Obeticholic Acid

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

For research use only.

Obeticholic Acid (INT-747, 6-ECDCA, 6-Ethylchenodeoxycholic acid) is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. Obeticholic Acid inhibits autophagy. Phase 3.

Obeticholic Acid Chemical Structure

CAS No. 459789-99-2

Selleck's Obeticholic Acid has been cited by 13 publications

Purity & Quality Control

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Biological Activity

Description Obeticholic Acid (INT-747, 6-ECDCA, 6-Ethylchenodeoxycholic acid) 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
insect cells MU\GeY5kfGmxbjDhd5NigQ>? NV7BfHFyOSCqch?= MY\B[49vcXO2IHHjeIl3cXS7IHH0JJJm[2:vYnnuZY51KGi3bXHuJGdUXC22YXfn[YQhTliUIHzp[4Fv\CCkaX7kbY5oKGSxbXHpckApOTl|IITvJFQ4OiC{ZYPp[JVmeyliZYjwdoV{e2WmIHnuJIJi[3Wub4\pdpV{KGmwZnXjeIVlKGmwc3XjeEBk\WyuczDhd5Nme3OnZDDhd{BqdmS3Y4Tpc44hd2ZiaX70[ZJi[3Srb36ge4l1cCCkaX;0bY4hdGGkZXzs[YQhW1KFLUGgZYZ1\XJiMTDodkBjgSCKVGLGJIF{e2G7LDDFR|UxKD1iMD6wNUDPxE1w NGm4eWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUG0PFgxPid-MkmxOFg5ODZ:L3G+
HEK293T MVTGeY5kfGmxbjDhd5NigQ>? Mo\mNlQhcHK| NUTsNHVMSWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBHYFJiZYjwdoV{e2WmIHnuJGhGUzJ7M2SgZ4VtdHNiYYPz[ZN{\WRiYYOgRnNGWCCycn;tc5RmeiCmcnn2[Y4h[2WubIXsZZIhfHKjboPjdolxfGmxbnHsJIFkfGm4aYT5JIFnfGW{IEK0JIhzeyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEWFNUCgQUAxNjB2MjFOwG0v MoPkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzNEi4NFYoRjJ7MUS4PFA3RC:jPh?=
COS1 NInhUVlHfW6ldHnvckBie3OjeR?= NYHrO5RESWexbnnzeEBi[3Srdnn0fUBifCCIWGKg[ZhxemW|c3XkJIlvKEORU{GgZ4VtdHNiYomgZ4VtdC2kYYPl[EBjcW:udX3pcoV{[2WwY3WgZZN{[XluIFXDOVAhRSByLkC5PUDPxE1w NED1dIw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MECxOFg4OCd-MkCwNVQ5PzB:L3G+
HeLa NH3QXVFHfW6ldHnvckBie3OjeR?= MkLQNlQhcHK| NWSwWIxJSWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBnfWyuIHzlcod1cCCIWGKg[ZhxemW|c3XkJIlvKEinTHGgZ4VtdHNiY3;0doFve2[nY4Tl[EB4cXSqIIDTS|UucHWvYX6gVnhTKGGodHXyJFI1KGi{czDifUBFfWGuLVfsc{BtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFXDOVAhRSByLkG2JO69VS5? MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl|NEKyO{c,OjV7M{SyNlc9N2F-
HeLa MkP3SpVv[3Srb36gZZN{[Xl? MlzLRYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDGXHIh\XiycnXzd4VlKGmwIHj1cYFvKEinTHGgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVk\XC2b4KgZYN1cX[jdHnvckBjgSCEU1XQJJBzd22xdHXyMYRzcX[nbjDmbZJm\my7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhTUN3MDC9JFAvOTZizszNMi=> M13HdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkW1NFM6Lz5{NUK1OVA{QTxxYU6=
