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Estradiol 3-(β-D-Glucuronide)(sodium salt)
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Estradiol 3-(β-D-Glucuronide)(sodium salt)图片
CAS NO:14982-12-8
包装与价格：
包装价格(元)
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substrate for multidrug resistance protein 2 (MRP2)
Cas No.14982-12-8
别名E23G,β-Estradiol 3-(β-D-Glucuronide),17β-Estradiol 3-(β-D-Glucuronide),17β-Oestradiol 3-(β-D-Glucuronide)
化学名(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+]
分子式C24H31O8o Na
分子量470.5
溶解度≤20mg/ml in DMSO;10mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.

 
 
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