TM5275

TM5275 is an orally bioavailable, selective small-molecule inhibitor of plasminogen activator inhibitor-1 (PAI-1, encoded by the SERPINE1 gene). Developed by Tohoku University and Renascience, TM5275 binds to the s4A position of the PAI-1 molecule, preventing its interaction with tissue plasminogen activator (tPA) and urokinase-type plasminogen activator (uPA), thereby preserving active tPA and enhancing fibrinolysis. It also inhibits the interaction between PAI-1 and low-density lipoprotein receptor-related protein 1 (LRP1). Preclinical studies have demonstrated its therapeutic potential as an antithrombotic agent without prolonging bleeding time, as well as its anti-fibrotic and anti-inflammatory effects in models of chronic pancreatitis, liver fibrosis (NASH), lung fibrosis, and diabetic nephropathy.

Other names

2-[2-[2-(4-benzhydrylpiperazin-1-yl)-2-oxoethoxy]acetamido]-5-chlorobenzoic acid5-chloro-2-[({2-[4-(diphenylmethyl)piperazin-1-yl]-2-oxoethoxy}acetyl)amino]benzoic acid5-chloro-2-[[2-[2-[4-(diphenylmethyl)-1-piperazinyl]-2-oxoethoxy]acetyl]amino]-benzoic acid5-chloro-2-[[2-[2-[4-(diphenylmethyl)-1-piperazinyl]-2-oxoethoxy]acetyl]amino]-benzoic acid, monosodium saltTM5275 sodiumTM-5275 sodiumTM 5275 sodiumTM5275 sodium saltTM-5275 sodium saltTM 5275 sodium salt