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%
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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10 mM * 1 mL in DMSO USD 55 In-stock
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Customer Review

Based on 38 publication(s) in Google Scholar

Top Publications Citing Use of Products

37 Publications Citing Use of MCE Obeticholic acid

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

    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].

    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].

    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.
    SMILES
    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)

    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
    10 mM 0.2377 mL 1.1887 mL 2.3774 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  1% Methylcellulose(MC)

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

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    • 4.

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

      Solubility: ≥ 4.76 mg/mL (11.32 mM); Clear solution

    • 5.

      Add each solvent one by one:  10% EtOH    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.94 mM); Clear solution

    • 6.

      Add each solvent one by one:  10% EtOH    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (5.94 mM); Clear solution

    • 7.

      Add each solvent one by one:  10% EtOH    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.94 mM); Clear solution

    • 8.

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (5.94 mM); Clear solution

    *All of the co-solvents are available by MCE.
    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
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    Product Name:
    Obeticholic acid
    Cat. No.:
    HY-12222
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