Estradiol 17-(β-D-Glucuronide) 

Estradiol 17-(β-D-Glucuronide) is a D-ring glucuronide metabolite of natural estrogen formed in the liver. Estradiol 17-(β-D-Glucuronide) is a substrate of the organic anion-transporting polypeptide family (Oatp) and multidrug resistance-associated protein 2 (Mrp2). Estradiol 17-(β-D-Glucuronide) regulates MRP8-mediated transport processes and inhibits MRP8-mediated transport of dehydroepiandrosterone 3-sulfate and taurocholic acid. Estradiol 17-(β-D-Glucuronide) induces immediate, reversible reduction of bile flow and acute intrahepatic cholestasis in female rats without altering the bile acid composition in bile. Estradiol 17-(β-D-Glucuronide) can be used in studies related to intrahepatic cholestasis^[1][2][3].

Estradiol 17-(β-D-Glucuronide) (1-1000 μM; 5-10 min) is a substrate of MRP8 in MRP8-transfected LLC-PK1 cell membrane vesicles, with a K_m of 62.9 μM and V_max of 62.0 pmol/mg/min, and it also acts as a concentration-dependent inhibitor of MRP8-mediated DHEAS and taurocholate transport^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Estradiol 17-(β-D-Glucuronide) (10 μmol/kg (4.5 mg/kg); i.v.; single dose) induces severe, reversible intrahepatic cholestasis in female Sprague-Dawley rats via reduced bile flow, with over 84% of the dose excreted into bile, without altering endogenous biliary bile acid composition^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

448.51

C₂₄H₃₂O₈

1806-98-0

Solid

White to off-white

C[C@@]12[C@](CC[C@@H]2O[C@@H]3O[C@@H]([C@H]([C@@H]([C@H]3O)O)O)C(O)=O)([H])[C@@]4([H])[C@@](CC1)([H])C5=CC=C(O)C=C5CC4

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Kinbara S, et al. Improvement of estradiol-17 beta-D-glucuronide-induced cholestasis by sodium tauroursodeoxycholate therapy in rats. Scand J Gastroenterol. 1997 Sep;32(9):947-52.  [Content Brief]

  [2]. Chen ZS, et al. Transport of bile acids, sulfated steroids, estradiol 17-beta-D-glucuronide, and leukotriene C4 by human multidrug resistance protein 8 (ABCC11). Mol Pharmacol. 2005;67(2):545-557.  [Content Brief]

  [3]. Sun H, et al. Increased estrogen sulfation of estradiol 17beta-D-glucuronide in metastatic tumor rat livers. J Pharmacol Exp Ther. 2006 Nov;319(2):818-31.  [Content Brief]