XEN723是一种新型且有效的硬脂酰辅酶A去饱和酶(SCD1)的噻唑基咪唑烷酮抑制剂,在小鼠和HepG2细胞中的IC50值分别为45和524nM。
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XEN723 is a novel and potent thiazolylimidazolidinone inhibitor of Stearoyl-CoA Desaturase (SCD1) with IC50s of 45 and 524 nM in mouse and HepG2 cell, respectively.
XEN723 is a novel and potent thiazolylimidazolidinone inhibitor of Stearoyl-CoA Desaturase (SCD1) with IC50s of 45 and 524 nM in mouse and HepG2 cell, respectively. XEN723 demonstrates an improvement in SCD1 in vitro potency of more than 560-fold compare to the original high throughput screen (HTS) hit[1].
[1]. Sun S, et al. Systematic evaluation of amide bioisosteres leading to the discovery of novel and potent thiazolylimidazolidinone inhibitors of SCD1 for the treatment of metabolic diseases. Bioorg Med Chem Lett. 2014 Jan 15;24(2):520-5.
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