EDP-305
Based on 1 Customer Validation
EDP-305 is an orally active, potent and selective farnesoid X receptor (FXR) agonist, with EC50 values of 34 nM (chimeric FXR in CHO cells) and 8 nM (full-length FXR in HEK cells). EDP-305 shows a potent and consistent antifibrotic effect. EDP-305 can be used for primary biliary cholangitis (PBC) and non-alcoholic steatohepatitis (NASH) research.
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- Purity: 96.02%
- CAS No.: 1933507-63-1
- 화학식: C36H58N2O5S
- 분자량:630.92
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보관: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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
IC50: 8 ± 3 nM (Full-length FXR in HEK cells), 34 ± 8 nM (Chimeric FXR in CHO cells), >15000 nM (TGR5 in CHO cells)[2]
EDP‐305 (10 μM, 72 h) directly activates FXR in liver hepatoctyes but not stellate cells[1].
EDP-305 (0-5 μM, 16 h) increases the expression of the FXR target gene, SHP, and downregulates CYP7A1 expression in HepaRG hepatocytes[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Hepatic stellate cell (HSC) lines, primary HSCs and hepatocytes
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Concentration:10 μM
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Incubation Time:72 h
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Result:Induced mRNA expression of SHP and FGF19 in human hepatocytes, and elicited no induction of downstream targets SHP or FGF15/19 in stellate lines.
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Cell Line:HepaRG hepatocytes
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Concentration:0.05, 0.1, 0.5, 1, 5, 10, 50, 100, 500, 1000, 5000 nM
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Incubation Time:16 h
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Result:Dose-dependently increased the expression of the FXR target gene, SHP, and downregulated CYP7A1 expression in HepaRG hepatocytes.
EDP‐305 (0-30 mg/kg, Oral gavage, daily for 6 weeks) reduces liver fibrosis in a dose-dependent manner in CDAHFD mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male CD rats (underwent BDL, n=24, n=8 for each group)[1]
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Dosage:0, 10 and 30 mg/kg
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Administration:Oral gavage, daily, started on day 4 after BDL and continued until days 17-18
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Result:Significantly reduced alanine aminotransferase and aspartate aminotransferase. Showed a dose-dependent reduction in CPA. Reduced hydroxyproline levels in whole liver tissue samples. Reduced messenger RNA (mRNA) relative quantification (RQ) for both Col1a1 and actin, alpha 2, smooth muscle, aorta (Acta2).
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Animal Model:Male C57BL/6 mice (n = 24, fed a CDAHFD consisting of 60% kcal fat and 0.1% methionine)[1]
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Dosage:0, 10 and 30 mg/kg
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Administration:Oral gavage, daily, started at the beginning of week 6 on the diet and were continued until week 12
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Result:Reduced serum triglycerides, and significantly reduced hydroxyproline and MR liver signal intensity in a dose-dependent manner. Showed a dose‐dependent reduction in mRNA expression of lysyl oxidase genes Lox and Loxl1-4.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1933507-63-1
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Appearance Solid
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분자량 630.92
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화학식 C36H58N2O5S
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Color White to off-white
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SMILES
O[C@H]1[C@]2([H])[C@@](CC[C@]3([C@@]2([H])CC[C@]3([H])[C@H](C)CCNC(NS(=O)(C4=CC=C(C=C4)C(C)(C)C)=O)=O)C)([H])[C@@]5([C@](C[C@@H](CC5)O)([H])[C@H]1CC)C
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : ≥ 100 mg/mL (158.50 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.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (3.96 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (3.96 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
순도&문서
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Data Sheet (278 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)
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 |
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| DMSO | 1 mM | 1.5850 mL | 7.9249 mL | 15.8499 mL | 39.6247 mL |
| 5 mM | 0.3170 mL | 1.5850 mL | 3.1700 mL | 7.9249 mL | |
| 10 mM | 0.1585 mL | 0.7925 mL | 1.5850 mL | 3.9625 mL | |
| 15 mM | 0.1057 mL | 0.5283 mL | 1.0567 mL | 2.6416 mL | |
| 20 mM | 0.0792 mL | 0.3962 mL | 0.7925 mL | 1.9812 mL | |
| 25 mM | 0.0634 mL | 0.3170 mL | 0.6340 mL | 1.5850 mL | |
| 30 mM | 0.0528 mL | 0.2642 mL | 0.5283 mL | 1.3208 mL | |
| 40 mM | 0.0396 mL | 0.1981 mL | 0.3962 mL | 0.9906 mL | |
| 50 mM | 0.0317 mL | 0.1585 mL | 0.3170 mL | 0.7925 mL | |
| 60 mM | 0.0264 mL | 0.1321 mL | 0.2642 mL | 0.6604 mL | |
| 80 mM | 0.0198 mL | 0.0991 mL | 0.1981 mL | 0.4953 mL | |
| 100 mM | 0.0158 mL | 0.0792 mL | 0.1585 mL | 0.3962 mL |
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