insect cells M3T5VmZ2dmO2aX;uJIF{e2G7 MWmxJIhz Mne2RYdwdmm|dDDhZ5Rqfmm2eTDheEBz\WOxbXLpcoFvfCCqdX3hckBIW1RvdHHn[4VlKE[[UjDMRmQhMDF7MzD0c{A1PzJicnXzbYR2\XNrIHX4dJJme3OnZDDpckBj[WO3bH;2bZJ2ey2rbn\lZ5Rm\CCrboPlZ5Qh[2WubIOgZZN{\XO|ZXSgZZMhemWlcoXpeI1mdnRib3[gZolwfGmweXzheIVlKFOUQ{GgdIVxfGmmZTDt[YF{fXKnZDDh[pRmeiBzIHjyJIJ6KEGucHjhd4Nz\WWwIHHzd4F6NCCHQ{WwJF0hOC5zODFOwG0v NILvelI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUK1PVc1Oid-MkmyOVk4PDJ:L3G+
COS1 NEPxPVNHfW6ldHnvckBie3OjeR?= MWG1JIhzew>? MmTsRYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDGXHIh\XiycnXzd4VlKGmwIFPPV|Eh[2WubIOgZYZ1\XJiNTDodpMh[nliQ2LFMYRzcX[nbjDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEWFNUCgQUAxNjN4MTFOwG0v NXywV5ZFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe2PFU3ODNpPkG3Olg2PjB|PD;hQi=>
CHO MU\GeY5kfGmxbjDhd5NigQ>? M2\oOFUhcHK| M2D0cmFod26rc4SgZYN1cX[rdImgZZQhcHWvYX6gWGdTPSCneIDy[ZN{\WRiaX6gR2hQKGOnbHzzJIFnfGW{IEWgbJJ{KGK7IFPSSU1lemm4ZX6gcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{WwJF0hOC55NUWg{txONg>? MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzZ6NU[wN{c,OTd4OEW2NFM9N2F-
HEK293 NUjO[GQxTnWwY4Tpc44h[XO|YYm= M3\ZZ|EhcHJ? MYjB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIGTHVlUh\XiycnXzd4VlKGmwIFjFT|I6OyClZXzsd{Bie3Onc4Pl[EBieyCrbnPy[YF{\SCrbjDpcpRz[WOnbHz1cIFzKGODTWCgcIV3\WxiYX\0[ZIhOSCqcjDifUBVWi2IUlXUJIF{e2G7LDDFR|UxKD1iMD64OEDPxE1w MkH4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{NUm3OFIoRjJ7MkW5O|QzRC:jPh?=
NCI-H716 MUjGeY5kfGmxbjDhd5NigQ>? MX7B[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIGTHVlUhemWlZYD0c5Ih\XiycnXzd4VlKGmwIF7DTU1JPzF4IHPlcIx{KGG|c3Xzd4VlKGG|IHnueJJi[2WubIXsZZIh[0GPUDDs[ZZmdCCkeTDUVk1HWkWWIHHzd4F6NCCHQ{WwJF0hOjBizszNMi=> NWSzPXhKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG0OVk2QDBpPkKxOFU6PThyPD;hQi=>
HepG2 NGrUe4xHfW6ldHnvckBie3OjeR?= M1fsTlIxKHWP NXT3fIdpUW6mdXP0bY9vKG:oIF\YVk1u\WSrYYTl[EBUUFBibWLORUBmgHC{ZYPzbY9vKGmwIHj1cYFvKEincFeyJINmdGy|IHH0JFIxKHWPIHL5JHJVNVCFUh?= M4C4SFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNEW5OVgxLz5{MUS1PVU5ODxxYU6=
HepG2 MnnCSpVv[3Srb36gZZN{[Xl? MVmxJJVO NFLnVoRKdmS3Y4Tpc44hd2ZiRmjSMY1m\GmjdHXkJHNJWCCvUl7BJIV5eHKnc4Ppc44hcW5iaIXtZY4hUGWyR{KgZ4VtdHNiYYSgNUB2VSCkeTDSWE1RS1J? MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTR3OUW4NEc,OjF2NUm1PFA9N2F-
