FXR
Inhibitory Selectivity
FXR Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S3736 |
Fondaparinux SodiumFondaparinux is a synthetic glucopyranoside with antithrombotic activity. It selectively binds to antithrombin III, thereby potentiating the innate neutralization of activated factor X (Factor Xa) by antithrombin; a synthetic inhibitor of Factor Xa. |
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| S3792New |
Guggulsterone E&ZGuggulsterone 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. |
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| S2782 |
GW4064GW4064 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. |
FXR agonist GW4064 reduced the association between β-Catenin/TCF4 complex and the TCF binding sites from Cyclin D1 promoter. ChIP analysis was carried out using antibodies against TCF4, β-Catenin, or normal IgG in lysates from Huh7 cells.
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| S2694 |
Turofexorate Isopropyl (XL335)Turofexorate Isopropyl (XL335) 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. |
(B) FXR agonists repressed β-Catenin mediated transcriptional activity. HEK293 cells were transfected with TOPflash reporter and pRLTK plasmid, and then treated with FXR agonists, GW4064 or WAY-36240, ranging from 1–4 μM. Luciferase activity was measured 12-24 hours post treatment. TOPflash/FOPflash activity was normalized to that of the controls. |
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| S1843 |
Chenodeoxycholic AcidChenodeoxycholic Acid is a naturally occurring human bile acid, and inhibits production of cholesterol in the liver and absorption in the intestines. |
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| S4003 |
Lithocholic acidLithocholic 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. |
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| S8733New |
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). |
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| S6413New |
fexaramineFexaramine 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. |
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| S7660 |
Obeticholic AcidObeticholic Acid is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. Phase 3. |
HuCCT1 cells were treated with OCA (1 μM) and control solvent in the presence and absence of IL-6 (20 ng/mL). EMT-related proteins were examined by western blotting. β-actin was used as a control.
|
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S3736 |
Fondaparinux SodiumFondaparinux is a synthetic glucopyranoside with antithrombotic activity. It selectively binds to antithrombin III, thereby potentiating the innate neutralization of activated factor X (Factor Xa) by antithrombin; a synthetic inhibitor of Factor Xa. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S3792New |
Guggulsterone E&ZGuggulsterone 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. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S2782 |
GW4064GW4064 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. |
FXR agonist GW4064 reduced the association between β-Catenin/TCF4 complex and the TCF binding sites from Cyclin D1 promoter. ChIP analysis was carried out using antibodies against TCF4, β-Catenin, or normal IgG in lysates from Huh7 cells.
|
|
| S2694 |
Turofexorate Isopropyl (XL335)Turofexorate Isopropyl (XL335) 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. |
(B) FXR agonists repressed β-Catenin mediated transcriptional activity. HEK293 cells were transfected with TOPflash reporter and pRLTK plasmid, and then treated with FXR agonists, GW4064 or WAY-36240, ranging from 1–4 μM. Luciferase activity was measured 12-24 hours post treatment. TOPflash/FOPflash activity was normalized to that of the controls. |
|
| S1843 |
Chenodeoxycholic AcidChenodeoxycholic Acid is a naturally occurring human bile acid, and inhibits production of cholesterol in the liver and absorption in the intestines. |
||
| S4003 |
Lithocholic acidLithocholic 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. |
||
| S8733New |
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). |
||
| S6413New |
fexaramineFexaramine 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. |
||
| S7660 |
Obeticholic AcidObeticholic Acid is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. Phase 3. |
HuCCT1 cells were treated with OCA (1 μM) and control solvent in the presence and absence of IL-6 (20 ng/mL). EMT-related proteins were examined by western blotting. β-actin was used as a control.
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