CAY10566

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CAY10566 在阻断 HepG2 细胞中饱和长链脂肪酸-CoA (LCFA-CoAs) 转化为单不饱和 LCFA-CoA 方面表现出优异的细胞活性（IC50=7.9 nM 或 6.8 nM）。 CAY10566 是一种有效的、口服生物可利用的、选择性硬脂酰辅酶A去饱和酶1 (SCD1) 抑制剂，在小鼠和人类酶测定中，IC50 分别为 4.5 和 26 nM。

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.After establishment of palpable tumors, the mice are treated with 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).

Cell Proliferation Assay Cell Line:Swiss 3T3 cells Concentration:0.0001, 0.001, 0.01, 0.1, 1, 10 μM Incubation Time:24 hours Result:Swiss 3T3 cell proliferation was concentration-dependently decreased.

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Metabolic Enzyme/Protease

Dehydrogenase

SCD1

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944808-88-2

389.81

C18H17ClFN5O2

>98% (HPLC)

DMSO:24 mg/mL (61.57 mM; Need ultrasonic)

Cc1nnc(o1)-c1ccc(nn1)N1CCC(CC1)Oc1cc(F)ccc1Cl

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(-20℃)

With Ice Pack

≥ 2 years