ML355 is a selective 12-lipoxygenase inhibitor with an IC50 value of 0.34 µM, with much less potency against 15-LO-1, 15-LO-2, and 5-LO (IC50s = 9.7, >100, and >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 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,2-8°C |
溶解度 |
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 |
动物实验配方 |