Linafexor
Based on 1 Customer Validation
Linafexor (CS-0159) is a FXR agonist and bile acid homeostasis modulator. Linafexor exerts its effects by activating FXR, a regulator of liver function. Linafexor is applicable to research related to primary sclerosing cholangitis (PSC). Linafexor is also suitable for research in the field of metabolic dysfunction-associated steatohepatitis (MASH).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.58%
- CAS 番号: 2765593-43-7
- 分子式: C28H25Cl2FN4O4
- 分子量:571.43
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2765593-43-7
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性状 Solid
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分子量 571.43
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分子式 C28H25Cl2FN4O4
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Color White to off-white
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SMILES
ClC(C=CC=C1Cl)=C1C2=NOC(C3CC3)=C2CO[C@@H]4C[C@@]5([H])N(C6=CC(F)=C(C7=NOC(N7)=O)C=C6)[C@@](CC5)([H])C4
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別名
CS-0159
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (175.00 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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 (4.37 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
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.
純度とドキュメンテーション
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データシート (275 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Pham HN, et al. Navigating the liver landscape: upcoming pharmacotherapies for primary sclerosing cholangitis. Expert Opin Pharmacother. 2024;25(7):895-906. [Content Brief]
[2]. Chai SY, et al. Epidemiology of metabolic dysfunction-associated steatotic liver disease/metabolic dysfunction-associated steatohepatitis and associated cardiometabolic factors in adults in China (2013-2023): A systematic review and meta-analysis. World J Gastroenterol. 2025;31(46):113608. [Content Brief]
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 | 1.7500 mL | 8.7500 mL | 17.5000 mL | 43.7499 mL |
| 5 mM | 0.3500 mL | 1.7500 mL | 3.5000 mL | 8.7500 mL | |
| 10 mM | 0.1750 mL | 0.8750 mL | 1.7500 mL | 4.3750 mL | |
| 15 mM | 0.1167 mL | 0.5833 mL | 1.1667 mL | 2.9167 mL | |
| 20 mM | 0.0875 mL | 0.4375 mL | 0.8750 mL | 2.1875 mL | |
| 25 mM | 0.0700 mL | 0.3500 mL | 0.7000 mL | 1.7500 mL | |
| 30 mM | 0.0583 mL | 0.2917 mL | 0.5833 mL | 1.4583 mL | |
| 40 mM | 0.0437 mL | 0.2187 mL | 0.4375 mL | 1.0937 mL | |
| 50 mM | 0.0350 mL | 0.1750 mL | 0.3500 mL | 0.8750 mL | |
| 60 mM | 0.0292 mL | 0.1458 mL | 0.2917 mL | 0.7292 mL | |
| 80 mM | 0.0219 mL | 0.1094 mL | 0.2187 mL | 0.5469 mL | |
| 100 mM | 0.0175 mL | 0.0875 mL | 0.1750 mL | 0.4375 mL |