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CAY10566 {[allProObj[0].p_purity_real_show]}

货号:A698046

CAY10566是一种选择性硬脂酰辅酶 A 去饱和酶 1 (SCD1) 抑制剂,具有生物可利用性,常用于研究脂肪酸代谢调节和代谢性疾病。

CAY10566 化学结构 CAS号:944808-88-2
CAY10566 化学结构
CAS号:944808-88-2
CAY10566 3D分子结构
CAS号:944808-88-2
CAY10566 化学结构 CAS号:944808-88-2
CAY10566 3D分子结构 CAS号:944808-88-2
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CAY10566 纯度/质量文件 产品仅供科研

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CAY10566 生物活性

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].

CAY10566 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.

CAY10566 实验方案

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

CAY10566 技术信息

CAS号944808-88-2
分子式C18H17ClFN5O2
分子量 389.811
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

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

动物实验配方
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