Estradiol 17-(β-D-Glucuronide) (sodium salt)
(Synonyms: Β雌二醇17-(Β-D-葡萄糖醛酸)钠盐,E217G,β-Estradiol 17-(β-D-Glucuronide),17β-Estradiol 17-(β-D-Glucuronide),17β-Oestradiol 17-(β-D-Glucuronide)) 目录号 : GC10964Estradiol 17-(β-D-Glucuronide)是雌二醇(一种主要的女性性激素)经过代谢形成的产物。
Cas No.:15087-02-2
Sample solution is provided at 25 µL, 10mM.
Estradiol 17-(β-D-Glucuronide) is a metabolic product of estradiol, the main female sex hormone. In the human body, estradiol can be combined with glucuronic acid to form estradiol glucuronide, namely Estradiol 17-(β-D-Glucuronide). Estradiol 17-(β-D-Glucuronide) is a substrate of the organic anion transporting peptide family (Oatp) and multidrug resistance protein (Mrp2)[1]. Estradiol 17-(β-D-Glucuronide) can induce cholestasis [2].
In vitro, treatment with 200µM Estradiol 17-(β-D-Glucuronide) for 20 minutes in rat hepatocytes can induce dysfunction and internalization of the canalicular transporter protein Abcc2 [3].
In vivo, Estradiol 17-(β-D-Glucuronide) (15 µmol/kg; i.v.) impairs bile salt (BS) output in female SD rats, inducing internalization of the bile salt export pump (Bsep) [4]. Estradiol 17-(β-D-Glucuronide) can inhibit rat bile flow, showing a dose-dependent effect on the degree of cholestasis within the intravenous dosage range of 8.5 to 21 µmol/kg. A dose of 11 µmol/kg administered over 15-30 minutes reduced the bile acid secretion rate by nearly 70% [5].
References:
[1] Huadong Sun, Lichuan Liu, and K. Sandy Pang.Increased Estrogen Sulfation of Estradiol 17β-D-Glucuronide in Metastatic Tumor Rat Livers[J]Journal of Pharmacology and Experimental Therapeutics . 2006. 319: 818-831.
[2] Zucchetti, AndrÉs E, Barosso I R , Boaglio A ,et al.Prevention of estradiol 17beta-D-glucuronide-induced canalicular transporter internalization by hormonal modulation of cAMP in rat hepatocytes.[J]. Molecular Biology of the Cell, 2011, 22(20):3902-3915.
[3] Barosso I R ,Zucchetti, AndrÉs E, Miszczuk G S ,et al. EGFR participates downstream of ERα in estradiol-17β-D-glucuronide-induced impairment of Abcc2 function in isolated rat hepatocyte couplets.[J]Archives of Toxicology, 2016, 90(4):891-903.
[4] Fernando A. Crocenzi,1Aldo D. Mottino, et al.Estradiol-17β-D-glucuronide induces endocytic internalization of Bsep in rats.[J]Am J Physiol Gastrointest Liver Physiol (285): 449-459, 2003.
[5] Meyers M, Slikker W, Pascoe G, Vore M. Characterization of cholestasis induced by estradiol-17 beta-D-glucuronide in the rat. J Pharmacol Exp Ther. 1980 Jul;214(1):87-93.
Estradiol 17-(β-D-Glucuronide)是雌二醇(一种主要的女性性激素)经过代谢形成的产物。在人体内,雌二醇可以通过与葡萄糖醛酸结合的方式形成雌二醇葡萄糖醛酸化物,即Estradiol 17-(β-D-Glucuronide)。Estradiol 17-(β-D-Glucuronide)是有机阴离子转运多肽家族(Oatp)和多药耐药蛋白(Mrp2)的底物[1]。Estradiol 17-(β-D-Glucuronide)可诱导胆汁淤积[2]。
在体外,Estradiol 17-(β-D-Glucuronide) 200µM处理大鼠肝细胞20 min可诱导 小管转运蛋白Abcc2功能损伤和内吞内化[3]。
在体内,Estradiol 17-(β-D-Glucuronide) (15 µmol/kg; i.v.) 会损害雌性SD大鼠胆盐(BS)输出,诱导胆盐输出泵(Bsep)内化[4]。 Estradiol 17-(β-D-Glucuronide)可抑制大鼠胆汁流动,在8.5至21 µmol/kg 静脉注射范围内对胆汁淤积程度具有剂量依赖性,11 µmol/kg 的剂量给药后15 -30分钟内使胆汁酸分泌率下降了近70%[5]。
| Cell experiment [1]: | |
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Cell lines |
rat hepatocyte SCRH |
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Preparation Method |
SCRH were treated with Estradiol 17-(β-D-Glucuronide) (200µM, 20min) or vehicle (DMSO, control) and then fixed with 4 % paraformaldehyde in PBS for 30 min, blocked and permeabilized with 3 % BSA and 0.5 % Triton X-100 for 30 min. |
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Reaction Conditions |
200µM；20 min |
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Applications |
Estradiol 17-(β-D-Glucuronide) induces Abcc2 damage and endocytic internalization. |
| Animal experiment [2]: | |
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Animal models |
Sprague-Dawley rats |
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Preparation Method |
The rats were anesthetized with urethane (1000 mg/kg ip) . The femoral vein and the common bile duct were cannulated with polyethylene tubing. Next, Estradiol 17-(β-D-Glucuronide) (4.25mmol/l in saline-propylene glycol-ethanol, 10:4:1; 15 µmol/kg i.v.) was administered , and bile was collected for 5 min, 15 min after Estradiol 17-(β-D-Glucuronide) administration. |
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Dosage form |
15 µmol/kg; i.v. |
|
Applications |
Estradiol 17-(β-D-Glucuronide) (15 µmol/kg i.v.) impaired bile salt (BS) output and induced Bsep internalization. |
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References: [1] Barosso I R ,Zucchetti, AndrÉs E, Miszczuk G S ,et al. EGFR participates downstream of ERα in estradiol-17β-D-glucuronide-induced impairment of Abcc2 function in isolated rat hepatocyte couplets.[J]Archives of Toxicology, 2016, 90(4):891-903. | |
| Cas No. | 15087-02-2 | SDF | |
| 别名 | Β雌二醇17-(Β-D-葡萄糖醛酸)钠盐,E217G,β-Estradiol 17-(β-D-Glucuronide),17β-Estradiol 17-(β-D-Glucuronide),17β-Oestradiol 17-(β-D-Glucuronide) | ||
| 化学名 | (17β)-3-hydroxyestra-1,3,5(10)-trien-17-yl β-D-glucopyranosiduronic acid, monosodium salt | ||
| Canonical SMILES | [H][C@@]12CCC3=CC(O)=CC=C3[C@@]1([H])CC[C@@]4(C)[C@@]2([H])CC[C@@H]4O[C@@]5([H])[C@H](O)[C@@H](O)[C@H](O)[C@@H](C([O-])=O)O5.[Na+] | ||
| 分子式 | C24H31O8 • Na[XH2O] | 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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| 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 |
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| 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 |
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| % 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，
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2.
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- Purity: >95.00%
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