HepG2 MWHGeY5kfGmxbjDhd5NigQ>? M3rkT|IxKHWP MUnJcoR2[3Srb36gc4YhTliULX3l[IlifGWmIFLTSXAhdVKQQTDlfJBz\XO|aX;uJIlvKGi3bXHuJGhmeEd{IHPlcIx{KGG2IEKwJJVOKGK7IGLUMXBEWg>? M2\ubVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNEW5OVgxLz5{MUS1PVU5ODxxYU6=
HepG2 NUfUZmVjTnWwY4Tpc44h[XO|YYm= M1HMPVIxKHWP MUnJcoR2[3Srb36gc4YhTliULX3l[IlifGWmIF;zeIJmfGFibWLORUBmgHC{ZYPzbY9vKGmwIHj1cYFvKEincFeyJINmdGy|IHH0JFIxKHWPIHL5JHJVNVCFUh?= MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTR3OUW4NEc,OjF2NUm1PFA9N2F-
HepG2 NUXZ[XBmTnWwY4Tpc44h[XO|YYm= Ml:yNUB2VQ>? MWTJcoR2[3Srb36gc4YhTliULX3l[IlifGWmIHTve44uemWpdXzheIlwdiCxZjDDfZA4STFibWLORUBmgHC{ZYPzbY9vKGmwIHj1cYFvKEincFeyJINmdGy|IHH0JFEhfU1iYomgVnQuWEOU NYXFO2ozRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG0OVk2QDBpPkKxOFU6PThyPD;hQi=>
HepG2 Ml;TSpVv[3Srb36gZZN{[Xl? NXTld5l5OjBidV2= M1O3XWlv\HWldHnvckBw\iCIWGKtcYVlcWG2ZXSg[I94di2{ZXf1cIF1cW:wIH;mJGN6eDeDMTDtVm5CKGW6cILld5Nqd25iaX6gbJVu[W5iSHXwS|Ih[2WubIOgZZQhOjBidV2gZpkhWlRvUFPS MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTR3OUW4NEc,OjF2NUm1PFA9N2F-
HepG2 NWnLXFQ{TnWwY4Tpc44h[XO|YYm= NUfGVnZZOjBidV2= MVfB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIF\YVkBmgHC{ZYPz[YQhcW5iSHXwS|Ih[2WubIOgZZN{\XO|ZXSgZZMhemWwaXzsZUBtfWOrZnXyZZNmKGGldHn2bZR6KGG2IEKwJJVOKGK7IHz1Z4ln\XKjc3WgZoF{\WRidILhcpNi[3SrdnH0bY9vKGG|c3H5 NHPwZVM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUS1PVU5OCd-MkG0OVk2QDB:L3G+
HepG2 NIXNdZBHfW6ldHnvckBie3OjeR?= MlzVNUB2VQ>? NFXtOWJKdmS3Y4Tpc44hd2ZiRmjSMY1m\GmjdHXkJGJUTVBibWLORUBmgHC{ZYPzbY9vKGmwIHj1cYFvKEincFeyJINmdGy|IHH0JFEhfU1iYomgVnQuWEOU NXL4SnRlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG0OVk2QDBpPkKxOFU6PThyPD;hQi=>
HepG2 MmfWSpVv[3Srb36gZZN{[Xl? NILGSW0yKHWP NIntXHpKdmS3Y4Tpc44hd2ZiRmjSMY1m\GmjdHXkJG9{fGKndHGgcXJPSSCneIDy[ZN{cW:wIHnuJIh2dWGwIFjldGczKGOnbHzzJIF1KDFidV2gZpkhWlRvUFPS MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTR3OUW4NEc,OjF2NUm1PFA9N2F-
HepG2 MVPGeY5kfGmxbjDhd5NigQ>? NYnrdGpkOTBidV2= MnjqWJJidnOjY4TpeoF1cW:wIH;mJIh2dWGwIF\YVkB1emGwc3\lZ5Rm\CCrbjDoeY1idiCKZYDHNkBk\WyuczDheEAyOCC3TTDifUBj\XSjLXfhcIFkfG:|aXThd4UhemWyb4L0[ZIh\2WwZTDhd5NigQ>? NHyybI09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO4O|MzPSd-MkSzPFc{OjV:L3G+
HepG2 NF;6e|hHfW6ldHnvckBie3OjeR?= MU[xNEB2VQ>? M1HYU|E5KGi{cx?= MVXB[49vcXO2IHHjeIl3cXS7IHH0JGZZWiCrbjDoeY1idiCKZYDHNkBk\WyuczDhd5Nme3OnZDDhd{B2eHKnZ4XsZZRqd25ib3[gU3NVNWGucHjhJI1TVkFiZYjwdoV{e2mxbjDheEAyOCC3TTDh[pRmeiBzODDodpMh[nliUmStVGNTKGGwYXz5d4l{ MlXqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|OEezNlUoRjJ2M{i3N|I2RC:jPh?=
