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FXR

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FXR Products

All (15)
FXR Inhibitor (1)
FXR Activator (1)
FXR Antagonist (1)
FXR Agonists (11)
FXR Modulator (1)
New FXR Products

Catalog No.	Product Name	Information	Product Use Citations
S4129	Sevelamer HCl	Sevelamer HCl is a phosphate binding drug used to treat hyperphosphatemia via binding to dietary phosphate and prevents its absorption.
S2449	Colforsin	Colforsin (Forskolin, HL 362, Coleonol) 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.	Signal Transduct Target Ther, 2022, 7(1):46 Adv Sci (Weinh), 2022, e2105568 Nat Commun, 2022, 13(1):2256
S3792	Guggulsterone E&Z	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.	Biochim Biophys Acta Mol Cell Biol Lipids, 2019, 1864(10):1293-1304 Int J Oncol, 2019, 54(3):879-892
S0037	Nidufexor (LMB-763)	Nidufexor (LMB763) is an agonist of farnesoid X receptor (FXR).
S0403	LY2562175	LY2562175 is a potent and selective agonist of FXR. LY2562175 promotes transcriptional activation of human FXR in a cell-based cotransfection assay with EC50 of 193 nM.
S0874	Vonafexor (EYP001)	Vonafexor (EYP001, PLX007) is a novel non-bile acid, selective, second generation farnesoid X receptor (FXR) agonist.
S1843	Chenodeoxycholic Acid	Chenodeoxycholic Acid (Chenodiol) is a naturally occurring human bile acid, and inhibits production of cholesterol in the liver and absorption in the intestines. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.	Food Funct, 2021, 10.1039/d1fo01272j Am J Transl Res, 2016, 8(11):5118-5124
S2694	Turofexorate Isopropyl (XL335)	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.	Cell Cycle, 2019, 18(15):1784-1797 Placenta, 2015, 36(5):545-51 Oncotarget, 2015, 6(6):4226-38
S2782	GW4064	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. GW4064 stimulates autophagy in MCF-7 cells.	Sci Immunol, 2022, 7(69):eabj1080 Cell Chem Biol, 2021, S2451-9456(21)00213-0 Theranostics, 2020, 10(23):10434-10447
S4003	Lithocholic acid	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.	Biomed Pharmacother, 2022, 149:112825 Hum Mol Genet, 2020, ddaa244 Int J Stem Cells, 2020, 10.15283/ijsc20152
S6413	fexaramine	Fexaramine is a potent, selective farnesoid X receptor (FXR) agonist with an EC50 of 25 nM and it displays no activity at hRXRα, hPPARα, hPPARγ, hPPARδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ and hVDR receptors.
S7076	T0901317	T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of ~50 nM and 5 μM, respectively. T0901317 is a dual inverse agonist of RORα and RORγ with Ki of 132 nM and 51 nM, respectively. T0901317 significantly suppresses cell proliferation and induces apoptosis.	Commun Biol, 2022, 5(1):132 Front Cardiovasc Med, 2021, 8:746989 Hepatology, 2020, 10.1002/hep.31594
S7660	Obeticholic Acid	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.	Nutrients, 2021, 13(3)940 Proc Natl Acad Sci U S A, 2020, 117(45):28263-28274 Nat Metab, 2020, 2(5):413-431
S8733	Tropifexor (LJN452)	Tropifexor (LJN452) is a novel and highly potent agonist of FXR with EC50 of 0.2 nM in HTRF assay. It shows no significant off-target activity against a broad panel of enzyme, ion channel, nuclear receptor, and GPCR (>10000-fold selectivity for FXR).
S1643	Ursodiol	Ursodiol (Ursodeoxycholic acid, UDCA) reduces cholesterol absorption and is used to dissolve (cholesterol) gallstones. (IC50=0.22 μM)
S4129	Sevelamer HCl	Sevelamer HCl is a phosphate binding drug used to treat hyperphosphatemia via binding to dietary phosphate and prevents its absorption.
S2449	Colforsin	Colforsin (Forskolin, HL 362, Coleonol) 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.	Signal Transduct Target Ther, 2022, 7(1):46 Adv Sci (Weinh), 2022, e2105568 Nat Commun, 2022, 13(1):2256
S3792	Guggulsterone E&Z	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.	Biochim Biophys Acta Mol Cell Biol Lipids, 2019, 1864(10):1293-1304 Int J Oncol, 2019, 54(3):879-892
S0037	Nidufexor (LMB-763)	Nidufexor (LMB763) is an agonist of farnesoid X receptor (FXR).
S0403	LY2562175	LY2562175 is a potent and selective agonist of FXR. LY2562175 promotes transcriptional activation of human FXR in a cell-based cotransfection assay with EC50 of 193 nM.
S0874	Vonafexor (EYP001)	Vonafexor (EYP001, PLX007) is a novel non-bile acid, selective, second generation farnesoid X receptor (FXR) agonist.
S1843	Chenodeoxycholic Acid	Chenodeoxycholic Acid (Chenodiol) is a naturally occurring human bile acid, and inhibits production of cholesterol in the liver and absorption in the intestines. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.	Food Funct, 2021, 10.1039/d1fo01272j Am J Transl Res, 2016, 8(11):5118-5124
S2694	Turofexorate Isopropyl (XL335)	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.	Cell Cycle, 2019, 18(15):1784-1797 Placenta, 2015, 36(5):545-51 Oncotarget, 2015, 6(6):4226-38
S2782	GW4064	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. GW4064 stimulates autophagy in MCF-7 cells.	Sci Immunol, 2022, 7(69):eabj1080 Cell Chem Biol, 2021, S2451-9456(21)00213-0 Theranostics, 2020, 10(23):10434-10447
S4003	Lithocholic acid	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.	Biomed Pharmacother, 2022, 149:112825 Hum Mol Genet, 2020, ddaa244 Int J Stem Cells, 2020, 10.15283/ijsc20152
S6413	fexaramine	Fexaramine is a potent, selective farnesoid X receptor (FXR) agonist with an EC50 of 25 nM and it displays no activity at hRXRα, hPPARα, hPPARγ, hPPARδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ and hVDR receptors.
S7076	T0901317	T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of ~50 nM and 5 μM, respectively. T0901317 is a dual inverse agonist of RORα and RORγ with Ki of 132 nM and 51 nM, respectively. T0901317 significantly suppresses cell proliferation and induces apoptosis.	Commun Biol, 2022, 5(1):132 Front Cardiovasc Med, 2021, 8:746989 Hepatology, 2020, 10.1002/hep.31594
S7660	Obeticholic Acid	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.	Nutrients, 2021, 13(3)940 Proc Natl Acad Sci U S A, 2020, 117(45):28263-28274 Nat Metab, 2020, 2(5):413-431
S8733	Tropifexor (LJN452)	Tropifexor (LJN452) is a novel and highly potent agonist of FXR with EC50 of 0.2 nM in HTRF assay. It shows no significant off-target activity against a broad panel of enzyme, ion channel, nuclear receptor, and GPCR (>10000-fold selectivity for FXR).
S1643	Ursodiol	Ursodiol (Ursodeoxycholic acid, UDCA) reduces cholesterol absorption and is used to dissolve (cholesterol) gallstones. (IC50=0.22 μM)