TM 5275 sodium salt

Modify Date: 2024-01-06 12:21:33

TM 5275 sodium salt structure	Common Name	TM 5275 sodium salt
	CAS Number	1103926-82-4	Molecular Weight	544.98
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₂₈H₂₈ClN₃NaO₅	Melting Point	N/A
	MSDS	Chinese USA	Flash Point	N/A
	Symbol	GHS07, GHS09	Signal Word	Warning

Use of TM 5275 sodium salt

TM5275 sodium is a plasminogen activator inhibitor (PAI-1) with an IC50 of 6.95 μM.

Name	sodium 5-chloro-2-[({2-[4-(diphenylmethyl)piperazin-1-yl]-2-oxoethoxy}acetyl)amino]benzoate
Synonym	More Synonyms

Description	TM5275 sodium is a plasminogen activator inhibitor (PAI-1) with an IC50 of 6.95 μM.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> PAI-1 Research Areas >> Cancer Research Areas >> Cardiovascular Disease
Target	IC50: 6.95 μM (PAI-1)[1]
In Vitro	Docking studies shows that TM5275 binds to strand 4 of the A β-sheet (s4A) position of PAI-1. TM5275 is a selective PAI-1 and (up to 100 μM) does not interfere with other serpin/serine protease systems[1]. TM5275 at concentrations of 20 and 100 μM significantly prolongs the retention of tPA-GFP on VECs by inhibiting tPA-GFP-PAI-1 high-molecular-weight complex formation. TM5275 enhances the time-dependent accumulation of plasminogen as well as the dissolution of fibrin clots on and around the tPA-GFP-expressing cells[2]. Cell viability at 72 h treatment is decreased with 70-100 μM TM5275 in ES-2 and JHOC-9 cells. From 48 h up to 96 h, cell growth is suppressed with 100 μM TM5275. Active PAI-1 in cell culture media is significantly decreased in cells treated with 100 μM TM5275 compared to control treatment. TM5275 is suggested to exert anti-proliferative effects in ovarian cancer with high PAI-1 expression[3].
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].
Kinase Assay	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].
Cell Assay	ES2 cells are treated with DMSO (control) or 100 μM TM5275 for the indicated periods (24, 48, 72, 96 hour). Cell growth is determined by CellTiter-Glo assay[1].
Animal Admin	Rats: Thrombus formation in arteriovenous shunts is achieved in male CD rats. Either TM5275 (10 and 50 mg/kg, n=9) or ticlopidine (500 mg/kg, n=6), suspended in 0.5% CMC solution, is administered orally by gavage 90 mins before the study. Control rats are administered only a 0.5% CMC solution (n=10). Blood is allowed to circulate through the shunt for 30 mins. The wet weight of the thrombus covering the silk thread is eventually measured[1]. Mice: TM5275 is administered orally by gavage to male ICR mice (50 mg/kg). Heparinized blood samples are collected from the vein before (0 h) and 1, 2, 6, and 24 h after oral drug administration. Plasma drug concentration is determined on a reverse-phase high-performance liquid chromatography[1].
References	[1]. Izuhara Y, et al. A novel inhibitor of plasminogen activator inhibitor-1 provides antithrombotic benefits devoid of bleeding effect in nonhuman primates. J Cereb Blood Flow Metab. 2010 May;30(5):904-12. [2]. Yasui H, et al. TM5275 prolongs secreted tissue plasminogen activator retention and enhances fibrinolysis on vascular endothelial cells. Thromb Res. 2013 Jul;132(1):100-5. [3]. Mashiko S, et al. Inhibition of plasminogen activator inhibitor-1 is a potential therapeutic strategy in ovarian cancer. Cancer Biol Ther. 2015;16(2):253-60.

Molecular Formula	C₂₈H₂₈ClN₃NaO₅
Molecular Weight	544.98
PSA	102.01000
LogP	2.54120
Storage condition	2-8°C

Symbol	GHS07, GHS09
Signal Word	Warning
Hazard Statements	H302-H400
Precautionary Statements	P273-P301 + P312 + P330-P391
RIDADR	UN 3077 9 / PGIII

sodium 2-(2-(2-(4-benzhydrylpiperazin-1-yl)-2-oxoethoxy)acetamido)-5-chlorobenzoate

TM5275

Sodium 5-chloro-2-[({2-[4-(diphenylmethyl)-1-piperazinyl]-2-oxoethoxy}acetyl)amino]benzoate

Benzoic acid, 5-chloro-2-[[2-[2-[4-(diphenylmethyl)-1-piperazinyl]-2-oxoethoxy]acetyl]amino]-, sodium salt (1:1)

TM5275 sodium salt

TM5275 (sodium)

DC Chemicals Limited
China
Product Name: TM5275 sodium salt
Price: $450.0/100mg $800.0/250mg $1600.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Get all suppliers and price by the below link:

TM 5275 sodium salt suppliers

Price: $173/10mM*1mLinDMSO

Reference only. check more TM 5275 sodium salt price

TM 5275 sodium salt

Use of TM 5275 sodium salt

Names

TM 5275 sodium salt Biological Activity

Chemical & Physical Properties

Safety Information

Synonyms