2. Membrane Transporter/Ion Channel
  3. Apical Sodium-Dependent Bile Acid Transporter
  4. Odevixibat

Odevixibat (A4250) is a selective and orally active ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor. Odevixibat decreases cholestatic liver and bile duct injury in mice model. Odevixibat has the potential for the treatment of primary biliary cirrhosis.

For research use only. We do not sell to patients.

Odevixibat Chemical Structure

Odevixibat Chemical Structure

CAS No. : 501692-44-0

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Based on 3 publication(s) in Google Scholar

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Description

Odevixibat (A4250) is a selective and orally active ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor. Odevixibat decreases cholestatic liver and bile duct injury in mice model. Odevixibat has the potential for the treatment of primary biliary cirrhosis[1].

IC50 & Target

ASBT[1].
In Vivo

Odevixibat (A4250)(0.01% (w/w) in chow diet; 4 weeks) improves sclerosing cholangitis and significantly reduces serum alanine aminotransferase, alkaline phosphatase and BAs levels, hepatic expression of pro-inflammatory and pro-fibrogenic genes and bile duct proliferation in Mdr2-/- mice[1].
In addition, Odevixibat (A4250) significantly reduces bile flow and biliary BA output, which correlates with reduced bsep transcription, while Ntcp and Cyp7a1 are induced[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Eight week old Mdr2-/- (Abcb4-/-) mice (model of cholestatic liver injury and sclerosing cholangitis)[1]
Dosage: 0.01% (w/w) in chow diet
Administration: 4 weeks
Result: Decreased cholestatic liver and bile duct injury in mice model.
Clinical Trial
Molecular Weight

740.93

Formula

C37H48N4O8S2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC[C@H](NC([C@H](NC(COC1=C(SC)C=C(C2=C1)N(C3=CC=CC=C3)CC(CCCC)(CCCC)NS2(=O)=O)=O)C4=CC=C(O)C=C4)=O)C(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 166.67 mg/mL (224.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3497 mL 6.7483 mL 13.4966 mL
5 mM 0.2699 mL 1.3497 mL 2.6993 mL
View the 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 4.17 mg/mL (5.63 mM); Clear solution

    This protocol yields a clear solution of ≥ 4.17 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (41.7 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 4.17 mg/mL (5.63 mM); Clear solution

    This protocol yields a clear solution of ≥ 4.17 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (41.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
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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% 
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%
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%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
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 (stored under nitrogen). 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 1.3497 mL 6.7483 mL 13.4966 mL 33.7414 mL
5 mM 0.2699 mL 1.3497 mL 2.6993 mL 6.7483 mL
10 mM 0.1350 mL 0.6748 mL 1.3497 mL 3.3741 mL
15 mM 0.0900 mL 0.4499 mL 0.8998 mL 2.2494 mL
20 mM 0.0675 mL 0.3374 mL 0.6748 mL 1.6871 mL
25 mM 0.0540 mL 0.2699 mL 0.5399 mL 1.3497 mL
30 mM 0.0450 mL 0.2249 mL 0.4499 mL 1.1247 mL
40 mM 0.0337 mL 0.1687 mL 0.3374 mL 0.8435 mL
50 mM 0.0270 mL 0.1350 mL 0.2699 mL 0.6748 mL
60 mM 0.0225 mL 0.1125 mL 0.2249 mL 0.5624 mL
80 mM 0.0169 mL 0.0844 mL 0.1687 mL 0.4218 mL
100 mM 0.0135 mL 0.0675 mL 0.1350 mL 0.3374 mL
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Odevixibat Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Odevixibat501692-44-0A4250A 4250A-4250Apical Sodium-Dependent Bile Acid TransporterASBTIleal Bile Acid TransporterIBATSLC10A2primary biliarycirrhosischolestatic liverbile duct injuryInhibitorinhibitorinhibit

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