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

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

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

Obeticholic acid (INT-747) is a potent and selective farnesoid X receptor (FXR) agonist with an EC50 of 99 nM.

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 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
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10 mg USD 84 In-stock
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50 mg USD 150 In-stock
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100 mg USD 290 In-stock
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200 mg USD 450 In-stock
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500 mg USD 650 In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

Top Publications Citing Use of Products

    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 and selective farnesoid X receptor (FXR) agonist with an EC50 of 99 nM.

    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].

    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].

    Clinical Trial
    Molecular Weight

    420.63

    Formula

    C₂₆H₄₄O₄

    CAS No.

    459789-99-2

    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:  10% DMSO    40% PEG300    5% Tween-80    45% saline

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

    • 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% EtOH    40% PEG300    5% Tween-80    45% saline

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

    • 5.

      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

    • 6.

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

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

    *All of the co-solvents are provided by MCE.
    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

    Purity: >98.0%

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    Product Name:
    Obeticholic acid
    Cat. No.:
    HY-12222
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