPK1).{69403} It selectively binds to RIPK1 over RIPK3 (Kds = 85 and >10,000 nM, respectively) and inhibits necrosome formation and phosphorylation of RIPK1 induced by TNF-α, SM-164 (Item No. 28632), and Z-VAD-FMK in HT-29 cells (EC50 = 22.4 nM). SMZ-1209 (10 and 20 mg/kg) decreases reductions in body temperature and improves survival in a mouse model of systemic inflammatory response syndrome (SIRS) induced by TNF-α and Z-VAD-FMK. It also reduces lung RIPK1 phosphorylation, IL-6 and TNF-α levels, and total protein content, as well as decreases the number of hemorrhagic sites and congestion edema, in a mouse model of acute lung injury (ALI) induced by short-term intratracheal exposure to 4-(N-nitrosomethylamino)-1-(3-pyridyl)-1-butanone (NNK; Item No. 16414).
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