Estradiol 3-glucuronide 

Estradiol 3-glucuronide is an estrogen metabolite, which is a glucuronide conjugate formed from Estradiol (HY-B0141) via catalysis by uridine diphosphate glucuronosyltransferases in tissues such as the liver. Estradiol 3-glucuronide is a potent substrate of Mrp2, with an S₅₀ value of 55.7 μM. Estradiol 3-glucuronide achieves hepatobiliary transport in hepatocytes through basolateral uptake via OATP1B1, OATP1B3 and OATP2B1, as well as apical efflux via MRP2 and BCRP^[1][2][3].

Estradiol 3-glucuronide (1-5 μM; 2 minutes) is a substrate for OATP1B1, OATP1B3, and OATP2B1 in transfected HEK293T cells, with OATP2B1 exhibiting the highest transport efficiency (V_max/K_m = 33.2) and acting as the primary transporter at low concentrations^[2].
Estradiol 3-glucuronide (5 μM; 2 minutes) uptake by OATP1B1, OATP1B3, and OATP2B1 in transfected HEK293T cells is differentially inhibited by known OATP substrates/inhibitors, with estrone-3-sulfate showing the strongest inhibitory effect on OATP1B1-mediated uptake (IC₅₀ = 0.05 μM)^[2].
Estradiol 3-glucuronide (50 μM; 2 minutes) weakly to moderately inhibits OATP1B3-, OATP2B1-mediated estrone-3-sulfate uptake and OATP1B1-, OATP1B3-, OATP2B1-mediated Rosuvastatin (HY-17504A) uptake in transfected HEK293T cells^[2].
Estradiol 3-glucuronide (30-110 nM; up to 20 min) is a substrate of rat Mrp2 expressed in Sf9 cell membrane vesicles, with an S₅₀ of 55.7 μM and slight negative cooperativity in transport^[1].
Estradiol 3-glucuronide (0.4-400 μM) competitively and completely inhibits rat Mrp2-mediated transport of Estradiol 17-glucuronide in Sf9 cell membrane vesicles with an IC₅₀ of 14.2 μM^[1].

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

Immunization of albino rabbits with the Estradiol 3-glucuronide-BSA conjugate yields high-affinity antiserum; after purification, this antiserum exhibits extremely high specificity for Estradiol 3-glucuronide and enables accurate direct radioimmunoassay of this compound in urine samples^[3].

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

448.51

C₂₄H₃₂O₈

15270-30-1

Solid

White to off-white

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Room temperature in continental US; may vary elsewhere.

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

* 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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

• [1]. Gerk PM, et al. Estradiol 3-glucuronide is transported by the multidrug resistance-associated protein 2 but does not activate the allosteric site bound by estradiol 17-glucuronide. Drug Metab Dispos. 2004;32(10):1139-1145.  [Content Brief]

  [2]. Li L, et al. Hepatic uptake of estradiol-3-glucuronide and estradiol-3-sulfate-17β-glucuronide by human organic anion transporting polypeptides 1B1, 1B3, and 2B1. Drug Metab Dispos. 2025 Sep;53(9):100132.
  

  [3]. Nambara T, et al. A direct radioimmunoassay of estradiol 3-glucuronide using specific antiserum. Chem Pharm Bull (Tokyo). 1983 Oct;31(10):3583-8.
   [Content Brief]