| CAS NO: | 362-05-0 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 288.4 |
| Cas No. | 362-05-0 |
| Formula | C18H24O3 |
| Synonyms | 2-HE2,NSC 61711 |
| Solubility | ≤20mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide |
| Chemical Name | estra-1,3,5(10)-triene-2,3,17β-triol |
| Canonical SMILES | OC1=C(O)C=C(CC[C@]2([H])[C@]3([H])CC[C@@]4(C)[C@@]2([H])CC[C@@H]4O)C3=C1 |
| 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。 |
2-Hydroxyestradiol is an angiogenesis inhibitor via the HIF-1a pathway.
HIF-1a, a basic helix-loop-helix PAS domain containing protein, is reported as the master transcriptional regulator of cellular and developmental response to hypoxia.
In vitro: In vitro evidences suggested that most of the cellular effects of 2-hydroxyestradiol were mediated by 2-methoxyestradiol, a metabolite of 2-hydroxyestradiol as an anti-cancer agent acting as an angiogenesis inhibitor via the HIF-1a pathway. Inhibition of catechol-O-methyltransferase (COMT), the enzyme methylating 2-hydroxyestradiol to 2-methoxyestradiol, blocked the ability of 2-hydroxyestradiol to inhibit growth of vascular smooth muscle cells, cardiac fibroblasts, as well as renal mesangial cells. Moreover, 2-hydroxyestradiol could inhibit vascular smooth muscle cell growth in cells obtained from wild-type mice but not in cells cultured from COMT knockout mice. In contrast to 2OHE, treatment of vascular smooth muscle cells with 2-methoxyestradiol inhibited serum-induced growth of cells from both wild-type and COMTknockout mice [1].
In vivo: Animal study showed that after administration of 2-hydroxyestradiol, plasma levels of 2-hydroxyestradiol declined extremely rapidly. Concomitant with the disappearance of 2-hydroxyestradiol, 2-methoxyestradiol occurred and then declined. After administration of 2-methoxyestradiol, plasma levels of 2MEOE declined with a plasma CL of 50 ml min(-1) kg(-1). We could not detect 2-hydroxyestradiol in plasma from rats receiving 2-methoxyestradiol. Thus, the authors conclude that the conversion of 2-hydroxyestradiol to 2-methoxyestradiol was so efficient, and the administration of 2-hydroxyestradiol is bioequivalent to administration of 2-methoxyestradiol itself [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Zacharia, L. C.,Piché, C.A.,Fielding, R.M., et al. 2-hydroxyestradiol is a prodrug of 2-methoxyestradiol. Journal of Pharmacology and Experimental Therapeutics 309(3), 1093-1097 (2004).
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