| CAS NO: | 15087-02-2 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 470.5 |
| Cas No. | 15087-02-2 |
| Formula | C24H31O8·Na |
| Synonyms | E217G,β-Estradiol 17-(β-D-Glucuronide),17β-Estradiol 17-(β-D-Glucuronide),17β-Oestradiol 17-(β-D-Glucuronide) |
| Solubility | ≤20mg/ml in DMSO;10mg/ml in dimethyl formamide |
| 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+] |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
Km: 75 μM
Estradiol 17-(β-D-Glucuronide) is a substrate of the multidrug resistance protein 2 (MRP2).
MRP2 is a member of the superfamily of ATP-binding cassette (ABC) transporters, which transport various molecules across extra- and intra-cellular membranes. MRP2 is a member of the MRP subfamily that is involved in multi-drug resistance. MRP2 is expressed in the apical side of the hepatocyte and functions in biliary transport.
In vitro: Estradiol 17-(β-D-Glucuronide) was identified as an ATP dependent, osmotically sensitive transport of the naturally occurring conjugated estrogen, and was found to be readily demonstrable in plasma membrane vesicles from populations of MRP-transfected HeLa cells. The involvement of MRP was confirmed by demonstrating that transport was completely inhibited by a monoclonal antibody specific for an intracellular conformational epitope of the protein [1].
In vivo: Animal study found that estradiol 17-(β-D-Glucuronide) could induce an immediate, profound and reversible inhibition of bile flow after its i.v. administration to the rat. Moreover, the cholestasis degree was found to be dose-dependent in the range of 8.5 to 21 mumol/kg i.v. A dose of 11 mumol/kg i.v. was able to inhibit bile flow and bile acid secretory rate 65 to 70% within 15 to 30 min of its administration. In addition, the bile flow and bile acid secretion returned to near control levels within 3 hours [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Loe, D. W.,Almquist, K.C.,Cole, S.P., et al. ATP-dependent 17β-estradiol 17-(β-D-glucuronide) transport by multidrug resistance protein (MRP). Inhibition by cholestatic steroids. The Journal of Biological Chemisty 271(16), 9683-9689 (1996).
[2] 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.
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