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Patamostat

(Synonyms: 帕莫司他; E-3123)

目录号: PL11235 纯度: ≥99%

Patamostat (E-3123) 是一种有效的蛋白酶 (protease) 抑制剂。Patamostat 有效抑制胰蛋白酶，纤溶酶和凝血酶，IC50 值分别为 39 nM，950 nM 和 1.9 μM。Patamostat 有潜力用于急性胰腺炎的研究。

CAS No. :114568-26-2

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中文名称	Patamostat
中文别名	帕莫司他
英文名称	Patamostat
英文别名	Benzoic acid,4-[(aminoiminomethyl)amino]-, 4-[[2-(2,5-dioxo-1-pyrrolidinyl)ethyl]thio]phenylester;[4-[2-(2,5-dioxopyrrolidin-1-yl)ethylsulfanyl]phenyl] 4-(diaminomethylideneamino)benzoate;4-(2-succinimidoethylthio)phenyl 4-guanidinobenzoate;Benzoic acid,4-[(aminoiminomethyl)amino]-, 4-[[2-(2,5-dioxo-1-pyrrolidinyl)ethyl]thio]phenyles...;4-{[2-(2,5-dioxopyrrolidin-1-yl)ethyl]sulfanyl}phenyl 4-[(diaminomethylidene)amino]benzoate;Benzoic acid, 4-((aminoiminomethyl)amino)-, 4-((2-(2,5-dioxo-1-pyrrolidinyl)ethyl)thio)phenyl ester;E 3123;p-((2-Succinimidoethyl)thio)phenyl p-guanidinobenzoate;Patamostat [INN];UNII-2T7W4EA51W;Patomostat;4-Guanidinobenzoic acid 4-[[2-(2,5-dioxopyrrolidin-1-yl)ethyl]thio]phenyl ester;Patamostat
Cas No.	114568-26-2
分子式	C₂₀H₂₀N₄O₄S
分子量	412.46
包装储存	4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
详情描述	Patamostat (E-3123) 是一种有效的蛋白酶 (protease) 抑制剂。Patamostat 有效抑制胰蛋白酶，纤溶酶和凝血酶，IC50 值分别为 39 nM，950 nM 和 1.9 μM。Patamostat 有潜力用于急性胰腺炎的研究。

产品详情	Patamostat (E-3123) 是一种有效的蛋白酶 (protease) 抑制剂。Patamostat 有效抑制胰蛋白酶，纤溶酶和凝血酶，IC₅₀ 值分别为 39 nM，950 nM 和 1.9 μM。Patamostat 有潜力用于急性胰腺炎的研究。
生物活性	Patamostat (E-3123) is a potent protease inhibitor. Patamostat potently inhibits trypsin, plasmin and thrombin with IC 50 s of 39 nM, 950 nM and 1.9 μM, respectively. Patamostat may possess suppressing effects on pathogenesis and development of acute pancreatitis.
性状	Solid
IC50 & Target[1][2]	IC50: 39 nM (trypsin), 950 nM (plasmin) and 1.9 μM (thrombin)
体内研究(In Vivo)	Patamostat (intravenous infusion) at 0.03-0.3 mg/kg in rats or at 0.3-3.0 mg/kg in rabbits reduces mortality after the induction of pancreatitis in a dose-dependent manner. Patamostat (1.0-3.0 mg/kg; intravenous infusion) reduces the increases of serum trypsin and lipase activities in dogs with pancreatitis. Patamostat (2 mg/kg per h; continuous infusion) improves almost all parameters, including mortality rate, serum and ascitic fluid amylase levels, plasma endotoxin and serum FDP levels, and distribution of lysosomal enzyme in male Wistar rats. 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	4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
参考文献	[1]. K Miyamoto, et al. [Effects of E-3123, a New Protease Inhibitor, on Several Protease Activities and on Experimental Acute Pancreatitis]. Nihon Yakurigaku Zasshi. 1988 May;91(5):285-93. [2]. T Hirano, et al. Protective Effect of a Cephalosporin, Shiomarin, Plus a New Potent Protease Inhibitor, E3123, on Rat Taurocholate-Induced Pancreatitis. J Gastroenterol Hepatol. Jan-Feb 1993;8(1):52-9.

溶解度数据	In Vitro: DMSO : 100 mg/mL (242.45 mM; Need ultrasonic)配制储备液

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[1]. K Miyamoto, et al. [Effects of E-3123, a New Protease Inhibitor, on Several Protease Activities and on Experimental Acute Pancreatitis]. Nihon Yakurigaku Zasshi. 1988 May;91(5):285-93.
[2]. T Hirano, et al. Protective Effect of a Cephalosporin, Shiomarin, Plus a New Potent Protease Inhibitor, E3123, on Rat Taurocholate-Induced Pancreatitis. J Gastroenterol Hepatol. Jan-Feb 1993;8(1):52-9.

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。

Patamostat

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