Obeticholic Acid

Catalog No.S7660 Synonyms: INT-747, 6-ECDCA

Obeticholic Acid Chemical Structure

Molecular Weight(MW): 420.63

Obeticholic Acid is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. Phase 3.

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  • (D) Expression of hepatic FXR target genes, n = 3. Data are expressed as mean ± SD, ###P < 0.001 versus group 1, *P < 0.05, **P < 0.01, and ***P b 0.001 versus group 2, sP < 0.05, ssP < 0.01, and sssP < 0.001 versus group 3

    Toxicol Appl Pharmacol, 2017, 315:23-34. Obeticholic Acid purchased from Selleck.

    (c) Functional bile canaliculi or lack thereof in PHHs within MPTCs (12 d of drug treatment) as visualized by transport of fluorescent (green) dye into the canaliculi between PHHs. DMSO-treated MPCC control image is shown to the far right. (d) Neutral lipid (Nile red, green) staining of PHHs within MPTCs (12 d of drug treatment). DMSO-treated MPCC control image is shown to the far right. (e) NR1I2 (PXR) gene expression in drug-treated MPTCs relative to DMSOtreated MPTC controls (12 d of treatment). (f) ABCC2 (MRP2) gene expression in drug-treated MPTCs relative to DMSO-treated MPTC controls (12 d of treatment). (g) IL-6 levels in drug-treated MPTC supernatants (6 d of treatment). In all panels, statistical significance is displayed relative to DMSO-treated MPTCs. *p r 0.05, **p r 0.01, ***p r 0.001, and ****p r 0.0001. Scale bars on images represent 80 mm.

    Integr Biol (Camb), 2017. Obeticholic Acid purchased from Selleck.

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Biological Activity

Description Obeticholic Acid is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
COS1 cells MV;GeY5kfGmxbjDhd5NigQ>? NXew[JVHSWexbnnzeEBi[3Srdnn0fUBifCCIWGKg[ZhxemW|c3XkJIlvKEORU{GgZ4VtdHNiYomgZ4VtdC2kYYPl[EBjcW:udX3pcoV{[2WwY3WgZZN{[XluIFXDOVA:QTlibl2= M4jiUlIxODF2OEew
HeLa cells MojsSpVv[3Srb36gZZN{[Xl? NFvySmczPCCq NF7mNZVC\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJIZ2dGxibHXu[5RpKE[[UjDlfJBz\XO|ZXSgbY4hUGWOYTDj[YxteyClb4TyZY5{\mWldHXkJJdqfGhicGPHOU1pfW2jbjDSXHIh[W[2ZYKgNlQhcHK|IHL5JGR2[WxvR3zvJIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiRVO1NF0xNjF4IN88US=> M1;aO|I2QTN2MkK3
CHO cells NF;xeVJHfW6ldHnvckBie3OjeR?= MWC1JIg> MYnB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIGTHVlUh\XiycnXzd4VlKGmwIFPIU{Bk\WyuczDh[pRmeiB3IHjyd{BjgSCFUlWt[JJqfmWwIHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhTUN3ME2wMlc2PSEQvF2= NUDidotiOTd4OEW2NFM>
NCI-H716 cells MULGeY5kfGmxbjDhd5NigQ>? NW\hXJR2SWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBVT1J3IILlZ4VxfG:{IHX4dJJme3OnZDDpckBPS0lvSEexOkBk\WyuczDhd5Nme3OnZDDhd{BqdnS{YXPlcIx2dGG{IHPBUXAhdGW4ZXygZpkhXFJvRmLFWEBie3OjeTygSWM2OD1{MDFOwG0> NGjvSZozOTR3OUW4NC=>
mouse GLUTag cells NXfORoxWTnWwY4Tpc44h[XO|YYm= NUL2WGpVSWexbnnzeEBi[3Srdnn0fUBifCCJUD3CRXIyKGmwIH3veZNmKEeOVWTh[{Bk\WyuczDhd5Nme3OnZDDhd{BqdmO{ZXHz[UBqdiCrboTyZYNmdGy3bHHyJINCVVBibHX2[Yw> MXqyOFM5PzN{NR?=
human HepG2 cells MVnGeY5kfGmxbjDhd5NigQ>? M13ZS|ExKM7:TR?= MkK2NVghcA>? MYfB[49vcXO2IHHjeIl3cXS7IHH0JGZZWiCrbjDoeY1idiCKZYDHNkBk\WyuczDhd5Nme3OnZDDhd{B2eHKnZ4XsZZRqd25ib3[gV2hRKG2UTlGg[ZhxemW|c3nvckBifCBzMDD1UUBi\nSncjCxPEBpenNiYomgVnQuWEOUIHHuZYx6e2m| MUmyOFM5PzN{NR?=
mouse primary hepatocytes MYTGeY5kfGmxbjDhd5NigQ>? NWD4fGs2SWexbnnzeEBi[3Srdnn0fUBifCCIWGKgbY4hdW:3c3WgdJJqdWG{eTDo[ZBifG:leYTld{Bie3Onc4Pl[EBieyC3cILl[5Vt[XSrb36gc4YhSkWVUDDtVm5CKGW6cILld5Nqd25? NHPte|IzPDN6N{OyOS=>

... Click to View More Cell Line Experimental Data

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

Animal Research:

[1]

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  • Animal Models: Rat cholestasis model
  • Formulation: 7 μmol/kg/min
  • Dosages: Saline
  • Administration: Infused at the right jugular vein using PE-50 polyethylene tubing
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 84 mg/mL (199.7 mM)
Ethanol 84 mg/mL warmed (199.7 mM)
Water 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.

Chemical Information

Molecular Weight 420.63
Formula

C26H44O4

CAS No. 459789-99-2
Storage powder
Synonyms INT-747, 6-ECDCA

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02430077 Recruiting Familial Partial Lipodystrophy University of Texas Southwestern Medical Center June 2016 Phase 2
NCT02654236 Recruiting Alcohol Consumption Suthat Liangpunsakul|National Institute on Alcohol Abuse and Alcoholism (NIAAA)|Intercept Pharmaceuticals|Indiana University April 2016 --
NCT02633956 Active, not recruiting Nonalcoholic Steatohepatitis Intercept Pharmaceuticals December 2015 Phase 2
NCT02548351 Recruiting Non Alcoholic Steatohepatitis (NASH) Intercept Pharmaceuticals September 2015 Phase 3
NCT02532335 Recruiting Obesity Sahlgrenska University Hospital, Sweden August 2015 Phase 1
NCT02308111 Recruiting Liver Cirrhosis, Biliary Intercept Pharmaceuticals December 2014 Phase 3

Tech Support

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID