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  • Estradiol 17-(β-D-Glucuronide) (sodium salt hydrate)
Estradiol 17-(β-D-Glucuronide) (sodium salt hydrate)的可视化放大

Estradiol 17-(β-D-Glucuronide) (sodium salt hydrate)

A substrate of multidrug resistance protein 2

原价
¥1212-6662
价格
970-5330
Estradiol 17-(β-D-Glucuronide) (sodium salt hydrate)的二维码

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  • 库存: 现货
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  • 货号: ajcx24944
  • CAS: N/A
  • 别名: E217G, βEstradiol 17(βDGlucuronide), 17βEstradiol 17(βDGlucuronide), 17βOestradiol 17(βDGlucuronide)
  • 分子式: C24H31O8·Na [XH2O]
  • 分子量: 470.5
  • 纯度: >98%
  • 溶解度: DMF: 10 mg/ml,DMSO: 20 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
  • 储存: -20°C
  • 库存: 现货

Background

Estradiol 17-(β-D-glucuronide) (E217G) is an estrogen metabolite formed in the liver and subsequently excreted in bile.1 It acts as a substrate of the multidrug resistance protein 2 (MRP2; Km = 75 µM), and through MRP2-mediated transport, functions as a cholestatic agent, decreasing bile flow.1,2 In addition to binding to the MRP2 transport site, E217G has been shown to bind to an allosteric site that through positive cooperativity activates its own transport via MRP2 and the transport of other MRP2 substrates, including the non-cholestatic estrogen metabolite, estradiol 3-(β-D-glucuronide) .2,3 E217G has also been reported to be transported by MDR1, MRP1, MRP3, MRP4, MRP7, ABCG2 (a breast cancer resistance protein transporter), and the rat organic anion-transporting polypeptides 1-4.2



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 steroidsThe Journal of Biological Chemisty271(16)9683-9689(1996) 2.Gerk, P.M., Li, W., and 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-glucuronideDrug Metabolism and Disposition32(10)1139-1145(2004) 3.Gerk, P.M., Li, W., Megaraj, W., et al.Human multidrug resistance protein 2 transports the therapeutic bile salt tauroursodeoxycholateJournal of Pharmacology and Experimental Therapeutics320(2)893-899(2007)

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