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HomeProduct name listTM 5275

TM 5275

Synonym(s):2-[2-[2-(4-Benzhydrylpiperazin-1-yl)-2-oxoethoxy]acetamido]-5-chlorobenzoic acid sodium salt;5-Chloro--[[2-[2-[4-(diphenylmethyl)-1-piperazinyl]-2-oxoethoxy]acetyl]amino]-benzoic acid sodium salt;Sodium 5-chloro-2-[({2-[4-(diphenylmethyl) piperazin-1-yl]-2-oxoethoxy}acetyl)amino]benzoate;TM 5275;TM-5275

TM 5275 Structural

What is TM 5275?

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.

The Uses of TM 5275

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.

Storage

Store at +4°C

Properties of TM 5275

storage temp.  2-8°C
solubility  DMSO:20.0(Max Conc. mg/mL);36.77(Max Conc. mM)
DMF:PBS (pH 7.2) (1:8):0.11(Max Conc. mg/mL);0.2(Max Conc. mM)
DMF:33.0(Max Conc. mg/mL);60.66(Max Conc. mM)
form  powder
color  white to beige

Safety information for TM 5275

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
ghs
Environment
GHS09
GHS Hazard Statements H302:Acute toxicity,oral
H400:Hazardous to the aquatic environment, acute hazard
Precautionary Statement Codes P273:Avoid release to the environment.

Computed Descriptors for TM 5275

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