2-Hydroxyestradiol (Synonyms: 2-HE2,NSC 61711) |
| Catalog No.GC13460 |
El 2-hidroxiestradiol, un metabolito del 17β-estradiol con actividad estrogénica mÍnima, posee efectos antioxidantes y reacciona con el ADN para formar aductos estables y ejerce genotoxicidad.
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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 | |
| Sinónimos | 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 |
| Solubility | 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 DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Quality Control & SDS
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- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)
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