1. Metabolic Enzyme/Protease Autophagy
  2. FXR Autophagy
  3. Obeticholic acid

Obeticholic acid  (Synonyms: INT-747; 6-ECDCA; 6-Ethylchenodeoxycholic acid)

Cat. No.: HY-12222 Purity: ≥98.0%
COA Handling Instructions

Acide obéticholique (INT-747) est un agoniste de FXR qui est puissant, sélectif et actif par voie orale avec un EC50 de 99 nM. Acide obéticholique a un effet anticholérétique et anti-inflammatoire. Acide obéticholique induit également l'autophagie.

Obeticholsäure (INT-747) ist ein potenter, selektiver und oral aktiver FXR-Agonist mit einer EC50 von 99 nM. Obeticholsäure hat eine anticholeretische und entzündungshemmende Wirkung. Obeticholsäure induziert auch autophagy.

Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy.

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

Obeticholic acid Chemical Structure

Obeticholic acid Chemical Structure

CAS No. : 459789-99-2

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Customer Review

Based on 57 publication(s) in Google Scholar

Other Forms of Obeticholic acid:

Top Publications Citing Use of Products

56 Publications Citing Use of MCE Obeticholic acid

WB

    Obeticholic acid purchased from MedChemExpress. Usage Cited in: J Am Soc Nephrol. 2018 Nov;29(11):2658-2670.  [Abstract]

    Western blots show that INT-767, INT-777, and INT747 upregulate AQP2 protein expression.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy[1][2][3].

    IC50 & Target

    EC50: 99 nM (FXR)

    In Vitro

    Obeticholic acid (INT-747) increases the expression of FXR-regulated genes in rat hepatocytes[1]. Obeticholic acid (INT-747) reduces expression of liver JNK-1 and JNK-2[2]. Obeticholic acid (INT-747) (256 μg/mL) shows complete inhibition of bacterial growth in all strains tested. Intestinal permeability remains unaffected after INT-747-addition to an IFN-γ-exposed intestinal epithelium of Caco-2 cells[3].

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

    In Vivo

    Obeticholic acid (INT-747) (10 mg/kg/day) completely reverted cholestasis induced by E217α. Administration of Obeticholic acid (INT-747) partially prevents the impairment in total bile acid output caused by E217α by increasing the relative abundance of β-MCA and TCDCA and TDCA[1]. Obeticholic acid (INT-747)7 (10 mg/kg) and HS increases the pulmonary congestion in the animals. INT-747 does not improve renal pathology in the HS-fed animals[2]. Obeticholic acid (INT-747) (5 mg/kg) significantly increases survival in BDL rats. Obeticholic acid (INT-747)-treated BDL rats exhibits a significant selective ileal increase in expression of pore-closing claudin-1. Ileal expression of ZO-1 is significantly up-regulated in INT-747-treated BDL rats[3].

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

    Clinical Trial
    Molecular Weight

    420.63

    Formula

    C26H44O4

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    C[C@@]([C@]1([H])[C@@H](CC)[C@H]2O)(CC[C@@H](O)C1)[C@]3([H])[C@]2([H])[C@@](CC[C@]4([H])[C@H](C)CCC(O)=O)([H])[C@]4(C)CC3

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (237.74 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : ≥ 50 mg/mL (118.87 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3774 mL 11.8869 mL 23.7739 mL
    5 mM 0.4755 mL 2.3774 mL 4.7548 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • 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)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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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    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 5 mg/mL (11.89 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
    • Protocol 2

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

      Solubility: ≥ 5 mg/mL (11.89 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  1% Methylcellulose(MC)

      Solubility: 5 mg/mL (11.89 mM); Suspension solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
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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).
    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

    Purity: ≥98.0%

    References
    Animal Administration
    [2]

    Initially, all animals (at 6-weeks age) are placed on a standard rodent diet for a week. Baseline blood and urine samples are collected and basal blood pressure (BP) is measured prior to grouping the animals. Subsequently, the animals are randomized into low (LS; n=9) or high salt (HS) diet groups. Hypertension is induced in the HS group by daily high-salt diet feeding and the group is subdivided to receive one of two doses of INT-747: low dose (10 mg/kg/day; n=15) or high dose (30 mg/kg/day; n=15) in 1% methylcellulose; or vehicle (1% methylcellulose in distilled water; n=15) orally everyday for 6 weeks. In parallel, the LS group also receive 1% methylcellulose. BP is measured weekly for the duration of the study as described below.

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

    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
    Ethanol / DMSO 1 mM 2.3774 mL 11.8869 mL 23.7739 mL 59.4347 mL
    5 mM 0.4755 mL 2.3774 mL 4.7548 mL 11.8869 mL
    10 mM 0.2377 mL 1.1887 mL 2.3774 mL 5.9435 mL
    15 mM 0.1585 mL 0.7925 mL 1.5849 mL 3.9623 mL
    20 mM 0.1189 mL 0.5943 mL 1.1887 mL 2.9717 mL
    25 mM 0.0951 mL 0.4755 mL 0.9510 mL 2.3774 mL
    30 mM 0.0792 mL 0.3962 mL 0.7925 mL 1.9812 mL
    40 mM 0.0594 mL 0.2972 mL 0.5943 mL 1.4859 mL
    50 mM 0.0475 mL 0.2377 mL 0.4755 mL 1.1887 mL
    60 mM 0.0396 mL 0.1981 mL 0.3962 mL 0.9906 mL
    80 mM 0.0297 mL 0.1486 mL 0.2972 mL 0.7429 mL
    100 mM 0.0238 mL 0.1189 mL 0.2377 mL 0.5943 mL
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    • 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.

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