Elobixibat
Based on 1 publication(s) in Google Scholar
Elobixibat (A 3309; AZD 7806) is an orally active, bile acid transporter (IBAT) inhibitor with IC50 values ??of 0.53 nM (human IBAT), 0.13 nM (mouse IBAT), and 5.8 nM (canine IBAT). Elobixibat can lower LDL cholesterol, increase serum GLP-1, promote colonic motility, and has the potential to study metabolic syndrome. Elobixibat can be used in the study of chronic functional constipation (CIC), dyslipidemia, non-alcoholic hepatitis, and liver tumors in the elderly.
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- Pureza: 99.91%
- No. CAS: 439087-18-0
- Fòrmula: C36H45N3O7S2
- Peso molecular:695.89
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Almacenamiento: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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Actividad biológica
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Elobixibat
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Actividad biológica
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IBAT 0.53 nM (IC50) |
IL-6 |
TNF-α |
TNF-β |
Elobixibat (0.2, 0.6, 1.2 mg/kg/d; gavage; 5 days per week) improves NASH-related histopathology, reduces cytokine (TNF-α, IL-6, and TGF-β) expression, and normalizes gut microbial composition in a non-steatohepatitis (NASH) mouse model[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mouse Model of Nonalcoholic Steatohepatitis (three-week-old male C57BL/6J mice)[2]
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Dosage:0.27 mg/kg/day for 20 weeks
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Administration:p.o.
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Result:Reduced the number and size of tumors.
Significantly reduced the number of Gram-positive bacteria in the phyla Firmicutes, Deferobacteria and Actinobacteria and increased the number of Proteobacteria.
Chemical Information
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No. CAS 439087-18-0
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Appearance Solid
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Peso molecular 695.89
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Fòrmula C36H45N3O7S2
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Color White to off-white
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SMILES
O=C(O)CNC([C@@H](C1=CC=CC=C1)NC(COC2=C(SC)C=C(C3=C2)N(C4=CC=CC=C4)CC(CCCC)(CCCC)CS3(=O)=O)=O)=O
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Synonyms
A 3309; AZD 7806
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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
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Metab
Alterations in intestinal bile acid transport provide a therapeutic target in patients with post-bariatric hypoglycaemia. [Abstract]2025 Apr;7(4):792-807. PMID: 40186075
Solvente y solubilidad
DMSO : 250 mg/mL (359.25 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)
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: ≥ 2.08 mg/mL (2.99 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 2.08 mg/mL (2.99 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 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 (20.8 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.
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Wong BS, et al. Elobixibat for the treatment of constipation. Expert Opin Investig Drugs. 2013 Feb; 22(2):277-84. [Content Brief]
[2]. Sugiyama Y, et al. Impact of elobixibat on liver tumors, microbiome, and bile acid levels in a mouse model of nonalcoholic steatohepatitis. Hepatol Int. 2023 Dec;17(6):1378-1392. [Content Brief]
[3]. Yamauchi R, et al. Elobixibat, an ileal bile acid transporter inhibitor, ameliorates non-alcoholic steatohepatitis in mice. Hepatol Int. 2021 Apr;15(2):392-404. [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 | 1.4370 mL | 7.1850 mL | 14.3701 mL | 35.9252 mL |
| 5 mM | 0.2874 mL | 1.4370 mL | 2.8740 mL | 7.1850 mL | |
| 10 mM | 0.1437 mL | 0.7185 mL | 1.4370 mL | 3.5925 mL | |
| 15 mM | 0.0958 mL | 0.4790 mL | 0.9580 mL | 2.3950 mL | |
| 20 mM | 0.0719 mL | 0.3593 mL | 0.7185 mL | 1.7963 mL | |
| 25 mM | 0.0575 mL | 0.2874 mL | 0.5748 mL | 1.4370 mL | |
| 30 mM | 0.0479 mL | 0.2395 mL | 0.4790 mL | 1.1975 mL | |
| 40 mM | 0.0359 mL | 0.1796 mL | 0.3593 mL | 0.8981 mL | |
| 50 mM | 0.0287 mL | 0.1437 mL | 0.2874 mL | 0.7185 mL | |
| 60 mM | 0.0240 mL | 0.1198 mL | 0.2395 mL | 0.5988 mL | |
| 80 mM | 0.0180 mL | 0.0898 mL | 0.1796 mL | 0.4491 mL | |
| 100 mM | 0.0144 mL | 0.0719 mL | 0.1437 mL | 0.3593 mL |
Elobixibat Related Classifications
HY-15790 Related Classifications
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