Estradiol 17-(β-D-Glucuronide)
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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.
For research use only. We do not sell to patients.
- Purity: 99.0%
- CAS No.: 1806-98-0
- Formula: C24H32O8
- Molecular Weight:448.51
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All Endogenous Metabolite Isoforms
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf9 | IC50 |
13.3 μM
Compound: Estradiol-17beta-D-glucuronide
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TP_TRANSPORTER: inhibition of DNP-SG uptake (DNP-SG: 0.05 uM) in membrane vesicles from Mrp2-expressing Sf9 cells
TP_TRANSPORTER: inhibition of DNP-SG uptake (DNP-SG: 0.05 uM) in membrane vesicles from Mrp2-expressing Sf9 cells
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[PMID: 11306690] |
| Sf9 | IC50 |
30 μM
Compound: Estradiol-17beta-D-glucuronide
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TP_TRANSPORTER: inhibition of DHEAS in membrane vesicles from MRP4-expressing Sf9 cells
TP_TRANSPORTER: inhibition of DHEAS in membrane vesicles from MRP4-expressing Sf9 cells
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[PMID: 12523936] |
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 Km of 62.9 μM and Vmax 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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (female, 160-250 g)[1]
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Dosage:10 μmol/kg
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Administration:i.v.; single dose
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Result:Caused severe, immediate, reversible reduction in bile flow.
Reached more than 84% of the administered dose in biliary excretion.
Showed no significant change in biliary composition of seven endogenous bile acids relative to intact control rats.
Chemical Information
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CAS No. 1806-98-0
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Appearance Solid
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Molecular Weight 448.51
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Formula C24H32O8
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Color White to off-white
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SMILES
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
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 4.5 mg/mL (10.03 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (277 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2296 mL | 11.1480 mL | 22.2960 mL | 55.7401 mL |
| 5 mM | 0.4459 mL | 2.2296 mL | 4.4592 mL | 11.1480 mL | |
| 10 mM | 0.2230 mL | 1.1148 mL | 2.2296 mL | 5.5740 mL |
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