CAY10566是一种选择性硬脂酰辅酶A去饱和酶1（SCD1）抑制剂（小鼠：IC50=4.5nM；人：IC50=4.5nM）。
Cas No.:944808-88-2
Sample solution is provided at 25 µL, 10mM.
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CAY10566 is a selective stearoyl-CoA desaturase 1 (SCD1) inhibitor (mouse: IC₅₀= 4.5nM; human: IC₅₀=4.5nM). CAY10566 blocks the conversion of saturated long-chain fatty acyl-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs (IC₅₀=7.9nM or 6.8nM). CAY10566 can be used in studies related to fatty acid metabolism regulation, metabolic diseases, as well as colorectal cancer, liver cancer, and ovarian cancer[1-4].
In vitro, Swiss 3T3 cells were treated with CAY10566 (0.1nM–10μM) for 48 hours. CAY10566 inhibited cell proliferation in a concentration-dependent manner[5]. Mia-PaCa2 or CFPAC-1 human pancreatic cancer cells were treated with CAY10566 (10μM) for 48 hours. CAY10566 reduced the expression of ACLY, FASN, ACACA, and ACACB genes in the cells[6].
In vivo, after establishing ischemic stroke (MCAO/R) model in mice, CAY10566 (20mg/kg; once daily) was administered by oral gavage to MCAO/R mice for 3 days starting 2 hours after reperfusion. CAY10566 significantly reduced cerebral infarct volume, alleviated neuronal apoptosis, and improved cognitive and motor functions of mice[7]. CAY10566 (7.5mg/kg; once every three days) was intraperitoneally injected into C57BL/6 mice fed a high-fat diet for 14 weeks. CAY10566 significantly ameliorated hepatic steatosis, reduced hepatic lipid droplet accumulation, and enhanced AMPK-mediated lipophagy in the mice[8].
References:
[1] Masuda M, Ting TC, Levi M, et al. Activating transcription factor 4 regulates stearate-induced vascular calcification. J Lipid Res. 2012 Aug;53(8):1543-52.
[2] Liu G, Lynch JK, Freeman J, et al. Discovery of potent, selective, orally bioavailable stearoyl-CoA desaturase 1 inhibitors. J Med Chem. 2007 Jun 28;50(13):3086-100.
[3] de Lima Luna AC, Forti FL. Modulation of SCD1 activity in hepatocyte cell lines: evaluation of genomic stability and proliferation. Mol Cell Biochem. 2021 Sep;476(9):3393-3405.
[4] Kamphorst JJ, Cross JR, Fan J, 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.
[5] Koeberle A, Shindou H, Harayama T, 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.
[6] Zhang X, Zhu B, Yan J, et al. Matrix stiffness boosts PDAC chemoresistance via SCD1-dependent lipid metabolic reprogramming. Regen Biomater. 2025 Jun 16;12:rbaf056.
[7] Li S, Li X Jr, Peng L, et al. Inhibition of SCD1 attenuates neuroinflammation and brain injury after cerebral ischemia-reperfusion. Brain Res Bull. 2026 Feb;235:111693.
[8] Zhou Y, Zhong L, Yu S, et al. Inhibition of stearoyl-coenzyme A desaturase 1 ameliorates hepatic steatosis by inducing AMPK-mediated lipophagy. Aging (Albany NY). 2020 Apr 23;12(8):7350-7362.
CAY10566是一种选择性硬脂酰辅酶A去饱和酶1（SCD1）抑制剂（小鼠：IC50=4.5nM；人：IC50=4.5nM）。CAY10566可阻断饱和长链脂肪酸辅酶A（LCFA-CoAs）向单不饱和LCFA-CoAs的转化（IC50=7.9nM或6.8nM）。CAY10566可用于脂肪酸代谢调节、代谢性疾病以及结直肠癌、肝癌和卵巢癌等相关研究[1-4]。
在体外，CAY10566（0.1nM–10μM）处理Swiss 3T3细胞48小时。CAY10566以浓度依赖性地抑制细胞增殖[5]。CAY10566（10μM）处理Mia-PaCa2或CFPAC-1人胰腺癌细胞48小时。CAY10566可降低细胞中ACLY、FASN、ACACA、ACACB基因的表达[6]。
在体内，在小鼠建立缺血性卒中模型（MCAO/R）2小时后，CAY10566（20mg/kg；每天一次）灌胃于MCAO/R小鼠3天。CAY10566显著减少了脑梗死体积、减轻了神经元凋亡，并改善了小鼠的认知和运动功能[7]。CAY10566（7.5mg/kg；每三天一次）腹腔注射于高脂饮食的C57BL/6小鼠，14周。CAY10566显著改善了小鼠的肝脏脂肪变性，减少了肝脏脂滴积累，并增强了AMPK介导的脂噬[8]。
| Cell experiment [1]: | |
Cell lines | Swiss 3T3 fibroblasts (mouse fibroblast cell line) |
Preparation Method | Swiss 3T3 cells were seeded into 12-well plates in DMEM containing 10% (v/v) charcoal-stripped FCS and treated with CAY10566 (0.1nM–10μM) and for 48h at 37°C and 5% CO₂. |
Reaction Conditions | 0.1nM–10μM; 48h |
Applications | CAY10566 concentration-dependently decreased Swiss 3T3 cell proliferation. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice (6-week-old, male) |
Preparation Method | Mice were fed a high-fat diet (HFD) for 14 weeks and received an intraperitoneal injection of CAY10566 (7.5mg/kg) once every three days for 14 weeks. Mice were sacrificed after 14 weeks of feeding for biochemical assays, histological staining, and Western blot analysis. |
Dosage form | 7.5mg/kg; i.p.; once every three days for 14 weeks |
Applications | CAY10566 treatment significantly decreased body weight, ameliorated serum levels of ALT, AST, TG, TCHO and NEFA, reduced hepatic steatosis and lipid droplet accumulation, increased AMPK phosphorylation, and enhanced lipophagy in HFD-fed mice. |
References: | |
| Cas No. | 944808-88-2 | SDF | |
| 化学名 | 3-[4-(2-chloro-5-fluorophenoxy)-1-piperidinyl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)-pyridazine | ||
| Canonical SMILES | Cc1nnc(o1)c1ccc(nn1)N1CCC(CC1)Oc1cc(F)ccc1Cl | ||
| 分子式 | C18H17ClFN5O2 | 分子量 | 389.8 |
| 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 | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5654 mL | 12.8271 mL | 25.6542 mL |
| 5 mM | 513.1 μL | 2.5654 mL | 5.1308 mL |
| 10 mM | 256.5 μL | 1.2827 mL | 2.5654 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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