For research use only. Not for therapeutic Use.
FXR antagonist 1 (compound F6) is an orally active and selective intestinal FXR antagonist (IC50=2.1 μM). FXR antagonist 1 selectively inhibits intestinal FXR signalling through antagonism of intestinal FXR and feedback activation of hepatic FXR to improve hepatic steatosis, inflammation and fibrosis in NASH (nonalcoholic steatohepatitis) models. FXR antagonist 1 can be used in NASH studies[1].
FXR antagonist 1 (0-100 µM; 24 h) shows FXR antagonistic activities in HEK293T cells[1].
FXR antagonist 1 (10 mg/kg; p.o.; single daily for 12 weeks) reduces adiposity and improves glucose sensitivity and ameliorates the progress of NASH in GAN-diet-induced NASH mice[1].
FXR antagonist 1 (10 mg/kg; p.o.; single daily for 12 weeks) inhibits intestinal FXR Signaling but indirectly activates hepatic FXR signaling in GAN-diet-induced mice[1].
FXR antagonist 1 (3, 10, 30 mg/kg; p.o.; single daily for 4 weeks) dose-dependently alleviates NASH pathologies in HFMCD-diet-induced mice[1].
| Catalog Number | I042816 |
| CAS Number | 2295804-68-9 |
| Synonyms | 2-[[(1S,3aS,5aR,5bR,9R,11aR)-9-butanoyloxy-5a,5b,8,8,11a-pentamethyl-1-propan-2-yl-1,2,3,4,5,6,7,7a,9,10,11,11b,12,13,13a,13b-hexadecahydrocyclopenta[a]chrysene-3a-carbonyl]amino]acetic acid |
| Molecular Formula | C36H59NO5 |
| Purity | ≥95% |
| InChI | InChI=1S/C36H59NO5/c1-9-10-29(40)42-27-15-16-33(6)25(32(27,4)5)14-17-35(8)26(33)12-11-24-30-23(22(2)3)13-18-36(30,20-19-34(24,35)7)31(41)37-21-28(38)39/h22-27,30H,9-21H2,1-8H3,(H,37,41)(H,38,39)/t23-,24?,25?,26?,27+,30?,33-,34+,35+,36-/m0/s1 |
| InChIKey | CLKCLHBPLVDIOB-SUZUPGMJSA-N |
| SMILES | CCCC(=O)OC1CCC2(C3CCC4C5C(CCC5(CCC4(C3(CCC2C1(C)C)C)C)C(=O)NCC(=O)O)C(C)C)C |
| Reference | [1]. Zhang C, et al. Discovery of Betulinic Acid Derivatives as Potent Intestinal Farnesoid X Receptor Antagonists to Ameliorate Nonalcoholic Steatohepatitis. J Med Chem. 2022 Sep 15. |
