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

FXR agonist 3 是一种抗 NASH 试剂，通过激活 FXR 起作用。FXR agonist 3 抑制 COL1A1、TGF-β1、α-SMA 和 TIMP1 的表达，具有抗纤维化活性。FXR agonist 3 显著减轻肝脏脂肪变性和炎症，改善肝纤维化水平。

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FXR agonist 3 Chemical Structure

FXR agonist 3 Chemical Structure

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规格 价格 是否有货 数量
1 mg ￥1300
In-stock
5 mg ￥3450
In-stock
10 mg ￥5520
In-stock
50 mg   询价  
100 mg   询价  

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Customer Review

FXR agonist 3 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FXR agonist 3 is an anti-NASH agent, acting by activating FXR. FXR agonist 3 inhibits COL1A1, TGF-β1, α-SMA and TIMP1 expression with anti-fibrogenic activity. FXR agonist 3 significantly reduces liver steatosis and inflammation, improves liver fibrosis level[1].

体外研究
(In Vitro)

FXR agonist 3 (compound 3a) (5 μM; 24 h) shows anti-fibrogenic activity, decreases multiple fibrogenic biomarkers level in LX-2 cells in a dose-dependent manner[1].
FXR agonist 3 shows cytotoxic concentration against LX2 cells with an CC50 value of 70.36 μM[1].

Metabolic stability of FXR agonist 3 in human, rat and mouse liver microsomes[1]

Species T1/2 (h) CLInt (mic) (μg/min/mg) CLInt (liver) (μg/min/mg) Remaining Ratio (%) (T=60 min)
Human 53.3 26.0 23.4 44.1
Rat 7.4 187.8 338.0 0.4
Mouse 7.4 187.9 744.1 39.0

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

FXR agonist 3 相关抗体:

Western Blot Analysis[1]

Cell Line: LX-2 cells
Concentration: 0, 2.5, 5, 7.5, and 10 μM
Incubation Time: 24 hours; with or without 2 ng/mL TGF-β1 for another 24 hr
Result: Decreased COL1A1, TGF-β1, α-SMA, and TIMP1 protein expressions in a dose-dependent manner.
体内研究
(In Vivo)

FXR agonist 3 (compound 3a) (200 mg/kg; p.o.; daily for 4 weeks) significantly attenuates the degree of liver fibrosis in choline-deficient, l-amino acid-defined, high-fat diet (CDAHFD)-induced NASH mice model[1].
FXR agonist 3 (200 mg/kg; p.o.; daily for 4 weeks) also exerts liver-protective and anti-fibrosis activities in bile duct ligation (BDL)-induced fibrosis rat model[1].

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

Animal Model: C57BL/6 N mice fed CDAHFD diet for 16 weeks[1]
Dosage: 200 mg/kg
Administration: Oral gavage; daily for 4 weeks after CDAHFD-induced
Result: Decreased expression of IL-1β and IL-6 in livers, indicating the liver-protective effect of 3a in CDAHFD mice may partially through inhibiting inflammasome activation.
Lowered the serum levels of biochemical markers of ALT, AST, ALP, LDH, LDL and TBiL significantly, while raised HDL and GLU levels.
Animal Model: C57BL/6 N mice inuced with BDL[1]
Dosage: 200 mg/kg
Administration: Oral gavage; daily for 4 weeks after induced
Result: Protected liver from accumulated bile acid-induced injury.
Increased the expression of FXR and decreased the expression of NTCP in BDL rats.
分子量

522.43

Formula

C28H28BrNO4
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 250 mg/mL (478.53 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9141 mL 9.5707 mL 19.1413 mL
5 mM 0.3828 mL 1.9141 mL 3.8283 mL
查看完整储备液配制表

* 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, 6 months; -20°C, 1 month。-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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

FXR agonist 3 相关分类

完整储备液配制表

* 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, 6 months; -20°C, 1 month。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9141 mL 9.5707 mL 19.1413 mL 47.8533 mL
5 mM 0.3828 mL 1.9141 mL 3.8283 mL 9.5707 mL
10 mM 0.1914 mL 0.9571 mL 1.9141 mL 4.7853 mL
15 mM 0.1276 mL 0.6380 mL 1.2761 mL 3.1902 mL
20 mM 0.0957 mL 0.4785 mL 0.9571 mL 2.3927 mL
25 mM 0.0766 mL 0.3828 mL 0.7657 mL 1.9141 mL
30 mM 0.0638 mL 0.3190 mL 0.6380 mL 1.5951 mL
40 mM 0.0479 mL 0.2393 mL 0.4785 mL 1.1963 mL
50 mM 0.0383 mL 0.1914 mL 0.3828 mL 0.9571 mL
60 mM 0.0319 mL 0.1595 mL 0.3190 mL 0.7976 mL
80 mM 0.0239 mL 0.1196 mL 0.2393 mL 0.5982 mL
100 mM 0.0191 mL 0.0957 mL 0.1914 mL 0.4785 mL
Help & FAQs
  • 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 3FXR agonist3FXR agonist-3FXRNR1H4Inhibitorinhibitorinhibit

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