Selonsertib

Selonsertib is an inhibitor of apoptosis signal-regulating kinase 1 (ASK1, IC50 = 5.01 nM). It decreases apoptosis and stellate cell activation in an in vitro 3D-human liver microtissue model of non-alcoholic steatohepatitis (NASH) induced by palmitic acid (Cay-10006627) when used at a concentration of 1 µM. Selonsertib (10 µM) sensitizes KB-C2 epidermoid carcinoma cells, which endogenously express ATP-binding cassette family B member 1 (ABCB1), to doxorubicin (Cay-15007) and paclitaxel (Cay-10461). It reduces hepatic necrosis and increases in serum TNF-alpha, IL-6, and chemokine (C-C motif) ligand 2 (CCL2) levels in a mouse model of LPS/D-galactosamine-induced acute liver failure when administered at doses of 15, 30, or 60 mg/kg.Formal Name: 5-(4-cyclopropyl-1H-imidazol-1-yl)-2-fluoro-4-methyl-N-[6-[4-(1-methylethyl)-4H-1,2,4-triazol-3-yl]-2-pyridinyl]-benzamide. CAS Number: 1448428-04-3. Synonyms: GS-4977, GS-4997. Molecular Formula: C24H24FN7O. Formula Weight: 445.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2), (1:7): 0.125 mg/ml, DMSO: 10 mg/ml, Ethanol: 1 mg/ml. lambdamax: 234, 297 nm. SMILES: CC(C)N1C=NN=C1C2=NC(NC(C3=C(F)C=C(C)C(N4C=C(C5CC5)N=C4)=C3)=O)=CC=C2. InChi Code: InChI=1S/C24H24FN7O/c1-14(2)32-13-27-30-23(32)19-5-4-6-22(28-19)29-24(33)17-10-21(15(3)9-18(17)25)31-11-20(26-12-31)16-7-8-16/h4-6,9-14,16H,7-8H2,1-3H3,(H,28,29,33). InChi Key: YIDDLAAKOYYGJG-UHFFFAOYSA-N.