A PAI-1 inhibitor (IC50 = 6.95 µM); inhibits formation of a complex consisting of tPA

TM5275 – 5 mg

Brand:
Cayman
CAS:
1103926-82-4
Storage:
-20
UN-No:
De Minimis - 3077 / 9

TM5275 is an inhibitor of plasminogen activator inhibitor 1 (PAI-1; IC50 = 6.95 µM), a serine-protease inhibitor involved in thrombosis.{39402} TM5275 inhibits formation of a complex consisting of tissue plasminogen activator (tPA), PAI-1, and GFP on vascular endothelial cells (VECs) in vitro, prolonging the time that tPA is retained on VECs.{39403} It also enhances fibrin clot dissolution and plasminogen accumulation in vitro and has antithrombotic effects in rat models of thrombosis.{39402} TM5275 (10 and 50 mg/kg) decreases blood clot weight in an arteriovenous shunt thrombosis model and increases the time to primary occlusion in a ferric chloride-treated carotid artery thrombosis model when used at doses of 1 and 3 mg/kg. In a cynomolgus monkey model of photochemical-induced arterial thrombosis, TM5275 (10 mg/kg) increases the time to primary occlusion. It does not affect platelet activity, activated partial thromboplastin time, prothrombin time, or prolong bleeding time.  

 

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Description

A PAI-1 inhibitor (IC50 = 6.95 µM); inhibits formation of a complex consisting of tPA, PAI-1, and GFP on VECsin vitro, prolonging the time that tPA is retained on VECs; decreases blood clot weight in a rat model of arteriovenous shunt thrombosis when used at doses of 10 and 50 mg/kg; increases the time to primary occlusion in a ferric chloride-treated carotid artery thrombosis model in rats when used at doses of 1 and 3 mg/kg; increases the time to primary occlusion in a cynomolgus monkey model of photochemical-induced arterial thrombosis when used at a dose of 10 mg/kg; does not affect platelet activity, activated partial thromboplastin time, prothrombin time, or prolong bleeding time

Formal name: 5-chloro-2-[[2-[2-[4-(diphenylmethyl)-1-piperazinyl]-2-oxoethoxy]acetyl]amino]-benzoic acid, monosodium salt

Synonyms: 

Molecular weight: 544

CAS: 1103926-82-4

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Blood Coagulation Factors||Research Area|Cardiovascular System|Blood|Acute Phase Reactants||Research Area|Cardiovascular System|Blood|Thrombosis||Research Area|Cardiovascular System|Vasculature|Endothelium

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