2-Hydroxyestradiol (Synonyms: 2-HE2,NSC 61711) |
| رقم الكتالوجGC13460 |
2-Hydroxyestradiol ، مستقلب من 17β-استراديول مع الحد الأدنى من نشاط الاستروجين ، يمتلك تأثيرات مضادة للأكسدة ويتفاعل مع الحمض النووي لتشكيل مقاربات مستقرة ويمارس السمية الجينية
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Cas No.: 362-05-0
Sample solution is provided at 25 µL, 10mM.
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).
| Cas No. | 362-05-0 | SDF | |
| المرادفات | 2-HE2,NSC 61711 | ||
| 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 | ||
| Formula | C18H24O3 | M.Wt | 288.4 |
| الذوبان | DMF: 20 mg/ml; DMSO: 25 mg/ml; Ethanol: 25 mg/ml; Ethanol:PBS (pH 7.2) (1:3): 0.25 mg/ml | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4674 mL | 17.337 mL | 34.6741 mL |
| 5 mM | 0.6935 mL | 3.4674 mL | 6.9348 mL |
| 10 mM | 0.3467 mL | 1.7337 mL | 3.4674 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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- Purity: >95.00%
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Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)
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