substrate for multidrug resistance protein 2 (MRP2)
CAS：14982-12-8
分子式：C24H31O8 ? Na
分子量：470.5
纯度：98%
存储：Store at -20°C

Background:

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