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FXR Products

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  • FXR Agonists (13)
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  • New FXR Products
Catalog No. Product Name Information Product Use Citations Product Validations
S2449 Forskolin (Colforsin) 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.
Circulation, 2024, 149(18):1435-1456
Cell Stem Cell, 2024, S1934-5909(24)00048-1
iScience, 2024, 27(2):108857
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.
Gut Microbes, 2024, 16(1):2379566
Mol Metab, 2024, 79:101841
Chin Med, 2024, 19(1):16
S7076 T0901317 T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of 20nM for LXRα and 5 μM for FXR, 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.
Front Immunol, 2022, 13:848367
J Anim Sci Biotechnol, 2022, 13(1):120
Commun Biol, 2022, 5(1):132
S7660 Obeticholic Acid (INT-747) Obeticholic Acid (INT-747) is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. Obeticholic Acid inhibits autophagy. Phase 3.
iScience, 2024, 27(3):109118
Phytomedicine, 2023, 119:155005
Nat Commun, 2022, 13(1):3419
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.
FEBS Open Bio, 2023, 13(9):1789-1806
FEBS Open Bio, 2023, 13(9):1789-1806
Biomed Pharmacother, 2022, 149:112825
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.
Gut Microbes, 2024, 16(1):2379566
Nat Commun, 2023, 14(1):6908
Nat Commun, 2023, 14(1):6908
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
Oncotarget, 2015, 6(6):4226-38
Placenta, 2015, 36(5):545-51
S1843 Chenodeoxycholic Acid 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. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
World J Gastroenterol, 2024, 30(5):485-498
Food Funct, 2021, 10.1039/d1fo01272j
Am J Transl Res, 2016, 8(11):5118-5124
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.
S0033 BAR502 BAR502 (Compound 30) is a dual FXR and GPBAR1 agonist with IC50 values of 2 μM and 0.4 μM, respectively.
S0037 Nidufexor (LMB-763) Nidufexor (LMB763) is an agonist of farnesoid X receptor (FXR).
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).
E4873New Mebhydroline Mebhydroline acts as a selective antagonist of farnesoid X receptor (FXR). Mebhydrolin improves blood glucose balance in in vivo mice models by inhibiting hepatic gluconeogenesis through the FXR/miR-22-3p/PI3K/AKT/FoxO1 pathway and enhancing glycogen synthesis. It also acts as a specific antagonist of histamine H1 receptor. It has potential for its use in the treatment of Type 2 diabetes mellitus (T2DM).
S0874 Vonafexor (EYP001) Vonafexor (EYP001, PLX007) is a novel non-bile acid, selective, second generation farnesoid X receptor (FXR) agonist.
S6547New Cilofexor (GS-9674) Cilofexor(GS-9674) is a potent, selective oral agonist of farnesoid X receptor (FXR) with an EC50 of 43 nM. It has demonstrated anti-inflammatory, antifibrotic effects, and reduced portal pressure in preclinical liver fibrosis models, showing potential therapeutic benefit for primary sclerosing cholangitis (PSC) and nonalcoholic steatohepatitis (NASH) research.
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.
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.
S4129 Sevelamer HCl Sevelamer HCl is a phosphate binding drug used to treat hyperphosphatemia via binding to dietary phosphate and prevents its absorption.
S2449 Forskolin (Colforsin) 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.
Circulation, 2024, 149(18):1435-1456
Cell Stem Cell, 2024, S1934-5909(24)00048-1
iScience, 2024, 27(2):108857
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.
Gut Microbes, 2024, 16(1):2379566
Nat Commun, 2023, 14(1):6908
Nat Commun, 2023, 14(1):6908
E4873New Mebhydroline Mebhydroline acts as a selective antagonist of farnesoid X receptor (FXR). Mebhydrolin improves blood glucose balance in in vivo mice models by inhibiting hepatic gluconeogenesis through the FXR/miR-22-3p/PI3K/AKT/FoxO1 pathway and enhancing glycogen synthesis. It also acts as a specific antagonist of histamine H1 receptor. It has potential for its use in the treatment of Type 2 diabetes mellitus (T2DM).
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.
Gut Microbes, 2024, 16(1):2379566
Mol Metab, 2024, 79:101841
Chin Med, 2024, 19(1):16
S7076 T0901317 T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of 20nM for LXRα and 5 μM for FXR, 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.
Front Immunol, 2022, 13:848367
J Anim Sci Biotechnol, 2022, 13(1):120
Commun Biol, 2022, 5(1):132
S7660 Obeticholic Acid (INT-747) Obeticholic Acid (INT-747) is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. Obeticholic Acid inhibits autophagy. Phase 3.
iScience, 2024, 27(3):109118
Phytomedicine, 2023, 119:155005
Nat Commun, 2022, 13(1):3419
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.
FEBS Open Bio, 2023, 13(9):1789-1806
FEBS Open Bio, 2023, 13(9):1789-1806
Biomed Pharmacother, 2022, 149:112825
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
Oncotarget, 2015, 6(6):4226-38
Placenta, 2015, 36(5):545-51
S1843 Chenodeoxycholic Acid 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. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
World J Gastroenterol, 2024, 30(5):485-498
Food Funct, 2021, 10.1039/d1fo01272j
Am J Transl Res, 2016, 8(11):5118-5124
S0033 BAR502 BAR502 (Compound 30) is a dual FXR and GPBAR1 agonist with IC50 values of 2 μM and 0.4 μM, respectively.
S0037 Nidufexor (LMB-763) Nidufexor (LMB763) is an agonist of farnesoid X receptor (FXR).
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).
S0874 Vonafexor (EYP001) Vonafexor (EYP001, PLX007) is a novel non-bile acid, selective, second generation farnesoid X receptor (FXR) agonist.
S6547New Cilofexor (GS-9674) Cilofexor(GS-9674) is a potent, selective oral agonist of farnesoid X receptor (FXR) with an EC50 of 43 nM. It has demonstrated anti-inflammatory, antifibrotic effects, and reduced portal pressure in preclinical liver fibrosis models, showing potential therapeutic benefit for primary sclerosing cholangitis (PSC) and nonalcoholic steatohepatitis (NASH) research.
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.
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.
S1643 Ursodiol Ursodiol (Ursodeoxycholic acid, UDCA) reduces cholesterol absorption and is used to dissolve (cholesterol) gallstones. (IC50=0.22 μM)
E4873New Mebhydroline Mebhydroline acts as a selective antagonist of farnesoid X receptor (FXR). Mebhydrolin improves blood glucose balance in in vivo mice models by inhibiting hepatic gluconeogenesis through the FXR/miR-22-3p/PI3K/AKT/FoxO1 pathway and enhancing glycogen synthesis. It also acts as a specific antagonist of histamine H1 receptor. It has potential for its use in the treatment of Type 2 diabetes mellitus (T2DM).
S6547New Cilofexor (GS-9674) Cilofexor(GS-9674) is a potent, selective oral agonist of farnesoid X receptor (FXR) with an EC50 of 43 nM. It has demonstrated anti-inflammatory, antifibrotic effects, and reduced portal pressure in preclinical liver fibrosis models, showing potential therapeutic benefit for primary sclerosing cholangitis (PSC) and nonalcoholic steatohepatitis (NASH) research.

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Tags: FXR inhibitor|FXR agonist|FXR activator|FXR inducer|FXR antagonist|FXR signaling pathway|FXR assay kit