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CAS No.: 1532593-30-8

ML355 Catalog No. CSN17912

Synonyms: ML355

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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400-920-2911

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生物活性

实验方案

技术信息

生物活性

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 (T_1/2 >30 minutes) and mouse (T_1/2 >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 (T_1/2 = 2.9 hours)^[1].
参考文献

[1] Discovery of ML355, a Potent and Selective Inhibitor of Human 12-Lipoxygenase

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2649 mL
- 11.3245 mL
- 22.6490 mL
- 5 mM
- 0.4530 mL
- 2.2649 mL
- 4.5298 mL
- 10 mM
- 0.2265 mL
- 1.1325 mL
- 2.2649 mL

技术信息

CAS号

1532593-30-8

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H19N3O4S2

运输

蓝冰

分子量

441.52

别名

ML355

溶解度

DMSO	240.0 mg/mL (543.6 mM)
Water	insoluble

动物实验配方

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