- Inhibitory Selectivity
|Catalog No.||Product Name||Solubility(25°C)|
|S2782||GW4064||<1 mg/mL||100 mg/mL||<1 mg/mL|
|S2694||Turofexorate Isopropyl (XL335)||<1 mg/mL||33 mg/mL||2 mg/mL|
|S1843||Chenodeoxycholic Acid||<1 mg/mL||79 mg/mL||79 mg/mL|
|S4003||Lithocholic acid||<1 mg/mL||75 mg/mL||47 mg/mL|
|S7660||Obeticholic Acid||<1 mg/mL||84 mg/mL||84 mg/mL|
- FXR Inhibitors (5)
|Catalog No.||Information||Product Use Citations||Product Validations|
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.
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.
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.
Chenodeoxycholic Acid is a naturally occurring human bile acid, and inhibits production of cholesterol in the liver and absorption in the intestines.
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.
Obeticholic Acid is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. Phase 3.
(D) Expression of hepatic FXR target genes, n = 3. Data are expressed as mean ± SD, ###P < 0.001 versus group 1, *P < 0.05, **P < 0.01, and ***P b 0.001 versus group 2, sP < 0.05, ssP < 0.01, and sssP < 0.001 versus group 3