Merck Frosst Centre for Therapeutic Research, PO Box 1005, Pointe-Claire-Dorval, Québec, Canada H9R 4P8.
Bioorg Med Chem Lett. 2010 Jan 15;20(2):499-502. doi: 10.1016/j.bmcl.2009.11.111. Epub 2009 Nov 26.
A series of stearoyl-CoA desaturase 1 (SCD1) inhibitors were developed. Investigations of enzyme potency and metabolism led to the identification of the thiadiazole-pyridazine derivative MF-438 as a potent SCD1 inhibitor. MF-438 exhibits good pharmacokinetics and metabolic stability, thereby serving as a valuable tool for further understanding the role of SCD inhibition in biological and pharmacological models of diseases related to metabolic disorders.
一系列硬脂酰辅酶 A 去饱和酶 1（SCD1）抑制剂被开发出来。对酶活性和代谢的研究导致了噻二唑-哒嗪衍生物 MF-438 的鉴定，它是一种有效的 SCD1 抑制剂。MF-438 表现出良好的药代动力学和代谢稳定性，因此可作为进一步了解 SCD 抑制在与代谢紊乱相关疾病的生物和药理学模型中作用的有价值工具。
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