Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds toestrogen receptorwith anIC₅₀of 290 μM. Raloxifene is a selective and nonsteroidalestrogen receptormodulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression^[1][2][3].

IC50: 290 μM (Estrogen receptor)^[2]

Expressed UGT1A8 catalyzes Raloxifene 6-glucuronide with an apparent K_mof 7.9 μM and a V_maxof 0.61 nmol/min/mg of protein. Based on rates of Raloxifene glucuronidation and known extrahepatic expression, UGT1A8 and 1A10 appear to be primary contributors to Raloxifene glucuronidation in human jejunum microsomes. For human liver microsomes, the variability of Raloxifene 6-glucuronide formation is 3-fold. Correlation analyses reveals that UGT1A1 is responsible for Raloxifene 6-glucuronide but not Raloxifene 4'-glucuronide in liver. Treatment of expressed UGTs with alamethicin results in minor increases in enzyme activity, whereas in human intestinal microsomes, maximal increases of 8-fold for the Raloxifene 6-glucuronide are observed. Intrinsic clearance values in intestinal microsomes are 17 μl/min/mg for the Raloxifene 6-glucuronide^[2].

649.71

C₃₄H₃₅NO₁₀S

174264-50-7

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.