货号	规格	价格	上海	北京	珠海	重庆	武汉
S80695-2mg买3赠1	99.90%	￥288.00 S80695-2mg ￥288.00 现货（买3赠1）	10 10	-	-	-	-
S80695-5mg买3赠1	99.90%	￥440.00 S80695-5mg ￥440.00 现货（买3赠1）	6 6	-	-	-	-
S80695-10mg促销	99.90%	￥600.00 ￥550.00 S80695-10mg ￥550.00 现货	5 5	-	-	-	-
S80695-25mg促销	99.90%	￥1200.00 ￥900.00 S80695-25mg ￥900.00 现货	7 7	-	-	-	-
S80695-50mg促销	99.90%	￥1800.00 ￥1450.00 S80695-50mg ￥1450.00 现货	1 1	-	-	-	-
S80695-100mg促销	99.90%	￥3360.00 ￥2650.00 S80695-100mg ￥2650.00 现货	1 1	-	-	-	-

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产品描述：

Tiplaxtinin is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC50 of 2.7 μM

靶点：

IC50: 2.7 μM (PAI-1);PAI-1

体内研究：

In the vena cava protocol, Tiplaxtinin (PAI-039) pretreatment significantly reduces thrombus weight at Tiplaxtinin doses of 3, 10 and 30 mg/kg. When Tiplaxtinin is dosed in a treatment paradigm 4 h after stable arterial and venous thrombosis, a significant reduction in thrombus weight is observed 24 h later at Tiplaxtinin doses of 3, 10 and 30 mg/kg. Tiplaxtinin (PAI-039) is administered by oral gavage to athymic mice bearing human bladder cancer cell line T24 xenografts and human cervical cancer HeLa cell xenografts. The subcutaneous tumor growth of both T24 and HeLa cell xenografts treated with Tiplaxtinin is markedly reduced compared with untreated controls. Specifically, at the end of the study, control T24 xenografts are noted to be 1,150±302 mm3 compared with 593±328 mm3 for T24 xenograft tumors treated with 5 mg/kg Tiplaxtinin (P<0.0001) and 627±248 mm3 for T24 xenografts treated with 20 mg/kg (P<0.0001). Tiplaxtinin (1, 3, and 10 mg/kg) is subjected to electrolytic injury of the coronary artery. Tiplaxtinin (PAI-039) causes prolongation in time to coronary occlusion (control, 31.7±6.3 min; 3 mg/kg Tiplaxtinin, 66.0±6.4 min; 10 mg/kg, 56.7±7.4 min; n=5-6; p<0.05) and a reduced thrombus weight (control, 7.6±1.5 mg; 10 mg/kg Tiplaxtinin, 3.6±1.0 mg; p<0.05).

参考文献：

1. Hennan JK, et al. Effect of Tiplaxtinin (PAI-039), an orally bioavailable PAI-1 antagonist, in a rat model of thrombosis. J Thromb Haemost. 2008 Sep;6(9):1558-64. 2. Gomes-Giacoia E, et al. Targeting plasminogen activator inhibitor-1 inhibits angiogenesis and tumor growth in a human cancer xenograft model. Mol Cancer Ther. 2013 Dec;12(12):2697-708. 3. Hennan JK, et al. Evaluation of PAI-039 [{1-benzyl-5-[4-(trifluoromethoxy)phenyl]-1H-indol-3-yl}(oxo)acetic acid], a novel plasminogen activator inhibitor-1 inhibitor, in a canine model of coronary artery thrombosis. J Pharmacol Exp Ther. 2005 Aug;314(2):

溶解性：

DMSO : 100 mg/mL (227.59 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble)

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.276 ml	11.38 ml	22.759 ml
5 mM	0.455 ml	2.276 ml	4.552 ml
10 mM	0.228 ml	1.138 ml	2.276 ml
50 mM	0.046 ml	0.228 ml	0.455 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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