产品说明书

MF-438

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Chemical Structure| 921605-87-0 同义名 : -
CAS号 : 921605-87-0
货号 : A1148548
分子式 : C19H18F3N5OS
纯度 : 95+%
分子量 : 421.439
MDL号 : MFCD28386313
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(59.32 mM)，配合低频超声助溶，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

DMF: 50 mg/mL(118.64 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 Stearoyl-CoA desaturase (SCD) is a long chain fatty acyl-CoA specific desaturase. In humans, elevated SCD activity is positively associated with a high body mass index, hyperinsulinemia, hypertriglyceridemia and liver steatosis. MF-438 is a potent and orally bioavailable SCD1 inhibitor with an EC50 of 2.3 nM for rSCD1. MF-438 had an overall good pharmacokinetic profile in rodents. Oral bioavailability was 73% in mice and 38% in rats with half-lives of 6.4 and 6.0 h, respectively. MF-438 inhibited activity of SCD with an ED50 between 1 and 3 mg/kg in the liver of mice on a high carbohydrate diet. After approximately one week of qd dosing with MF-438 at 5 mg/kg in DIO mice, the first symptoms of alopecia and partial eye closure began to appear[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.37mL

0.47mL

0.24mL

11.86mL

2.37mL

1.19mL

23.73mL

4.75mL

2.37mL
参考文献

[1]Léger S, et al. Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438). Bioorg Med Chem Lett. 2010 Jan 15;20(2):499-502