BI-4394

BI-4394 is an inhibitor of matrix metalloproteinase-13 (MMP-13, IC50 = 0.001 µM for the recombinant human enzyme). It is selective for MMP-13 over MMP-1-3, 7-10, -12, and -14 with IC50 values ranging from 8.3 to greater than 22 µM for the recombinant human enzymes. BI-4394 inhibits the degradation of isolated bovine nasal cartilage explants cultured with human MMP-13 (IC50 = 0.031 µM). It decreases disease severity in a mouse model of anti-type II collagen antibody and LPS-induced arthritis when administered at a dose of 100 mg/kg.Formal Name: 5-[3-[[[(4-carboxyphenyl)methyl]amino]carbonyl]-1-methyl-1H-pyrazol-5-yl]-1H-indole-2-carboxylic acid, 2-ethyl ester. CAS Number: 1222173-37-6. Molecular Formula: C24H22N4O5. Formula Weight: 446.5. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 10mM. SMILES: O=C(OCC)C1=CC2=C(N1)C=CC(C3=CC(C(NCC4=CC=C(C(O)=O)C=C4)=O)=NN3C)=C2. InChi Code: InChI=1S/C24H22N4O5/c1-3-33-24(32)20-11-17-10-16(8-9-18(17)26-20)21-12-19(27-28(21)2)22(29)25-13-14-4-6-15(7-5-14)23(30)31/h4-12,26H,3,13H2,1-2H3,(H,25,29)(H,30,31). InChi Key: MMJPVSDTLGFIQW-UHFFFAOYSA-N.