Estradiol 17-(β-D-Glucuronide) (sodium salt) (Synonyms: E217G,β-Estradiol 17-(β-D-Glucuronide),17β-Estradiol 17-(β-D-Glucuronide),17β-Oestradiol 17-(β-D-Glucuronide)) |
| Catalog No.GC10964 |
Estradiol 17-(β-D-Glucuronide) is a metabolic product of estradiol, the main female sex hormone.
Products are for research use only. Not for human use. We do not sell to patients.
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.
| Cell experiment [1]: | |
|
Cell lines |
rat hepatocyte SCRH |
|
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. |
|
Reaction Conditions |
200µM；20 min |
|
Applications |
Estradiol 17-(β-D-Glucuronide) induces Abcc2 damage and endocytic internalization. |
| Animal experiment [2]: | |
|
Animal models |
Sprague-Dawley rats |
|
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. |
|
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. |
|
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 | |
| Synonyms | E217G,β-Estradiol 17-(β-D-Glucuronide),17β-Estradiol 17-(β-D-Glucuronide),17β-Oestradiol 17-(β-D-Glucuronide) | ||
| Chemical Name | (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+] | ||
| Formula | C24H31O8 • Na [XH2O] | M.Wt | 470.5 |
| Solubility | ≤20mg/ml in DMSO;10mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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- Purity: >95.00%
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