貨號	規(guī)格	價(jià)格	上海	北京	武漢	南京
S81987-1mg	96.7%	￥220.00 S81987-1mg ￥220.00 現(xiàn)貨	10 10	-	-	-
S81987-2mg	96.7%	￥380.00 S81987-2mg ￥380.00 現(xiàn)貨	10 10	-	-	-
S81987-5mg	96.7%	￥490.00 S81987-5mg ￥490.00 現(xiàn)貨	10 10	-	-	-
S81987-10mg	96.7%	￥760.00 S81987-10mg ￥760.00 現(xiàn)貨	7 7	-	-	-
S81987-25mg	96.7%	￥1360.00 S81987-25mg ￥1360.00 現(xiàn)貨	2 2	-	-	-
S81987-50mg	≥96%	￥2050.00 S81987-50mg ￥2050.00 2-3天	0 貨期：2-3天	-	-	-
S81987-100mg	≥96%	￥2900.00 S81987-100mg ￥2900.00 2-3天	0 貨期：2-3天	-	-	-

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產(chǎn)品介紹

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

產(chǎn)品描述：

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

靶點(diǎn)：

IC50: 6.95 μM (PAI-1);PAI-1

體外研究：

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. 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. 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

體內(nèi)研究：

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)

參考文獻(xiàn)：

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.

溶解性：

soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	1.835 ml	9.175 ml	18.349 ml
5 mM	0.367 ml	1.835 ml	3.67 ml
10 mM	0.183 ml	0.917 ml	1.835 ml
50 mM	0.037 ml	0.183 ml	0.367 ml

注意：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻(xiàn)

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TM5275 (sodium)