Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds toestrogen receptorwith anIC₅₀of 370 μM.^[1][2]. Raloxifene is a selectiveestrogen receptormodulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression^[3].

IC50: 370 μM (Estrogen receptor)^[2]

Expressed UGT1A8 catalyzes Raloxifene 4'-glucuronide with an apparent K_mof 59 μM and a V_maxof 2.0 nmol/min/mg. 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 4'-glucuronide formation is 4-fold. Treatment of expressed UGTs with alamethicin results in minor increases in enzyme activity, whereas in human intestinal microsomes, maximal increases of 9-fold for the Raloxifene 4'-glucuronide are observed. Intrinsic clearance values in intestinal microsomes are 95 μl/min/mg for the Raloxifene 4'-glucuronide^[2].

649.71

C₃₄H₃₅NO₁₀S

182507-22-8

Room temperature in continental US; may vary elsewhere.

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