Estradiol 3-(β-D-Glucuronide) (sodium salt)_多药耐药蛋白2(MRP2)的底物_14982-12-8_Apexbio
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产品说明书
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产品名: Cas No.: 分子量: 分子式: 别名:
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溶解性: 储存条件: 一般建议:
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生物活性
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产品名: Estradiol 3-(β-D-Glucuronide) (sodium salt) 修订日期: 6/30/2016
Estradiol 3-(β-D-Glucuronide) (sodium salt) 14982-12-8 470.5 C24H31O8 • Na E23G,β-Estradiol 3-(β-D-Glucuronide),17β-Estra diol 3-(β-D-Glucuronide),17β-Oestr adiol 3-(β-D-Glucuronide) (17β)-17-hydroxyestra-1,3,5(10)-trien-3-yl β-D-glucopyranosiduronic acid, monosodium salt [O-]C([C@H]([C@@H](O)[C@H](O)[C@H]1O)O[C@H]1OC2=CC=C3C( CC[C@]4([H])[C@]3([H])CC[C@@]5(C)[C@@]4([H])CC[C@@H]5O)= C2)=O.[Na+] Soluble in DMSO Store at -20°C For obtaining a higher solubility , please warm the tube at 37°C and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
参考文献: [1] Gerk P M, Li W, 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-glucuronide[J]. Drug metabolism and disposition, 2004, 32(10): 1139-1145. [2] Gerk P M, Li W, Megaraj V, et al. Human multidrug resistance protein 2 transports the therapeutic bile salt tauroursodeoxycholate[J]. Journal of Pharmacology and Experimental Therapeutics, 2007, 320(2): 893-899. [3] Borst P, Evers R, Kool M, et al. The multidrug resistance protein family[J]. Biochimica et Biophysica Acta (BBA)-Biomembranes, 1999, 1461(2): 347-357.
特别声明
产品仅用于研究，
不针对患者销售，望谅解。
每个产品具体的储存和使用信息显示在产品说明书中。ApexBio 产品在推荐的条件下是稳定 的。产品会根据不同的推荐温度进行运输。许多产品短期运输是稳定的，运输温度不同于长 期储存的温度。我们确保我们的产品是在保持试剂质量的条件下运输的。收到产品后，按照 产品说明书上的要求进行储存。
ApexBio Technology
Membrane Transporter/Ion Channel P-gp
产品描述:
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 ~ 100 μM. The noncholestatic E23G behaved as an Mrp2 substrate which could compete with E217G for transport, but did not activate the allosteric site. In Sf9 cell membranes expressing multidrug resistance protein 2 (MRP2), E23G functioned as a substrate for MRP2 with Km of 122 μM, competing with E217G for MRP2-mediated transport [3].
化学wenku.baidu.com质
产品名: Cas No.: 分子量: 分子式: 别名:
化学名: SMILES:
溶解性: 储存条件: 一般建议:
运输条件:
生物活性
靶点 : 信号通路:
产品名: Estradiol 3-(β-D-Glucuronide) (sodium salt) 修订日期: 6/30/2016
Estradiol 3-(β-D-Glucuronide) (sodium salt) 14982-12-8 470.5 C24H31O8 • Na E23G,β-Estradiol 3-(β-D-Glucuronide),17β-Estra diol 3-(β-D-Glucuronide),17β-Oestr adiol 3-(β-D-Glucuronide) (17β)-17-hydroxyestra-1,3,5(10)-trien-3-yl β-D-glucopyranosiduronic acid, monosodium salt [O-]C([C@H]([C@@H](O)[C@H](O)[C@H]1O)O[C@H]1OC2=CC=C3C( CC[C@]4([H])[C@]3([H])CC[C@@]5(C)[C@@]4([H])CC[C@@H]5O)= C2)=O.[Na+] Soluble in DMSO Store at -20°C For obtaining a higher solubility , please warm the tube at 37°C and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
参考文献: [1] Gerk P M, Li W, 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-glucuronide[J]. Drug metabolism and disposition, 2004, 32(10): 1139-1145. [2] Gerk P M, Li W, Megaraj V, et al. Human multidrug resistance protein 2 transports the therapeutic bile salt tauroursodeoxycholate[J]. Journal of Pharmacology and Experimental Therapeutics, 2007, 320(2): 893-899. [3] Borst P, Evers R, Kool M, et al. The multidrug resistance protein family[J]. Biochimica et Biophysica Acta (BBA)-Biomembranes, 1999, 1461(2): 347-357.
特别声明
产品仅用于研究，
不针对患者销售，望谅解。
每个产品具体的储存和使用信息显示在产品说明书中。ApexBio 产品在推荐的条件下是稳定 的。产品会根据不同的推荐温度进行运输。许多产品短期运输是稳定的，运输温度不同于长 期储存的温度。我们确保我们的产品是在保持试剂质量的条件下运输的。收到产品后，按照 产品说明书上的要求进行储存。
ApexBio Technology
Membrane Transporter/Ion Channel P-gp
产品描述:
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 ~ 100 μM. The noncholestatic E23G behaved as an Mrp2 substrate which could compete with E217G for transport, but did not activate the allosteric site. In Sf9 cell membranes expressing multidrug resistance protein 2 (MRP2), E23G functioned as a substrate for MRP2 with Km of 122 μM, competing with E217G for MRP2-mediated transport [3].