GLUTag MYHGeY5kfGmxbjDhd5NigQ>? NFTqT|JC\2:waYP0JIFkfGm4aYT5JIF1KEeSLVLBVlEhcW5ibX;1d4UhT0yXVHHnJINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKGmwdILhZ4VtdHWuYYKgZ2FOWCCuZY\lcC=> MonNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|OEezNlUoRjJ2M{i3N|I2RC:jPh?=
HepG2 MnXjSpVv[3Srb36gZZN{[Xl? NYrSbo97OTBidV2= M1zWfFE5KGi{cx?= Mnr5RYdwdmm|dDDhZ5Rqfmm2eTDheEBHYFJiaX6gbJVu[W5iSHXwS|Ih[2WubIOgZZN{\XO|ZXSgZZMhfXC{ZXf1cIF1cW:wIH;mJHNJWCCvUl7BJIV5eHKnc4Ppc44h[XRiMUCgeW0h[W[2ZYKgNVghcHK|IHL5JHJVNVCFUjDhcoFtgXOrcx?= Mnv6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|OEezNlUoRjJ2M{i3N|I2RC:jPh?=
HepG2 NVv1cWIzTnWwY4Tpc44h[XO|YYm= MYixNEB2VQ>? NXnGc|FtOThiaILz MkixRYdwdmm|dDDhZ5Rqfmm2eTDheEBHYFJiaX6gbJVu[W5iSHXwS|Ih[2WubIOgZZN{\XO|ZXSgZZMhfXC{ZXf1cIF1cW:wIH;mJGJGW1BibWLORUBmgHC{ZYPzbY9vKGG2IEGwJJVOKGGodHXyJFE5KGi{czDifUBTXC2SQ2KgZY5idHm|aYO= NWLSW5B6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzPFc{OjVpPkK0N|g4OzJ3PD;hQi=>
GLUTag Mm\vSpVv[3Srb36gZZN{[Xl? NV\UdG9rSWexbnnzeEBi[3Srdnn0fUBifCCJUD3CRXIyKGmwIH3veZNmKEeOVWTh[{Bk\WyuczDhd5Nme3OnZDDhd{BqdmO{ZXHz[UBqdiCJTGCtNUBz\WynYYPl MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN6N{OyOUc,OjR|OEezNlU9N2F-
Assay
Methods Test Index PMID
Western blot XBP1s ; p-IRE1α 29377207
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)

Animal Research:

[1]

  • Animal Models: Rat cholestasis model
  • Dosages: Saline
  • Administration: Infused at the right jugular vein using PE-50 polyethylene tubing

Solubility (25°C)

In vitro

DMSO 84 mg/mL
(199.7 mM)
Water Insoluble
Ethanol ''84 mg/mL warmed

Chemical Information

Molecular Weight 420.63
Formula

C26H44O4

CAS No. 459789-99-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCC1C2CC(CCC2(C3CCC4(C(C3C1O)CCC4C(C)CCC(=O)O)C)C)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02633956 Completed Drug: Obeticholic Acid|Drug: Atorvastatin|Drug: Placebo Nonalcoholic Steatohepatitis Intercept Pharmaceuticals December 4 2015 Phase 2
NCT02548351 Active not recruiting Drug: Obeticholic Acid|Drug: Placebo Non Alcoholic Steatohepatitis (NASH) Intercept Pharmaceuticals September 22 2015 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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.

Handling Instructions

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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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