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Estradiol 17-(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 17-(β-D-Glucuronide)(sodium salt)图片
CAS NO:15087-02-2
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍

化学性质

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt470.5
Cas No.15087-02-2
FormulaC24H31O8·Na
SynonymsE217G,β-Estradiol 17-(β-D-Glucuronide),17β-Estradiol 17-(β-D-Glucuronide),17β-Oestradiol 17-(β-D-Glucuronide)
Solubility≤20mg/ml in DMSO;10mg/ml in dimethyl formamide
Chemical Name(17β)-3-hydroxyestra-1,3,5(10)-trien-17-yl β-D-glucopyranosiduronic acid, monosodium salt
Canonical SMILES[H][C@@]12CCC3=CC(O)=CC=C3[C@@]1([H])CC[C@@]4(C)[C@@]2([H])CC[C@@H]4O[C@@]5([H])[C@H](O)[C@@H](O)[C@H](O)[C@@H](C([O-])=O)O5.[Na+]
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

资料参考

Km: 75 μM

Estradiol 17-(β-D-Glucuronide) is a substrate of the multidrug resistance protein 2 (MRP2).

MRP2 is a member of the superfamily of ATP-binding cassette (ABC) transporters, which transport various molecules across extra- and intra-cellular membranes. MRP2 is a member of the MRP subfamily that is involved in multi-drug resistance. MRP2 is expressed in the apical side of the hepatocyte and functions in biliary transport.

In vitro: Estradiol 17-(β-D-Glucuronide) was identified as an ATP dependent, osmotically sensitive transport of the naturally occurring conjugated estrogen, and was found to be readily demonstrable in plasma membrane vesicles from populations of MRP-transfected HeLa cells. The involvement of MRP was confirmed by demonstrating that transport was completely inhibited by a monoclonal antibody specific for an intracellular conformational epitope of the protein [1].

In vivo: Animal study found that estradiol 17-(β-D-Glucuronide) could induce an immediate, profound and reversible inhibition of bile flow after its i.v. administration to the rat. Moreover, the cholestasis degree was found to be dose-dependent in the range of 8.5 to 21 mumol/kg i.v. A dose of 11 mumol/kg i.v. was able to inhibit bile flow and bile acid secretory rate 65 to 70% within 15 to 30 min of its administration. In addition, the bile flow and bile acid secretion returned to near control levels within 3 hours [2].

Clinical trial: So far, no clinical study has been conducted.

References:
[1] Loe, D. W.,Almquist, K.C.,Cole, S.P., et al. ATP-dependent 17β-estradiol 17-(β-D-glucuronide) transport by multidrug resistance protein (MRP). Inhibition by cholestatic steroids. The Journal of Biological Chemisty 271(16), 9683-9689 (1996).
[2] Meyers M, Slikker W, Pascoe G, Vore M.  Characterization of cholestasis induced by estradiol-17 beta-D-glucuronide in the rat. J Pharmacol Exp Ther. 1980 Jul;214(1):87-93.