FXR

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FXR Products

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  • 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 Product Validations
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)
Tags: FXR inhibitor|FXR agonist|FXR activator|FXR inducer|FXR antagonist|FXR signaling pathway|FXR assay kit