1103926-82-4 Usage
Description
TM5275 is an inhibitor of plasminogen activator inhibitor 1 (PAI-1; IC50 = 6.95 μM), a serine-protease inhibitor involved in thrombosis. 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. It also enhances fibrin clot dissolution and plasminogen accumulation in vitro and has antithrombotic effects in rat models of thrombosis. 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.
Uses
TM 5275 Sodium Salt is a novel inhibitor of plasminogen activator inhibitor-1 (PAI-1), which provides antithrombitic benefits devoid of bleeding in primates.
Biochem/physiol Actions
TMS5275 is an orally available, potent and selective inhibitor of PAI-1 that delivers antithrombotic benefits devoid of bleeding effect in nonhuman primates.
Check Digit Verification of cas no
The CAS Registry Mumber 1103926-82-4 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,1,0,3,9,2 and 6 respectively; the second part has 2 digits, 8 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 1103926-82:
(9*1)+(8*1)+(7*0)+(6*3)+(5*9)+(4*2)+(3*6)+(2*8)+(1*2)=124
124 % 10 = 4
So 1103926-82-4 is a valid CAS Registry Number.
1103926-82-4Relevant articles and documents
Structure-activity relationships of new N-acylanthranilic acid derivatives as plasminogen activator inhibitor-1 inhibitors
Yamaoka, Nagahisa,Kodama, Hidehiko,Izuhara, Yuko,Miyata, Toshio,Meguro, Kanji
experimental part, p. 215 - 224 (2011/04/16)
Novel anthranilic acid derivatives having substituted N-acyl side chains were designed and synthesized for evaluation as plasminogen activator inhibitor-1 (PAI-1) inhibitors. Compounds with a 4-diphenylmethyl-1-piperazinyl moiety on the acyl side chains in general exhibited potent in vitro PAI-1 inhibitory activity and good pharmacokinetic profiles after oral administration in rats. Compound 16f (TM5275) was identified as a promising candidate for further pharmacological evaluation.
