FXR agonist 4
Based on 1 Customer Validation
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).
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- Pureté: 99.37%
- CAS No.: 3025841-47-5
- Formule: C21H28ClN3O
- Masse moléculaire:373.92
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
FXR agonist 4 (10 nM-10 μM) shows FXR agonistic activity with an EC50 value of 1.05 μM in HEK293T cells[1]. FXR agonist 4 (1 nM-10 μM) dose-dependently increarses steroid receptor coactivator (SRC)-2 recruitment with an EC50 value of 1.04 μM[1]. FXR agonist 4 (0.1 nM-10 μM) activates FXR in cells with fatty accumulation[1]. FXR agonist 4 (10-50 μM; 48 h) is not toxic to HepG2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cell line
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Concentration:10, 30 and 50 μM
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Incubation Time:48 hours
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Result:Showed no toxic effects to HepG2 cells at the testing dose up to 50 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:High fat diet (HFD)-induced C57BL/6J obese (DIO) mice[1]
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Dosage:100 mg/kg
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Administration:Oral administration; 100 mg/kg once
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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).
Chemical Information
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CAS No. 3025841-47-5
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Appearance Solid
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Masse moléculaire 373.92
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Formule C21H28ClN3O
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Color Off-white to light brown
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SMILES
ClC1=CC(N2CCN(C(C34C[C@@H]5C[C@H](C4)C[C@@H](C5)C3)=O)CC2)=C(N)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (267.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (277 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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Instruction de manipulation (2659 KB)
Références
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 |
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| DMSO | 1 mM | 2.6744 mL | 13.3718 mL | 26.7437 mL | 66.8592 mL |
| 5 mM | 0.5349 mL | 2.6744 mL | 5.3487 mL | 13.3718 mL | |
| 10 mM | 0.2674 mL | 1.3372 mL | 2.6744 mL | 6.6859 mL | |
| 15 mM | 0.1783 mL | 0.8915 mL | 1.7829 mL | 4.4573 mL | |
| 20 mM | 0.1337 mL | 0.6686 mL | 1.3372 mL | 3.3430 mL | |
| 25 mM | 0.1070 mL | 0.5349 mL | 1.0697 mL | 2.6744 mL | |
| 30 mM | 0.0891 mL | 0.4457 mL | 0.8915 mL | 2.2286 mL | |
| 40 mM | 0.0669 mL | 0.3343 mL | 0.6686 mL | 1.6715 mL | |
| 50 mM | 0.0535 mL | 0.2674 mL | 0.5349 mL | 1.3372 mL | |
| 60 mM | 0.0446 mL | 0.2229 mL | 0.4457 mL | 1.1143 mL | |
| 80 mM | 0.0334 mL | 0.1671 mL | 0.3343 mL | 0.8357 mL | |
| 100 mM | 0.0267 mL | 0.1337 mL | 0.2674 mL | 0.6686 mL |
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