F44-A13
Based on 1 Customer Validation
F44-A13 is an orally active and highly selective farnesoid X receptor (FXR) antagonist with an IC50 value of 1.1 μM. F44-A13 can optimize cholesterol metabolism and reduce its activity by inducing CYP7A1 expression. F44-A13 reduces levels of cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-C) in mouse models. F44-A13 can be used in the study of metabolic diseases associated with lipid disorders.
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- Pureza: 96.73%
- No. CAS: 1338190-14-9
- Fòrmula: C28H40N4O5S
- Peso molecular:544.71
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
|
PPARα |
PPARβ |
RXR α |
RXRβ |
RXRγ |
RORγ |
F44-A13 demonstrates high selectivity towards various nuclear receptors, including retinoic acid receptor α/β/γ (RARα/β/γ), retinoid X receptor α/β/γ (RXRα/β/γ), pregnane X receptor (PXR), peroxisome proliferators-activated receptors α/β (PPARα/β), thyroid hormone receptor β (THRβ), and retinoic acid receptor-related orphan receptors γ (RORγ)[1].
F44-A13 (50 μM, 24 h) inhibites FXR transcriptional activity in a dose-dependent manner in the presence of 50 μM CDCA (HY-76847) with an IC50 value of 3.0 μM. F44-A13 is a low-toxicity, highly selective FXR antagonist[1].
F44-A13 (F44-A13: 3, 10, 30 μM; CDCA: 100 μM; 24 hours) can improve cholesterol metabolism and reduce cholesterol activity by inducing the expression of CYP7A1. F44-A13 can decrease the expression level of Shp and Bsep, and increase the expression level of CYP7A1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 , HEK293A cells
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Concentration:100 μM
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Incubation Time:24h
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Result:Was not cytotoxic to HepG2 and HEK293A cells
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Cell Line:HepG2 cells
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Concentration:F44-A13: 3, 10, 30 μM; CDCA: 100 μM
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Incubation Time:24h
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Result:Was able to reverse the regulation of FXR downstream target genes Shp, Bsep and Cyp7a1 by CDCA in a dose-dependent manner.
Decreased the expression level of Shp and Bsep, and increased the expression level of Cyp7a1.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice[1]
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Dosage:20, 40 mg/kg
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Administration:Intraperitoneal injection (i.p.) and Oral gavage (p.o.); 4 days
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Result:Intraperitoneal injection significantly reduced TC levels by more than 28%, and oral administration significantly reduced TC levels in a dose-dependent manner.
Reduced TG levels by more than 30% at both 20 and 40 mg/kg orally, while intraperitoneal injection did not significantly reduce TG levels.
Oral doses of 20 and 40 mg/kg were effective in reducing LDL-C levels by 12% and 23%, and intraperitoneal injections by 38%.
Chemical Information
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No. CAS 1338190-14-9
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Appearance Solid
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Peso molecular 544.71
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Fòrmula C28H40N4O5S
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Color White to light brown
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SMILES
CCN(C1=CC(OS(=O)(C2=CC=C(C=C2)NC(C)=O)=O)=C(C=C1)CN(C(NC(C)(C)C)=O)CC3CC3)CC
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (183.58 mM; ultrasonic and warming and heat to 60°C; 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 1.8358 mL | 9.1792 mL | 18.3584 mL | 45.8960 mL |
| 5 mM | 0.3672 mL | 1.8358 mL | 3.6717 mL | 9.1792 mL | |
| 10 mM | 0.1836 mL | 0.9179 mL | 1.8358 mL | 4.5896 mL | |
| 15 mM | 0.1224 mL | 0.6119 mL | 1.2239 mL | 3.0597 mL | |
| 20 mM | 0.0918 mL | 0.4590 mL | 0.9179 mL | 2.2948 mL | |
| 25 mM | 0.0734 mL | 0.3672 mL | 0.7343 mL | 1.8358 mL | |
| 30 mM | 0.0612 mL | 0.3060 mL | 0.6119 mL | 1.5299 mL | |
| 40 mM | 0.0459 mL | 0.2295 mL | 0.4590 mL | 1.1474 mL | |
| 50 mM | 0.0367 mL | 0.1836 mL | 0.3672 mL | 0.9179 mL | |
| 60 mM | 0.0306 mL | 0.1530 mL | 0.3060 mL | 0.7649 mL | |
| 80 mM | 0.0229 mL | 0.1147 mL | 0.2295 mL | 0.5737 mL | |
| 100 mM | 0.0184 mL | 0.0918 mL | 0.1836 mL | 0.4590 mL |
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