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Tiplaxtinin

(Synonyms: PAI-039; Tiplasinin)

目录号: PL04393 纯度: ≥98%

Tiplaxtinin 是一种有效的，具有口服活性的选择性的纤溶酶原激活物抑制剂-1 (PAI-1) 抑制剂，IC50 为 2.7 μM。

CAS No. :393105-53-8

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中文名称	Tiplaxtinin
中文别名	ALPHA-氧代-1-(苯基甲基)-5-[4-(三氟甲氧基)苯基]-1H-吲哚-3-乙酸;Tiplaxtinin（PAI-039）抑制剂
英文名称	Tiplaxtinin
英文别名	1H-Indole-3-aceticacid, a-oxo-1-(phenylmethyl)-5-[4-(trifluoromethoxy)phenyl]-;2-[1-benzyl-5-[4-(trifluoromethoxy)phenyl]indol-3-yl]-2-oxo-acetic aci d;2-[1-benzyl-5-[4-(trifluoromethoxy)phenyl]indol-3-yl]-2-oxoacetic acid;PAI-039;Tiplaxtinin;{1-benzyl-5-[4-(trifluoromethoxy)phenyl]-1H-indol-3-yl}(oxo)acetic acid;2-{1-benzyl-5-[4-(trifluoromethoxy)phenyl]-1H-indol-3-yl}-2-oxoacetic acid;Tiplasinin;Tiplasinin [USAN];UNII-L396QIB983;PAI 039;WAY-168039;alpha-Oxo-1-(phenylmethyl)-5-[4-(trifluoromethoxy)phenyl]-1H-indole-3-acetic acid;(1-Benzyl-5-(4-(trifluoromethoxy)phenyl)-1H-indol-3-yl)oxoacetic acid;a-Oxo-1-(phenylmethyl)-5-[4-(trifluoromethoxy)phenyl]-1H-indole-3-acetic acid;(1-Benzyl-5-(4-(trifluoromethoxy)phenyl)-1H-indol-3-yl)oxoacetic acid; a-Oxo-1-(phenylmethyl)-5-[4-(trifluoromethoxy)phenyl]-1H-indole-3-acetic acid;L396QIB983;2-(1-benzyl-5-(4-(trifluoromethoxy)phenyl)-1H-indol-3-yl)-2-oxoacetic acid;Tiplasinin [USAN:INN];Tiplasinin (USAN);MLS006
Cas No.	393105-53-8
分子式	C₂₄H₁₆F₃NO₄
分子量	439.38
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	Tiplaxtinin 是一种有效的，具有口服活性的选择性的纤溶酶原激活物抑制剂-1 (PAI-1) 抑制剂，IC50 为 2.7 μM。

产品详情	Tiplaxtinin 是一种有效的，具有口服活性的选择性的纤溶酶原激活物抑制剂-1 (PAI-1) 抑制剂，IC₅₀ 为 2.7 μM。
生物活性	Tiplaxtinin is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC 50 of 2.7 μM.
性状	Solid
IC50 & Target[1][2]	IC50: 2.7 μM (PAI-1)
体外研究(In Vitro)	Tiplaxtinin (PAI-039), a small-molecule inhibitor of PAI-1 activity, on the urothelial cell lines. A significant inhibition in cellular proliferation is noted in T24 cells treated with Tiplaxtinin with the documentation of a favorable IC50 value of 43.7±6.3 μM and in UM-UC-14 cells 52.8±1.6 μM whereas the benign cell line, UROtsa, is noted to have a higher IC50 value of 70.3±0.1 μM. Notably, IC50 values of Tiplaxtinin in detached cells, 19.7±3.8 μM in T24, 44.5±6.5 μM in UM-UC-14, and 31.6±6.1 μM in UROtsa, are significantly lower than the IC50 values calculated for cells cultured in the presence of Tiplaxtinin under attached conditions. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	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 mm compared with 593±328 mm for T24 xenograft tumors treated with 5 mg/kg Tiplaxtinin (P<0.0001) and 627±248 mm for T24 xenograf
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
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.

溶解度数据	In Vitro: DMSO : 100 mg/mL (227.59 mM; Need ultrasonic)H₂O : < 0.1 mg/mL (insoluble)配制储备液

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[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.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Tiplaxtinin

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