FXR

FXR製品

• All (34)
• FXR阻害剤 (2)
• FXR活性剤(1)
• FXR拮抗剤(2)
• FXR作動薬(14)
• FXRモジュレータ(1)
• 新製品

製品コード	製品名称	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S2449	Forskolin (Colforsin)	コルホルチン (Forskolin (Colforsin)) は、広範な細胞腫における真核生物のアデニル酸シクラーゼ (adenylate cyclase, AC) の遍在する活性化因子であり、細胞生理学の研究において cAMP のレベルを上げるために一般的に使用されています。ホルスコリン (Forskolin) は、PXR と FXR も活性化します。 ホルスコリンはオートファジー (autophagy) を刺激します。	Cell Host Microbe, 2025, 33(3):408-419.e8 Gut, 2025, gutjnl-2025-336105 Cell Stem Cell, 2025, S1934-5909(25)00265-6
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.	Life Metab, 2025, 4(2):loaf004 Gut Microbes, 2024, 16(1):2379566 Mol Metab, 2024, 79:101841
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.	J Clin Invest, 2025, 135(10)e186478 J Exp Med, 2025, 222(3)e20230647 Neurobiol Dis, 2025, 215:107094
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.	Nat Commun, 2025, 16(1):2093 Cell Commun Signal, 2025, 23(1):236 Am J Physiol Gastrointest Liver Physiol, 2025, 328(5):G558-G577
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.	Acta Pharm Sin B, 2024, 14(8):3513-3527 World J Gastroenterol, 2024, 30(5):485-498 Food Funct, 2021, 10.1039/d1fo01272j
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).
E4873	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.
S6547	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.
E5874New	INT-767	INT-767 is a dual agonist of farnesoid X receptor (FXR)/TGR5 with an EC50 of 0.033 μM and 0.67 μM, respectively. It significantly improves serum liver enzymes, hepatic inflammation, and biliary fibrosis, while inducing bile flow and biliary HCO₃⁻ output, making it a promising tool for chronic cholangiopathy 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.	Mol Med, 2025, 31(1):258
E4617New	Gly-β-MCA	胆汁酸であるGly - β - MCAは、強力で安定的な、腸選択的かつ経口で生物学的活性を有するファルネソイドX受容体（FXR）阻害剤であり、代謝障害の治療薬の候補となり得る。
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.	Life Metab, 2025, 4(2):loaf004 Gut Microbes, 2024, 16(1):2379566 Mol Metab, 2024, 79:101841
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.	J Clin Invest, 2025, 135(10)e186478 J Exp Med, 2025, 222(3)e20230647 Neurobiol Dis, 2025, 215:107094
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.	Nat Commun, 2025, 16(1):2093 Cell Commun Signal, 2025, 23(1):236 Am J Physiol Gastrointest Liver Physiol, 2025, 328(5):G558-G577
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.	Acta Pharm Sin B, 2024, 14(8):3513-3527 World J Gastroenterol, 2024, 30(5):485-498 Food Funct, 2021, 10.1039/d1fo01272j
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.
S6547	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.
E5874New	INT-767	INT-767 is a dual agonist of farnesoid X receptor (FXR)/TGR5 with an EC50 of 0.033 μM and 0.67 μM, respectively. It significantly improves serum liver enzymes, hepatic inflammation, and biliary fibrosis, while inducing bile flow and biliary HCO₃⁻ output, making it a promising tool for chronic cholangiopathy 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.	Mol Med, 2025, 31(1):258
S4129	Sevelamer HCl	Sevelamer HCl is a phosphate binding drug used to treat hyperphosphatemia via binding to dietary phosphate and prevents its absorption.
E4617New	Gly-β-MCA	胆汁酸であるGly - β - MCAは、強力で安定的な、腸選択的かつ経口で生物学的活性を有するファルネソイドX受容体（FXR）阻害剤であり、代謝障害の治療薬の候補となり得る。
S2449	Forskolin (Colforsin)	コルホルチン (Forskolin (Colforsin)) は、広範な細胞腫における真核生物のアデニル酸シクラーゼ (adenylate cyclase, AC) の遍在する活性化因子であり、細胞生理学の研究において cAMP のレベルを上げるために一般的に使用されています。ホルスコリン (Forskolin) は、PXR と FXR も活性化します。 ホルスコリンはオートファジー (autophagy) を刺激します。	Cell Host Microbe, 2025, 33(3):408-419.e8 Gut, 2025, gutjnl-2025-336105 Cell Stem Cell, 2025, S1934-5909(25)00265-6
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
E4873	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.	Life Metab, 2025, 4(2):loaf004 Gut Microbes, 2024, 16(1):2379566 Mol Metab, 2024, 79:101841
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.	J Clin Invest, 2025, 135(10)e186478 J Exp Med, 2025, 222(3)e20230647 Neurobiol Dis, 2025, 215:107094
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.	Nat Commun, 2025, 16(1):2093 Cell Commun Signal, 2025, 23(1):236 Am J Physiol Gastrointest Liver Physiol, 2025, 328(5):G558-G577
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.	Acta Pharm Sin B, 2024, 14(8):3513-3527 World J Gastroenterol, 2024, 30(5):485-498 Food Funct, 2021, 10.1039/d1fo01272j
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.
S6547	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.
E5874New	INT-767	INT-767 is a dual agonist of farnesoid X receptor (FXR)/TGR5 with an EC50 of 0.033 μM and 0.67 μM, respectively. It significantly improves serum liver enzymes, hepatic inflammation, and biliary fibrosis, while inducing bile flow and biliary HCO₃⁻ output, making it a promising tool for chronic cholangiopathy 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.	Mol Med, 2025, 31(1):258
S1643	Ursodiol	Ursodiol (Ursodeoxycholic acid, UDCA) reduces cholesterol absorption and is used to dissolve (cholesterol) gallstones. (IC50=0.22 μM)
E5874New	INT-767	INT-767 is a dual agonist of farnesoid X receptor (FXR)/TGR5 with an EC50 of 0.033 μM and 0.67 μM, respectively. It significantly improves serum liver enzymes, hepatic inflammation, and biliary fibrosis, while inducing bile flow and biliary HCO₃⁻ output, making it a promising tool for chronic cholangiopathy research.
E4617New	Gly-β-MCA	胆汁酸であるGly - β - MCAは、強力で安定的な、腸選択的かつ経口で生物学的活性を有するファルネソイドX受容体（FXR）阻害剤であり、代謝障害の治療薬の候補となり得る。
E5874New	INT-767	INT-767 is a dual agonist of farnesoid X receptor (FXR)/TGR5 with an EC50 of 0.033 μM and 0.67 μM, respectively. It significantly improves serum liver enzymes, hepatic inflammation, and biliary fibrosis, while inducing bile flow and biliary HCO₃⁻ output, making it a promising tool for chronic cholangiopathy research.