MF-438
产品说明书
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同义名 : | - |
| CAS号 : | 921605-87-0 | |
| 货号 : | A1148548 | |
| 分子式 : | C19H18F3N5OS | |
| 纯度 : | 95+% | |
| 分子量 : | 421.44 | |
| MDL号 : | MFCD28386313 | |
| 存储条件： |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 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 | |
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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 |
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