Obeticholic Acid (INT-747)

Catalog No.S7660 Batch:S766006

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Technical Data

Formula

C26H44O4
Molecular Weight 420.63 CAS No. 459789-99-2
Solubility (25°C)* In vitro DMSO 84 mg/mL (199.7 mM)
Ethanol 84 mg/mL (199.7 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Obeticholic Acid (INT-747) is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. Obeticholic Acid inhibits autophagy. Phase 3.
Targets
FXR [1]
99 nM(EC50)
In vitro

In HuH7 cells, Obeticholic Acid acts as a potent FXR agonist with EC50 of 85 nM. [1]
In vivo

In rat cholestasis model, Obeticholic Acid promotes bile flow, and protects hepatocytes against acute necrosis caused by LCA. [1]

Obeticholic Acid (p.o.) improves proteinuria, ameliorates renal structural changes, and modulates renal inflammation and oxidative stress in WD-fed DBA mice. [2]

In thioacetamide (TAA)-intoxicated and bile-duct-ligated (BDL) rats, Obeticholic Acid (30 mg/kg p.o.) reactivates the FXR downstream signaling pathway and decreases portal pressure by lowering total IHVR without deleterious systemic hypotension. [3]

Protocol (from reference)

Kinase Assay:

[1]
  • Binding Potency of Obeticholic Acid to FXR

    The compound is tested in an established cell-free ligand sensing assay, which measures the ligand-dependent recruitment of an SRC1 peptide to FXR by fluorescence resonance energy transfer.
Animal Study:

[1]
  • Animal Models

    Rat cholestasis model

  • Dosages

    Saline

  • Administration

    Infused at the right jugular vein using PE-50 polyethylene tubing

Customer Product Validation

, , Integr Biol (Camb), 2017, 9(8):662-677

Data from [Data independently produced by , , Cell Physiol Biochem, 2018, 48(1):158-172]

Data from [Data independently produced by , , Toxicol Appl Pharmacol, 2017, 315:23-34]

Selleck's Obeticholic Acid (INT-747) has been cited by 19 publications

FXR controls duodenogastric reflux-induced gastric inflammation through negatively regulating ER stress-associated TNXIP/NLPR3 inflammasome [ iScience, 2024, 27(3):109118] PubMed: 38439955
Tetrahydropalmatine ameliorates hepatic steatosis in nonalcoholic fatty liver disease by switching lipid metabolism via AMPK-SREBP-1c-Sirt1 signaling axis [ Phytomedicine, 2023, 119:155005] PubMed: 37562090
Ursodeoxycholic acid reduces antitumor immunosuppression by inducing CHIP-mediated TGF-β degradation [ Nat Commun, 2022, 13(1):3419] PubMed: 35701426
Systemic ASBT inactivation protects against liver damage in obstructive cholestasis in mice [ JHEP Rep, 2022, 4-11:100573] PubMed: 36160754
A Quantitative Systems Pharmacology Platform Reveals NAFLD Pathophysiological States and Targeting Strategies [ Metabolites, 2022, 12(6)528] PubMed: 35736460
A Quantitative Systems Pharmacology Platform Reveals NAFLD Pathophysiological States and Targeting Strategies [ Metabolites, 2022, 10.3390/metabo12060528] PubMed: 35736460
Obeticholic Acid Inhibits Anxiety via Alleviating Gut Microbiota-Mediated Microglia Accumulation in the Brain of High-Fat High-Sugar Diet Mice [ Nutrients, 2021, 13(3)940] PubMed: 33803974
Resolution of NASH and Hepatic Fibrosis by the GLP-1R/GcgR Dual-Agonist Cotadutide via Modulating Mitochondrial Function and Lipogenesis [ Nat Metab, 2020, 2(5):413-431] PubMed: 32478287
Stimulation of soluble guanylate cyclase exerts antiinflammatory actions in the liver through a VASP/NF-κB/NLRP3 inflammasome circuit [ Proc Natl Acad Sci U S A, 2020, 117(45):28263-28274] PubMed: 33106416
FXR Regulates Intestinal Cancer Stem Cell Proliferation [Fu T, et al Cell, 2019, 176(5):1098-1112] PubMed: 30794774

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.