1. Metabolic Enzyme/Protease
  2. FXR
  3. INT-747

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

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

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.

INT-747 Chemical Structure

INT-747 Chemical Structure

CAS No. : 459789-99-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 84 In-stock
Estimated Time of Arrival: December 31
50 mg USD 150 In-stock
Estimated Time of Arrival: December 31
100 mg USD 290 In-stock
Estimated Time of Arrival: December 31
200 mg USD 450 In-stock
Estimated Time of Arrival: December 31
500 mg USD 650 In-stock
Estimated Time of Arrival: December 31
1 g   Get quote  
5 g   Get quote  

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Customer Review

Top Publications Citing Use of Products

    INT-747 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

    • Technical Information

    • Purity & Documentation

    • References

    Description

    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

    6-ECDCA increases the expression of FXR-regulated genes in rat hepatocytes[1]. INT-747 reduces expression of liver JNK-1 and JNK-2[2]. 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

    6-ECDCA (10 mg/kg/day) completely reverted cholestasis induced by E217α. Administration of 6-ECDCA 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]. INT-747 (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]. INT-747 (5 mg/kg) significantly increases survival in BDL rats. 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
    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)

    *"≥" 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    90% corn oil

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

    • 2.

      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

    • 3.

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

      Solubility: ≥ 5 mg/mL (11.89 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
    Molecular Weight

    420.63

    Formula

    C₂₆H₄₄O₄

    CAS No.

    459789-99-2

    SMILES
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: >98.0%

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    Inquiry Information

    Product Name:
    INT-747
    Cat. No.:
    HY-12222
    Quantity:

    INT-747

    Cat. No.: HY-12222