Obeticholic Acid (INT-747)

Synonyms: 6-ECDCA, 6-Ethylchenodeoxycholic acid

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.

Obeticholic Acid (INT-747) Chemical Structure

Obeticholic Acid (INT-747) Chemical Structure

CAS: 459789-99-2

Selleck's Obeticholic Acid (INT-747) has been cited by 17 Publications

3 Customer Reviews

Purity & Quality Control

Batch: Purity: >97%
97

Obeticholic Acid (INT-747) Related Products

Choose Selective FXR Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
insect cells Function assay 1 hr Agonist activity at recombinant human GST-tagged FXR ligand binding domain (193 to 472 residues) expressed in baculovirus infected insect cells assessed as induction of interaction with biotin labelled SRC-1 after 1 hr by HTRF assay, EC50 = 0.01 μM. 29148806
HEK293T Function assay 24 hrs Agonist activity at human FXR expressed in HEK293T cells assessed as BSEP promoter driven cellular transcriptional activity after 24 hrs by luciferase reporter gene assay, EC50 = 0.042 μM. 29148806
COS1 Function assay Agonist activity at FXR expressed in COS1 cells by cell-based bioluminescence assay, EC50 = 0.099 μM. 20014870
HeLa Function assay 24 hrs Agonist activity at human full length FXR expressed in HeLa cells cotransfected with pSG5-human RXR after 24 hrs by Dual-Glo luciferase reporter gene assay, EC50 = 0.16 μM. 25934227
HeLa Function assay Agonist activity at human FXR expressed in human HeLa cells assessed as receptor activation by BSEP promoter-driven firefly luciferase reporter gene assay, EC50 = 0.16 μM. 25255039
insect cells Function assay 1 hr Agonist activity at recombinant human GST-tagged FXR LBD (193 to 472 residues) expressed in baculovirus-infected insect cells assessed as recruitment of biotinylated SRC1 peptide measured after 1 hr by Alphascreen assay, EC50 = 0.18 μM. 29259742
COS1 Function assay 5 hrs Agonist activity at human FXR expressed in COS1 cells after 5 hrs by CRE-driven luciferase reporter gene assay, EC50 = 0.361 μM. 17685603
CHO Function assay 5 hrs Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay, EC50 = 0.755 μM. 17685603
HEK293 Function assay 1 hr Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assay, EC50 = 0.84 μM. 29259742
NCI-H716 Function assay Agonist activity at human TGR5 receptor expressed in NCI-H716 cells assessed as intracellular cAMP level by TR-FRET assay, EC50 = 20 μM. 21459580
HepG2 Function assay 20 uM Induction of FXR-mediated SHP mRNA expression in human HepG2 cells at 20 uM by RT-PCR 21459580
HepG2 Function assay 1 uM Induction of FXR-mediated SHP mRNA expression in human HepG2 cells at 1 uM by RT-PCR 21459580
HepG2 Function assay 20 uM Induction of FXR-mediated BSEP mRNA expression in human HepG2 cells at 20 uM by RT-PCR 21459580
HepG2 Function assay 20 uM Induction of FXR-mediated Ostbeta mRNA expression in human HepG2 cells at 20 uM by RT-PCR 21459580
HepG2 Function assay 1 uM Induction of FXR-mediated down-regulation of Cyp7A1 mRNA expression in human HepG2 cells at 1 uM by RT-PCR 21459580
HepG2 Function assay 20 uM Induction of FXR-mediated down-regulation of Cyp7A1 mRNA expression in human HepG2 cells at 20 uM by RT-PCR 21459580
HepG2 Function assay 20 uM Agonist activity at human FXR expressed in HepG2 cells assessed as renilla luciferase activity at 20 uM by luciferase based transactivation assay 21459580
HepG2 Function assay 1 uM Induction of FXR-mediated BSEP mRNA expression in human HepG2 cells at 1 uM by RT-PCR 21459580
HepG2 Function assay 1 uM Induction of FXR-mediated Ostbeta mRNA expression in human HepG2 cells at 1 uM by RT-PCR 21459580
HepG2 Function assay 10 uM Transactivation of human FXR transfected in human HepG2 cells at 10 uM by beta-galactosidase reporter gene assay 24387325
HepG2 Function assay 10 uM 18 hrs Agonist activity at FXR in human HepG2 cells assessed as upregulation of OST-alpha mRNA expression at 10 uM after 18 hrs by RT-PCR analysis 24387325
GLUTag Function assay Agonist activity at GP-BAR1 in mouse GLUTag cells assessed as increase in intracellular cAMP level 24387325
HepG2 Function assay 10 uM 18 hrs Agonist activity at FXR in human HepG2 cells assessed as upregulation of SHP mRNA expression at 10 uM after 18 hrs by RT-PCR analysis 24387325
HepG2 Function assay 10 uM 18 hrs Agonist activity at FXR in human HepG2 cells assessed as upregulation of BESP mRNA expression at 10 uM after 18 hrs by RT-PCR analysis 24387325
GLUTag Function assay Agonist activity at GP-BAR1 in mouse GLUTag cells assessed as increase in GLP-1 release 24387325
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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 vitro

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

Kinase Assay 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot XBP1s p-IRE1α 29377207
In Vivo
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]

Animal Research Animal Models Rat cholestasis model
Dosages Saline
Administration Infused at the right jugular vein using PE-50 polyethylene tubing
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05740631 Recruiting
Healthy
Universitaire Ziekenhuizen KU Leuven|Intercept Pharmaceuticals
August 22 2022 Not Applicable
NCT02633956 Completed
Nonalcoholic Steatohepatitis
Intercept Pharmaceuticals
December 4 2015 Phase 2
NCT02548351 Terminated
Non Alcoholic Steatohepatitis (NASH)
Intercept Pharmaceuticals
September 22 2015 Phase 3

Chemical Information & Solubility

Molecular Weight 420.63 Formula

C26H44O4

CAS No. 459789-99-2 SDF Download Obeticholic Acid (INT-747) SDF
Smiles CCC1C2CC(CCC2(C3CCC4(C(C3C1O)CCC4C(C)CCC(=O)O)C)C)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 84 mg/mL ( (199.7 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 84 mg/mL

Water : Insoluble


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

Question 1:
What formulation can we use to dissolve Obeticholic Acid (Catalog No.S7660) for mice in vivo study?

Answer:
You can use the vehicle of: 1% wt/vol methyl-cellulose as indicated in this paper, http://www.sciencedirect.com/science/article/pii/S0925443911000883 "daily oral gavage with 5 mg/kg/day INT-747 (6-ethyl-chenodeoxycholic acid, Obeticholic acid, Intercept Pharmaceuticals Inc, New York, NY) or vehicle (1% wt/vol methyl-cellulose) from 3 days prior to induction of colitis"

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