Upamostat|590368-25-5|(WX-671)-陌孚医药/Medlife

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Upamostat (Synonyms: WX-671)

目录号: PL08755 纯度: ≥98.0%

CAS No. :590368-25-5

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中文名称	Upamostat
中文别名	4-[(2S)-3-[3-[(羟基氨基)亚氨基甲基]苯基]-1-氧代-2-[[[2,4,6-三(1-甲基乙基)苯基]磺酰基]氨基]丙基]-1-哌嗪甲酸乙酯
英文名称	Upamostat
英文别名	1-Piperazinecarboxylic acid, 4-[(2S)-3-[3-[(hydroxyamino)iminomethyl]phenyl]-1-oxo-2-[[[2,4,6-tris(1- methylethyl)phenyl]sulfonyl]amino]propyl]-, ethyl ester;1-Piperazinecarboxylic acid, 4-[(2S)-3-[3-[(hydroxyamino)iminomethyl]phenyl]-1-oxo-2-[[[2,4,6-tris(1- methylethyl)phenyl]su;1-Piperazinecarboxylic acid, 4-[(2S)-3-[3-[(hydroxyamino)iminomethyl]phenyl]-1-oxo-2-[[[2,4,6-...;ethyl 4-[(2S)-3-[3-[(E)-(hydroxyhydrazinylidene)methyl]phenyl]-2-[[2,4,6-tri(propan-2-yl)phenyl]sulfonylamino]propanoyl]piperazine-1-carboxylate;WX 671;WX-671;4-[(2S)-3-[3-[(Hydroxyamino)iminomethyl]phenyl]-1-oxo-2-[[[2,4,6-tris(1-methylethyl)phenyl]sulfonyl]amino]propyl]-1-piperazinecarboxylic acid ethyl ester;Upamostat;WX 671
Cas No.	590368-25-5
分子式	C₃₂H₄₇N₅O₆S
分子量	629.81
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Upamostat (WX-671) 是一种丝氨酸蛋白酶抑制剂。Upamostat 是具有口服活性的 WX-UK1 前药，是一种尿激酶型纤溶酶原激活剂 (uPA) 抑制剂。

生物活性

Upamostat (WX-671) is a serine protease inhibitor. Upamostat is the orally available prodrug of the WX-UK1, which is a urokinase plasminogen activator (uPA) inhibitor.

性状

Solid

IC50 & Target[1][2]

Serine protease, uPA

体外研究(In Vitro)

Upamostat is the urokinase plasminogen activator (uPA) inhibitor. Upamostat is the oral pro-drug of the active metabolite WX-UK1, a novel uPA inhibitor. Upamostat inhibits the urokinase-type plasminogen activator (uPA) system, which plays a major role in tumor invasion and metastasis. Upamostat is the orally available amidoxime- (i.e. hydroxyamidine-) prodrug of the pharmacologically active form, WX-UK1. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

The validated method is used to evaluate the pharmacokinetics of Upamostat (Mesupron) in rats. The mean plasma concentrations of Upamostat after a single intravenous injection of 2 mg/kg in five rats are measured. The substance decays in a mono-phasic pattern with a terminal half-life of 0.5 h; its volume of distribution is 2.0 L/kg, and clearance is about 2.7 L/h/kg. has not independently confirmed the accuracy of these methods. They are for reference only.

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

ClinicalTrial

参考文献

[1]. Heinemann V, et al. Phase II randomised proof-of-concept study of the urokinase inhibitor upamostat (WX-671) in combination with gemcitabine compared with gemcitabine alone in patients with non-resectable, locally advanced pancreatic cancer. Br J Cancer.
[2]. Froriep D, et al. Activation of the anti-cancer agent upamostat by the mARC enzyme system. Xenobiotica. 2013 Sep;43(9):780-4.

溶解度数据	In Vitro: DMSO : ≥ 250 mg/mL (396.95 mM)配制储备液

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产品使用指南

Data Sheet

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。

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