FXR agonist 3
Based on 1 publication(s) in Google Scholar
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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- Reinheit : 96.51%
- CAS. Nr.: 3037847-72-3
- Formel: C28H28BrNO4
- Molecular Weight:522.43
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) FXR agonist 3
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Biologische Aktivität
Beschreibung
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LX-2 | CC50 |
70.36 μM
Compound: 3a
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Cytotoxicity against human LX2 cells assessed as inhibition of cell growth
Cytotoxicity against human LX2 cells assessed as inhibition of cell growth
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[PMID: 36347091] |
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. Further protocols information, click here.
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Cell Line:LX-2 cells
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Concentration:0, 2.5, 5, 7.5, and 10 μM
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Incubation Time:24 hours; with or without 2 ng/mL TGF-β1 for another 24 hr
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Result:Decreased COL1A1, TGF-β1, α-SMA, and TIMP1 protein expressions in a dose-dependent manner.
In Vivo
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.
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Animal Model:C57BL/6 N mice fed CDAHFD diet for 16 weeks[1]
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Dosage:200 mg/kg
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Administration:Oral gavage; daily for 4 weeks after CDAHFD-induced
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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.
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Animal Model:C57BL/6 N mice inuced with BDL[1]
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Dosage:200 mg/kg
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Administration:Oral gavage; daily for 4 weeks after induced
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Result:Protected liver from accumulated bile acid-induced injury.
Increased the expression of FXR and decreased the expression of NTCP in BDL rats.
Chemical Information
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CAS. Nr. 3037847-72-3
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Appearance Solid
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Molecular Weight 522.43
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Formel C28H28BrNO4
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Color Light yellow to yellow
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SMILES
COC1=C(C=C2C(CC[N+]3=C2C=C4C=CC(OC)=C(C4=C3)OCC5=CC(C)=CC=C5)=C1)OC.[Br-]
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Science
2026 Feb 5;391(6785):eadz4075. PMID: 41643022
Lösungsmittel & Löslichkeit
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.
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Protokoll
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Fibrosis/Collagen Morphometry
Fibrosis and collagen morphometry is based on the quantitative visualization of fibrillar collagen deposition in tissue sections using histochemical stains such as Sirius Red (Picrosirius Red) or Masson's trichrome, followed by image-based or polarization-enhanced analysis to estimate collagen proportional area as a surrogate of extracellular matrix accumulation during fibrotic remodeling. Sirius Red combined with polarized light microscopy enhances detection of collagen fibers due to birefringence properties, enabling more specific visualization of collagen type I and III fibrils compared to conventional bright-field histology, while whole-section or region-restricted digital morphometry reduces field-selection bias in fibrosis assessment. Alternative quantitative approaches include second harmonic generation (SHG) and two-photon excited fluorescence microscopy, which enable label-free detection of fibrillar collagen and have been validated against histological staining and biochemica
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Collagen: Sirius Red Staining
Sirius Red or picrosirius red staining is a histochemical method for visualizing collagen-rich extracellular matrix in tissue sections, and collagen fibers are detected as red-stained structures under bright-field microscopy with enhanced birefringence under polarized light. Picrosirius red is useful for assessing total collagen organization, distribution, and fibrosis burden, but polarized color should not be interpreted as a definitive collagen type I versus type III readout because color is affected by fiber orientation, thickness, and packing.
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Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
Masson’s Trichrome (collagen/trichrome staining) is a histological technique that differentially stains tissue compartments using sequential acidic dyes to distinguish collagen from muscle and cytoplasmic components based on dye affinity and tissue permeability differences, enabling visualization of fibrosis and connective tissue architecture in histological sections. The classical formulation typically uses Weigert's iron hematoxylin for nuclear staining, Biebrich scarlet-acid fuchsin for cytoplasm and muscle, and aniline blue (or light green variants) for collagen, producing a characteristic blue/green collagen signal contrasted against red cytoplasm and dark nuclei. The staining principle relies on selective displacement of smaller dye molecules by larger anionic dyes in collagen-rich regions under controlled acidified conditions, which enhances collagen-specific dye retention. This property makes the method widely used for fibrosis assessment in organs such as heart, liver, lung, a
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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Liver Histomorphometry
Liver histomorphometry is a quantitative histological approach used to measure structural alterations in hepatic tissue, including parenchymal loss, steatosis, fibrosis, and vascular remodeling, by combining stained tissue section analysis with stereological or computerized image-based measurements. Classical morphometric frameworks quantify volume fractions of liver compartments and fibrotic regions using systematic sampling and image analysis, enabling objective comparison of pathological changes across experimental groups. These approaches are widely applied in liver cirrhosis and fibrosis studies to reduce subjectivity in histological scoring and improve reproducibility of tissue evaluation. Recent methodological advances integrate automated image analysis and radiomics-based extraction of histological features from standard liver stains (e. g. , H&E and fibrotic stains), enabling quantitative correlation between morphometric features and fibrosis stages in non-alcoholic fatty live
Reinheit & Dokumentation
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Data Sheet (281 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
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 |