2. Metabolic Enzyme/Protease GPCR/G Protein Apoptosis NF-κB Immunology/Inflammation
  3. FXR G protein-coupled Bile Acid Receptor 1 TNF Receptor Reactive Oxygen Species (ROS)
  4. FXR agonist 17

FXR agonist 17 是一种口服有效的、甾体类的 FXR 激动剂，其 EC50 值分别为 42.2 (TR-FRET) 和 176.4 (荧光素酶报告基因实验) nM。FXR agonist 17 可激活 TGR5 (EC₅₀ = 2.6 μM)，但不会激活 hMRGPRX4。FXR agonist 17 具有抗炎、保肝和抗纤维化作用，可改善代谢功能障碍相关脂肪性肝炎 (NAFLD) 活动度评分并降低肝纤维化严重程度。FXR agonist 17 可用于 NAFLD、胆汁淤积性肝病和肝纤维化的研究。

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FXR agonist 17

FXR agonist 17 Chemical Structure

CAS No. : 3107769-23-0

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FXR agonist 17 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 17 is an orally active, steroidal FXR agonist with EC50 values of 42.2 nM (TR-FRET) and 176.4 nM (luciferase reporter assay), respectively. FXR agonist 17 activates TGR5 (EC50 = 2.6 μM) but does not activate hMRGPRX4. FXR agonist 17 exerts anti-inflammatory, hepatoprotective and antifibrotic effects, improves the non-alcoholic steatohepatitis (NAFLD) activity score and reduces the severity of liver fibrosis. FXR agonist 17 can be used for the research of NAFLD, cholestatic liver disease and liver fibrosis[1].

体外研究
(In Vitro)

FXR agonist 17 (Compound 10) (0.5-100 μM; 25 h) 在浓度≤ 40 μM 时对 RAW264.7 小鼠巨噬细胞无细胞毒性作用，但在浓度≥ 60 μM 时会降低细胞活力[1]。
FXR agonist 17 (Compound 10) (5-20 μM; 25 h) 可通过激活 FXR 呈剂量依赖性地减轻 RAW264.7 小鼠巨噬细胞中 LPS (HY-D1056) 诱导的炎症反应，其显著作用包括降低亚硝酸盐、TNF-α 和 ROS 水平，以及调控胆汁酸代谢和炎症相关基因的表达[1]。
FXR agonist 17 (0-500 μM; 25 h) 在 HEK-293、HepG2 和 HEK-293 T 细胞中的 IC50 值分别为 62.2 μM、57 μM 和 46.3 μM[1]。

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

FXR agonist 17 相关抗体:

Cell Viability Assay[1]

Cell Line: RAW264.7 mouse macrophages
Concentration: 0.5, 1, 2, 5, 10, 20, 40, 60, 80, 100 μM
Incubation Time: 1 h pretreatment; 24 h LPS stimulation
Result: Showed no significant decrease in cell viability at concentrations ≤ 40 μM; showed significant cytotoxicity at 60, 80, and 100 μM.
药代动力学
(Parmacokinetics)
Species Dose Route Bioavailability T1/2 Tmax Cmax AUC0-24 CL
Rat[1] 2 mg/kg i.v. / 1.27 h 0.0333 h 8210 ng/mL 2540 ng·h/mL 824 mL/h/kg
Rat[1] 10 mg/kg p.o. 18.5 % 1.66 h 1.67 h 636 ng/mL 2340 ng·h/mL 3970 mL/h/kg
体内研究
(In Vivo)

FXR agonist 17 (Compound 10) (20 mg/kg；口服；每日一次；连续 5 天) 可显著减轻经 ANIT 处理的雄性 C57BL/6 小鼠的胆汁淤积性肝损伤[1]。
FXR agonist 17 (20 mg/kg；口服；每日一次；28 天) 可显著减轻 CCl4 处理的雄性 C57BL/6 小鼠的肝纤维化[1]。
FXR agonist 17 (20 mg/kg；口服；每日一次；连续 28 天，于 12 周诱导期的第 8-12 周给药) 可显著改善雄性 C57BL/6 小鼠的肝脏病理状况[1]。

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

Animal Model: C57BL/6 (male, 6-8 weeks old, SPF-grade, ANIT-induced)[1]
Dosage: 20 mg/kg
Administration: p.o.; daily; 5 days
Result: Significantly reduced serum levels of ALP, TBA, and TBIL relative to the ANIT-induced group.
Reduced liver injury as evidenced by decreased cellular necrosis, inflammatory infiltration, and hemorrhage on H&E staining.
Lowered average H&E liver injury score to 4.0, compared to 6.2 in the ANIT-induced group.
Animal Model: C57BL/6 (male, 6-8 weeks old, SPF-grade, CCl4-induced)[1]
Dosage: 20 mg/kg
Administration: p.o.; daily; 28 days
Result: Significantly reduced serum levels of TBA and TBIL relative to the CCl4-induced group.
Reduced hepatic collagen accumulation, with Sirius red-positive staining area decreasing to 1.48% from 1.98% in the CCl4-induced group.
Animal Model: C57BL/6 (male, 6-8 weeks old, SPF-grade, high-sugar high-fat diet + CCl4-induced)[1]
Dosage: 20 mg/kg
Administration: p.o.; daily; 28 days (administered during weeks 8-12 of 12-week induction period)
Result: Significantly reduced serum levels of TC, HDL, and LDL relative to the MASH group.
Reduced hepatic triglyceride and total cholesterol levels relative to the MASH group.
Improved liver histopathology with reduced steatosis, lobular inflammation, and hepatocyte ballooning.
Lowered NAFLD activity score (NAS) to 4.0 from 5.9 in the MASH group.
Reduced hepatic collagen accumulation, with Sirius red-positive staining area decreasing to 1.75% from 2.55% in the MASH group.
分子量

502.75

Formula

C29H46N2O3S
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 17 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FXR agonist 173107769-23-0FXR agonist17FXR agonist-17FXRG protein-coupled Bile Acid Receptor 1TNF ReceptorReactive Oxygen Species (ROS)NR1H4G-protein coupled receptor 19GPCR19TGR5GPBAR1Tumor Necrosis Factor ReceptorTNFRC57BL/6 micehMRGPRX4cholestatic liver diseaseRAW264.7 mouse macrophagesliver fibrosismetabolic dysfunction-associated steatohepatitisCHO-K1 cellsHEK-293 cellsNAFLDInhibitorinhibitorinhibit

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