| Identification | Back Directory | [Name]
TM 5275 | [CAS]
1103926-82-4 | [Synonyms]
CS-2524
TM 5275
TM5275 (sodium)
TM 5275;TM-5275
TM 5275 sodium salt
TM5275 sodium salt >=98% (HPLC)
2-(2-(2-(4-benzhydrylpiperazin-1-yl)-2-oxoethoxy)acetamido)-5-chlorobenzoic acid sodium salt
5-Chloro-2-[[2-[2-[4-(Diphenylmethyl)-1-piperazinyl]-2-oxoethoxy]acetyl]amino]benzoic acid sodium salt | [Molecular Formula]
C28H27ClN3O5*Na | [MDL Number]
MFCD28396414 | [MOL File]
1103926-82-4.mol | [Molecular Weight]
546 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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. | [in vivo]
TM5275 exhibits a favorable pharmacokinetics profile and very low toxicity to mice and rats. In rat thrombosis models. Blood clot weights are significantly lower in rats administered 10 and 50 mg/kg of TM5275 (60.9±3.0 and 56.8±2.8 mg, respectively) than in vehicle-treated rats (72.5±2.0 mg). The antithrombotic effectiveness of TM5275 (50 mg/kg) is equivalent to that of ticlopidine (500 mg/kg), a reference antithrombotic compound. Plasma concentration of TM5275 reaches 17.5±5.2 μM after a dose of 10 mg/kg. TM5275 (5 mg/kg) combined with tPA (0.3 mg/kg) significantly enhances the antithrombotic effect of tPA (0.3 mg/kg) alone and provides a benefit similar to that of a high tPA dose (3 mg/kg)[1]. | [storage]
Store at -20°C |
|
| Company Name: |
Sigma-Aldrich
|
| Tel: |
021-61415566 800-8193336 |
| Website: |
https://www.sigmaaldrich.cn |
|