| S2782 |
GW4064
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GW4064 is an agonist of farnesoid X receptor (FXR) with EC50 of 65 nM in CV1 cell line and displays no activity at other nuclear receptors at concentrations up to 1 μM. This compound stimulates autophagy in MCF-7 cells.
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Life Metab, 2025, 4(2):loaf004
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Gut Microbes, 2024, 16(1):2379566
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Mol Metab, 2024, 79:101841
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| S2449 |
Forskolin (Colforsin)
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Forskolin (Colforsin) is a ubiquitous activator of eukaryotic adenylyl cyclase (AC) in a wide variety of cell types, commonly used to raise levels of cAMP in the study and research of cell physiology. Forskolin also activates PXR and FXR activity. Forskolin stimulates autophagy.
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Cell Mol Gastroenterol Hepatol, 2026, 20(1):101640
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Cell Host Microbe, 2025, 33(3):408-419.e8
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Gut, 2025, gutjnl-2025-336105
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| S7660 |
Obeticholic Acid (INT-747)
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Obeticholic Acid (INT-747) is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM, and it inhibits autophagy. This compound is in Phase 3.
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Nat Commun, 2025, 16(1):2093
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Cell Commun Signal, 2025, 23(1):236
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Am J Physiol Gastrointest Liver Physiol, 2025, 328(5):G558-G577
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| S4003 |
Lithocholic acid
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Lithocholic acid is a toxic secondary bile acid, causes intrahepatic cholestasis, has tumor-promoting activity, its toxic effect can be protected after it activates the vitamin D receptor, PXR and FXR.
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FEBS Open Bio, 2023, 13(9):1789-1806
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FEBS Open Bio, 2023, 13(9):1789-1806
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Biomed Pharmacother, 2022, 149:112825
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| S3792 |
Guggulsterone E&Z
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Guggulsterone is one of the active constituent of Commiphora mukul. It occurs in two isomeric forms, namely Z-GS and E-GS. Guggulsterone act as antagonist ligands for the bile acid receptor, farnesoid X receptor, and as active ingredients responsible for the hypolipidemic activity.
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Gut Microbes, 2024, 16(1):2379566
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Nat Commun, 2023, 14(1):6908
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Nat Commun, 2023, 14(1):6908
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| S2694 |
Turofexorate Isopropyl (XL335)
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Turofexorate Isopropyl (XL335, Fxr 450) is a potent, selective FXR agonist with EC50 of 4 nM, highly selective versus other nuclear receptors, such as LXR, PPAR, ER and etc. Phase 1.
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Cell Cycle, 2019, 18(15):1784-1797
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Oncotarget, 2015, 6(6):4226-38
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Placenta, 2015, 36(5):545-51
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| S1843 |
Chenodeoxycholic Acid
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Chenodeoxycholic Acid (Chenodiol, Chenodesoxycholic acid, Chenocholic acid,CDCA) is a naturally occurring human bile acid, and inhibits production of cholesterol in the liver and absorption in the intestines. This compound is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
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Acta Pharm Sin B, 2024, 14(8):3513-3527
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World J Gastroenterol, 2024, 30(5):485-498
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Food Funct, 2021, 10.1039/d1fo01272j
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| S4129 |
Sevelamer HCl
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Sevelamer HCl is a phosphate binding drug used to treat hyperphosphatemia via binding to dietary phosphate and prevents its absorption.
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| S0033 |
BAR502
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BAR502 (Compound 30) is a dual FXR and GPBAR1 agonist with IC50 values of 2 μM and 0.4 μM, respectively.
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| S0037 |
Nidufexor (LMB-763)
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Nidufexor (LMB763) is an agonist of farnesoid X receptor (FXR).
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