921605-87-0|2-Methyl-5-(6-(4-(2-(trifluoromethyl)phenoxy)piperidin-1-yl)pyridazin-3-yl)-1,3,4-thiadiazole|CsnPharm

CAS No.: 921605-87-0

MF-438 Catalog No. CSN27614

Synonyms: 2-methyl-5-(6-(4-(2-(trifluoromethyl)phenoxy)piperidin-1-yl)pyridazin-3-yl)-1,3,4-thiadiazole

MF-438 is an inhibitor of stearoyl-CoA desaturase 1 (SCD1) with EC50 of 2.3 nM for rSCD1.

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实验方案

技术信息

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].
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

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
- 2.3728 mL
- 11.8641 mL
- 23.7282 mL
- 5 mM
- 0.4746 mL
- 2.3728 mL
- 4.7456 mL
- 10 mM
- 0.2373 mL
- 1.1864 mL
- 2.3728 mL

技术信息

CAS号

921605-87-0

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H18F3N5OS

运输

蓝冰

分子量

421.44

别名

2-methyl-5-(6-(4-(2-(trifluoromethyl)phenoxy)piperidin-1-yl)pyridazin-3-yl)-1,3,4-thiadiazole

溶解度

DMSO	29.0 mg/mL (68.8 mM)
Water	Insoluble
Ethanol	8.0 mg/mL (19.0 mM)

动物实验配方

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