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描述 | CAY10566 is identified as a potent, orally bioavailable, and selective inhibitor of stearoyl-CoA desaturase1 (SCD1), exhibiting IC50s of 4.5 and 26 nM in mouse and human enzymatic assays, respectively. It also demonstrates strong cellular efficacy in HepG2 cells by inhibiting the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs, with an IC50 of 7.9 nM or 6.8 nM[1].[2]. |
体内研究 | In vivo studies reveal that after the establishment of palpable tumors, treatment with CAY10566 at a dose of 2.5 mg/kg administered orally twice daily exhibits a more pronounced effect on Akt-driven tumors compared to Ras-driven tumors. The mean tumor volume, relative to untreated tumors by day 13 or 14 post-therapy, is significantly lower in the Akt-driven tumor group (0.5±0.04) than in the Ras-driven tumor group (0.67±0.05), with a P-value of 0.01 for the comparison between Ras and Akt-driven tumors as determined by a two-tailed t-test[4]. |
体外研究 | Additionally, CAY10566 concentration-dependently reduces the proliferation of Swiss 3T3 cells over 24 hours, with a concentration range of 0.0001-10 μM[3]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.57mL 0.51mL 0.26mL |
12.83mL 2.57mL 1.28mL |
25.65mL 5.13mL 2.57mL |
CAS号 | 944808-88-2 |
分子式 | C18H17ClFN5O2 |
分子量 | 389.811 |
别名 | |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,2-8°C |
溶解方案 |
DMSO: 25 mg/mL(64.13 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |