FXR

FXR製品

All (28)
FXR阻害剤 (1)
FXR活性剤(1)
FXR拮抗剤(1)
FXR作動薬(12)
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
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 Stem Cell, 2024, S1934-5909(24)00048-1 iScience, 2024, 27(2):108857 Invest Ophthalmol Vis Sci, 2024, 65(3):37
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.	Mol Metab, 2024, 79:101841 Chin Med, 2024, 19(1):16 Nat Commun, 2023, 14(1):2656
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.	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.	Nat Commun, 2023, 14(1):6908 Nat Commun, 2023, 14(1):6908 Front Immunol, 2022, 13:889646
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.	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).
S0874	Vonafexor (EYP001)	Vonafexor (EYP001, PLX007) is a novel non-bile acid, selective, second generation farnesoid X receptor (FXR) agonist.
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.
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.	Mol Metab, 2024, 79:101841 Chin Med, 2024, 19(1):16 Nat Commun, 2023, 14(1):2656
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.	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.	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.
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)	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 Stem Cell, 2024, S1934-5909(24)00048-1 iScience, 2024, 27(2):108857 Invest Ophthalmol Vis Sci, 2024, 65(3):37
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.	Nat Commun, 2023, 14(1):6908 Nat Commun, 2023, 14(1):6908 Front Immunol, 2022, 13:889646
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.	Mol Metab, 2024, 79:101841 Chin Med, 2024, 19(1):16 Nat Commun, 2023, 14(1):2656
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.	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.	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.
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)

FXR阻害剤の選択性比較