CAY10566

A potent, selective inhibitor of stearoyl-CoA desaturase

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1mg

￥650.00

520.00

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5mg

￥2062.00

1650.00

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10mg

￥3887.00

3110.00

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25mg

￥8525.00

6820.00

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50mg

￥13500.00

10800.00

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货号: ajci21358
CAS: 944808-88-2
别名:
分子式: C18H17ClFN5O2
分子量: 389.8
纯度: >98%
溶解度: DMF: 20 mg/ml,DMF:PBS (pH 7.2) (1:5): 0.15 mg/ml,DMSO: 10 mg/ml,Ethanol: 0.15 mg/ml
储存: Store at -20°C
库存: 现货

Background

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 also 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)[1][2].

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

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)[4].

参考文献:
[1]. Masuda M, et al. Activating transcription factor 4 regulates stearate-induced vascular calcification. J Lipid Res. 2012 Aug;53(8):1543-52.
[2]. Liu G, et al. Discovery of potent, selective, orally bioavailable stearoyl-CoA desaturase 1 inhibitors. J Med Chem. 2007 Jun 28;50(13):3086-100.
[3]. Koeberle A, et al. Palmitoleate is a mitogen, formed upon stimulation with growth factors, and converted to palmitoleoyl-phosphatidylinositol. J Biol Chem. 2012 Aug 3;287(32):27244-54.
[4]. Kamphorst JJ, et al. Hypoxic and Ras-transformed cells support growth by scavenging unsaturated fatty acids from lysophospholipids. Proc Natl Acad Sci U S A. 2013 May 28;110(22):8882-7.