2. Metabolic Enzyme/Protease
  3. FXR
  4. FXR agonist 4

FXR agonist 4 (compound 10a) 是法尼酯 X 受体 (FXR) 激动剂，EC50 值为 1.05 μM。FXR agonist 4 有效改善 DIO 小鼠高脂血症、肝脏脂肪变性、胰岛素抵抗和肝脏炎症。FXR agonist 4 可用于非酒精性脂肪性肝病 (NAFLD) 的研究。

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FXR agonist 4 Chemical Structure

FXR agonist 4 Chemical Structure

CAS No. : 3025841-47-5

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FXR agonist 4 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FXR agonist 4 (compound 10a) is an agonist of farnesoid X receptor (FXR) with an EC50 value of 1.05 μM. FXR agonist 4 effectively improves hyperlipidemia, hepatic steatosis, insulin resistance and hepatic inflammation in DIO mice. FXR agonist 4 can be used for the research of non-alcoholic fatty liver disease (NAFLD)[1].

体外研究
(In Vitro)

FXR agonist 4 (10 nM-10 μM) 对 FXR 具有激动活性，在 HEK293T 细胞中的 EC50 值为 1.05 μM[1]。
FXR agonist 4 (1 nM-10 μM) 剂量依赖性地增加类固醇受体辅激活物 SRC-2 募集，EC50 值为 1.04 μM[1]。
FXR agonist 4 (0.1 nM-10 μM) 可激活脂肪堆积的细胞中的 FXR[1]。
FXR agonist 4 (10-50 μM; 48 h) 对 HepG2 细胞无毒性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

FXR agonist 4 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: HepG2 cell line
Concentration: 10, 30 and 50 μM
Incubation Time: 48 hours
Result: Showed no toxic effects to HepG2 cells at the testing dose up to 50 μM.
体内研究
(In Vivo)

FXR agonist 4 (100 mg/kg；口服给药，一次) 改善 DIO 小鼠的高脂血症，肝脏脂肪变性，胰岛素抵抗和肝脏炎症[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: High fat diet (HFD)-induced C57BL/6J obese (DIO) mice[1]
Dosage: 100 mg/kg
Administration: Oral administration; 100 mg/kg once
Result: Decreased blood triglyceride, total cholesterol and low-density lipoprotein cholesterol levels of DIO mice after treatment for 3 week. Significantly decreased the serum alanine aminotransferase (ALT) level and promoted cholesterol excretion after treatment for 45 days. Increased the expression of Srebp1c, stearoyl-CoA desaturase 1 (Scd1), fatty acid synthetase (Fasn), Diac ylgycerol Acyltransferase 2 (Dgat2), 3 Hydroxy-3-methylglutaryl Coenzyme A Reductase (Hmgcr) and sterol regulatory element binding protein 2 (Srebp2). Improved insulin sensitivity of DIO mice. Reduced mRNA levels of interleukin 1 beta (Il-1β), Il5, Il6, cluster of differentiation 36 (Cd36), inducible nitric oxide synthase (iNOS) and mouse EGF-like module-containing mucin-like hormone receptor-like 1 (F4/80).
分子量

373.92

Formula

C21H28ClN3O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

FXR agonist 4 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

FXR agonist 43025841-47-5FXR agonist4FXR agonist-4FXRNR1H4XJ034piperazine ringOCANAFLDinsulinhepatic inflammationDIO miceInhibitorinhibitorinhibit

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