ML355是一种选择性的12-脂氧合酶(12-LOX)抑制剂,IC50值为0.34 µM,对15-LO-1、15-LO-2和5-LO的效力较弱(IC50分别为9.7、>100和>100 µM)。
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产品名称 | lipoxygenase ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Zileuton | ✔ | 97% | |||||||||||||||||
Nordihydroguaiaretic acid | ✔ | 99%+ | |||||||||||||||||
MK-886 | ✔ | 99%+ | |||||||||||||||||
Esculetin | ✔ | 98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Human lipoxygenases (LOXs) are enzymes involved in catalyzing the oxidation of polyunsaturated fatty acids to provide the corresponding bioactive hydroxyeicosatetraenoic acid (HETE) metabolites as the end product. These eicosanoid signaling molecules are involved in a number of physiologic responses such as platelet aggregation, inflammation and cell proliferation. ML355 is a potent and selective inhibitor of human 12-lipoxygenase with nM potency. ML355 has been shown to decrease calcium mobilization and PAR-4 induced platelet aggregation in patient derived human platelets and to significantly inhibit AA/IONO-induced (Arachidonic acid and calcium ionophore) 12-HETE (a downstream target of the 12-LOX protein) in mouse BTC3 cells and human islets at 10 µM. Moreover, ML355 demonstrated excellent microsomal stability with both rat (T1/2 >30 minutes) and mouse (T1/2 >300 minutes) and was found to be stable to mouse plasma over a 2 hour period (100% remaining). In vivo PK studies where ML355 was administered as a solution via IV (3 mpk) and PO (30 mpk) demonstrated that ML355 is orally bioavailable (%F = 20) with good half-life (T1/2 = 2.9 hours)[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.26mL 0.45mL 0.23mL |
11.32mL 2.26mL 1.13mL |
22.65mL 4.53mL 2.26mL |
CAS号 | 1532593-30-8 |
分子式 | C21H19N3O4S2 |
分子量 | 441.523 |
别名 | |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place,Inert atmosphere,2-8°C |
溶解方案 |
DMSO: 40 mg/mL(90.6 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |