A substrate of multidrug resistance protein 2
货号:ajcx24944
CAS:N/A
分子式:C24H31O8·Na [XH2O]
分子量：470.5
溶解度:DMF: 10 mg/ml,DMSO: 20 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
纯度：98%
存储：Store at -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.¹It acts as a substrate of the multidrug resistance protein 2 (MRP2; K_m= 75 µM), and through MRP2-mediated transport, functions as a cholestatic agent, decreasing bile flow.^1,2In 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 transportviaMRP2 and the transport of other MRP2 substrates, including the non-cholestatic estrogen metabolite, estradiol 3-(β-D-glucuronide) .^2,3E₂17G 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)