TM5441

TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor 1 (PAI-1), a serine-protease inhibitor involved in thrombosis. It decreases survival of HT1080, HCT116, Daoy, MDA-MB-231, and Jurkat cancer cells with IC50 values ranging from 13.9 to 51.1 µM. TM5441 inhibits branching of human umbilical vein endothelial cells (HUVECs) in a vasculature assay in vitro when used at a concentration of 50 µM but does not affect HUVEC survival or apoptosis. It also disrupts tumor vasculature in HT1080 and HCT116 mouse xenograft models when used at a dose of 20 mg/kg per day. TM5441 prevents hypertension and cardiac hypertrophy and reduces periaortic fibrosis induced by L-NAME (Cay-80210). It protects against high-fat diet-induced non-alcoholic fatty liver disease (NAFLD) in mice when administered concurrently with a high-fat diet or after glucose tolerance has developed. TM5441 also increases median lifespan by 4-fold and reduces signs of senescence in Klotho-deficient mice, a mouse model of aging.Formal Name: 5-chloro-2-[[2-[2-[[3-(3-furanyl)phenyl]amino]-2-oxoethoxy]acetyl]amino]-benzoic acid. CAS Number: 1190221-43-2. Molecular Formula: C21H17ClN2O6. Formula Weight: 428.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 33 m/ml, DMF:PBS(pH 7.2)(1:6): 0.14 mg/ml, DMSO: 20 mg/ml. lambdamax: 226 nm. SMILES: O=C(COCC(NC1=CC=C(Cl)C=C1C(O)=O)=O)NC2=CC(C3=COC=C3)=CC=C2. InChi Code: InChI=1S/C21H17ClN2O6/c22-15-4-5-18(17(9-15)21(27)28)24-20(26)12-30-11-19(25)23-16-3-1-2-13(8-16)14-6-7-29-10-14/h1-10H,11-12H2,(H,23,25)(H,24,26)(H,27,28). InChi Key: BGGMLMAPVODXAU-UHFFFAOYSA-N.