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ML355

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Chemical Structure| 1532593-30-8 同义名 : -
CAS号 : 1532593-30-8
货号 : A764546
分子式 : C21H19N3O4S2
纯度 : 98%
分子量 : 441.523
MDL号 : MFCD28167822
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
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：
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 (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].
实验方案
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
参考文献

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