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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
规格:98%
分子量:470.5
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
substrate of the multidrug resistance protein 2 (MRP2)
CAS:15087-02-2
分子式:C24H31O8 ? Na
分子量:470.5
纯度:98%
存储:Store at -20°C

Background:

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.


参考文献:
[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.