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

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.

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FXR agonist 3 Chemical Structure

FXR agonist 3 Chemical Structure

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Based on 1 publication(s) in Google Scholar

FXR agonist 3 Related Antibodies

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Description

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].

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

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

FXR agonist 3 Related Antibodies

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.
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].

MedChemExpress (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.
Molecular Weight

522.43

Formula

C28H28BrNO4
Appearance

Solid

Color

Light yellow to yellow

SMILES

COC1=C(C=C2C(CC[N+]3=C2C=C4C=CC(OC)=C(C4=C3)OCC5=CC(C)=CC=C5)=C1)OC.[Br-]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 250 mg/mL (478.53 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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FXR agonist 3 Related Classifications

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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