Estradiol 3-(β-D-Glucuronide) (sodium salt) (Synonyms: E23G,β-Estradiol 3-(β-D-Glucuronide),17β-Estradiol 3-(β-D-Glucuronide),17β-Oestradiol 3-(β-D-Glucuronide)) |
| Catalog No.GC17065 |
substrate for multidrug resistance protein 2 (MRP2)
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 14982-12-8
Sample solution is provided at 25 µL, 10mM.
β-estradiol 3-(β-d-glucuronide) (E23G) is a noncholestatic regioisomer of the estrogen metabolite, E217G (β-Estradiol 17-(β-d-glucuronide)) [1]. E23G functions as a substrate for multidrug resistance associated protein 2 (MRP2) [2].
MRP2 is a member of the MRP subfamily, belongs to the superfamily of ATP-binding cassette (ABC) transporters. MRP2 has been expressed in the canalicular (apical) part of the hepatocyte involved in multi-drug resistance, and functions in biliary transport [3].
In vitro: In Sf9 cells infected with the recombinant baculovirus of which baculovirus genome containing rat Mrp2, E23G (0.4-400 μM) completely and competitively inhibited E217G transport with an IC50 value of 14.2 μM. Doses of E217G at 0.01-250 μM inhibited only 53% of E23G transport with an IC50 of 33.4 μM [1]. It has been reported E23G inhibited E217G transport through rat organic anion-transporting polypeptide 1 with a Ki value of 9.7 μM. E23G was a low-affinity inhibitor of both MRP4 and MRP7 with IC50s of ~ 100 μM. The noncholestatic E23G behaved as an Mrp2 substrate which could compete with E217G for transport, but did not activate the allosteric site. In Sf9 cell membranes expressing multidrug resistance protein 2 (MRP2), E23G functioned as a substrate for MRP2 with Km of 122 μM, competing with E217G for MRP2-mediated transport [3].
References:
[1] Gerk P M, Li W, Vore M. Estradiol 3-glucuronide is transported by the multidrug resistance-associated protein 2 but does not activate the allosteric site bound by estradiol 17-glucuronide[J]. Drug metabolism and disposition, 2004, 32(10): 1139-1145.
[2] Gerk P M, Li W, Megaraj V, et al. Human multidrug resistance protein 2 transports the therapeutic bile salt tauroursodeoxycholate[J]. Journal of Pharmacology and Experimental Therapeutics, 2007, 320(2): 893-899.
[3] Borst P, Evers R, Kool M, et al. The multidrug resistance protein family[J]. Biochimica et Biophysica Acta (BBA)-Biomembranes, 1999, 1461(2): 347-357.
| Cas No. | 14982-12-8 | SDF | |
| Synonyms | E23G,β-Estradiol 3-(β-D-Glucuronide),17β-Estradiol 3-(β-D-Glucuronide),17β-Oestradiol 3-(β-D-Glucuronide) | ||
| Chemical Name | (17β)-17-hydroxyestra-1,3,5(10)-trien-3-yl β-D-glucopyranosiduronic acid, monosodium salt | ||
| Canonical SMILES | [O-]C([C@H]([C@@H](O)[C@H](O)[C@H]1O)O[C@H]1OC2=CC=C3C(CC[C@]4([H])[C@]3([H])CC[C@@]5(C)[C@@]4([H])CC[C@@H]5O)=C2)=O.[Na+] | ||
| Formula | C24H31O8 • Na | M.Wt | 470.5 |
| Solubility | ≤20mg/ml in DMSO;10mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1254 mL | 10.627 mL | 21.254 mL |
| 5 mM | 0.4251 mL | 2.1254 mL | 4.2508 mL |
| 10 mM | 0.2125 mL | 1.0627 mL | 2.1254 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >95.00%
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Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)
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