Estradiol 3-(β-D-Glucuronide) (sodium salt)
(Synonyms: E23G,β-Estradiol 3-(β-D-Glucuronide),17β-Estradiol 3-(β-D-Glucuronide),17β-Oestradiol 3-(β-D-Glucuronide)) 目录号 : GC17065An isomer of estradiol-(β-D-glucuronide)
Cas No.:14982-12-8
Sample solution is provided at 25 µL, 10mM.
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].
References:
[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.
| Cas No. | 14982-12-8 | SDF | |
| 别名 | E23G,β-Estradiol 3-(β-D-Glucuronide),17β-Estradiol 3-(β-D-Glucuronide),17β-Oestradiol 3-(β-D-Glucuronide) | ||
| 化学名 | (17β)-17-hydroxyestra-1,3,5(10)-trien-3-yl β-D-glucopyranosiduronic acid, monosodium salt | ||
| Canonical SMILES | [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+] | ||
| 分子式 | C24H31O8 • Na | 分子量 | 470.5 |
| 溶解度 | ≤20mg/ml in DMSO;10mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1254 mL | 10.627 mL | 21.254 mL |
| 5 mM | 0.4251 mL | 2.1254 mL | 4.2508 mL |
| 10 mM | 0.2125 mL | 1.0627 mL | 2.1254 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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