CAY10566 是选择性的、口服具有活性的硬脂酰辅酶 A 去饱和酶 1 抑制剂，在小鼠和人酶测定中IC50分别为 4.5 和 26 nM。它具有显著的细胞活性，可阻断 HepG2 细胞中饱和长链脂肪酸-CoAs (LCFA-CoAs) 向单不饱和 LCFA-CoAs 的转化 。

CAY10566 shows excellent cellular activity in blocking the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs in HepG2 cells (IC50=7.9 nM or 6.8 nM). CAY10566 is a potent, orally bioavailable and selective stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50s of 4.5 and 26 nM in mouse and human enzymatic assays, respectively..

CAY10566 (0.0001-10 μM; 24 hours) concentration-dependently decreases Swiss 3T3 cell proliferation [3].

After the establishment of palpable tumors, the mice are treated with a vehicle or SCD1 inhibitor (2.5 mg/kg CAY10566 orally twice daily). The effect of SCD1 inhibition on the Akt-driven tumors is greater than on the Ras-driven tumors. With the mean tumor volume at day 13 or 14 post-therapy, relative to untreated tumors, 0.5±0.04 and 0.67±0.05 respectively (P=0.01 for Ras-Akt comparison, by two-tailed t-test) [4].

944808-88-2

C18H17ClFN5O2

389.81

DMSO:24 mg/mL (61.57 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years