Fulacimstat

Fulacimstat is an inhibitor of chymase (IC50s = 4 and 3 nM for the human and hamster enzyme, respectively). It reduces cardiac fibrosis induced by the beta1-adrenergic receptor (B1-AR) and beta2-AR agonist isoprenaline (isoproterenol, Cay-15592) in hamsters when administered at doses of 1, 3, and 10 mg/kg. Fulacimstat (2 and 5 mg/kg per day) inhibits microembolism-induced decreases in left ventricular ejection fraction and increases in left ventricular end-systolic volume, decreases in plasma levels of N-terminal pro-brain natriuretic peptide (nt-proBNP), TGF-beta1, and TNF-alpha, as well as the levels of interstitial fibrosis and the cross-sectional area of myocytes, a measure of myocyte hypertrophy, in a coronary microembolism-induced canine model of heart failure.Formal Name: 1-(2,3-dihydro-3-methyl-2-oxo-6-benzoxazolyl)-3-[(1R)-2,3-dihydro-4-(trifluoromethyl)-1H-inden-1-yl]-1,2,3,4-tetrahydro-2,4-dioxo-5-pyrimidinecarboxylic acid. CAS Number: 1488354-15-9. Synonyms: BAY-1142524. Molecular Formula: C23H16F3N3O6. Formula Weight: 487.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble. SMILES: O=C1N(C(C(C(O)=O)=CN1C2=CC=C(N(C(O3)=O)C)C3=C2)=O)[C@@]4([H])C5=CC=CC(C(F)(F)F)=C5CC4. InChi Code: InChI=1S/C23H16F3N3O6/c1-27-17-7-5-11(9-18(17)35-22(27)34)28-10-14(20(31)32)19(30)29(21(28)33)16-8-6-12-13(16)3-2-4-15(12)23(24,25)26/h2-5,7,9-10,16H,6,8H2,1H3,(H,31,32)/t16-/m1/s1. InChi Key: JDARDSVOVYVQST-MRXNPFEDSA-N.