Membrane Transporters-Ion Channels

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  1. FXR agonist

    GW4064 is a selective, non-steroidal farnesoid X receptor (FXR) agonist (EC50 = 15 nM).
  2. FXR agonist

    WAY-362450 is a highly potent, selective, and orally bioavailable farnesoid X receptor (FXR) agonist (EC50: 4 nM, eff=149%).

  3. FXR agonist

    Lithocholic acid is a bile acid that acts as a detergent to solubilize fats for absorption.
  4. LXR/FXR agonist

    T0901317 is a potent and selective agonist for LXR and FXR, with EC50s of 50 nM and 5 μM, respectively
  5. FXR agonist

    Obeticholic Acid is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM
  6. FXR antagonist

    DY 268 is a trisubstituted-pyrazol carboamide based compound that acts as a potent FXR antagonist (IC50 = 7.5 nM).
  7. Sevelamer hydrochloride is a phosphate binding drug used to treat hyperphosphatemia in patients with chronic kidney disease; consists of polyallylamine that is crosslinked with epichlorohydrin.
  8. FXR anonist

    Tropifexor, also known as LJN452, is a farnesoid X receptor agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH).
  9. Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt.
  10. FXR agonist

    Fexaramine is a small molecule farnesoid X receptor (FXR) agonist with 100-fold increased affinity relative to natural compounds.

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