α-Estradiol
(Synonyms: α-雌二醇; Alfatradiol; Epiestradiol; Epiestrol) 目录号 : GC15975
A weak estrogen with neuroprotective effects
Cas No.:57-91-0
Sample solution is provided at 25 µL, 10mM.
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Alpha-Estradiol is a weak estrogen and a 5α-reductase inhibitor which is used as a topical medication in the treatment of androgenic alopecia.
Alpha-Estradiol (17 alpha-Estradiol) is a 5α-reductase inhibitor, and inhibits testosterone metabolism catalyzed by 5 alpha-reductase[1]. Alpha-Estradiol (17 Alpha-estradiol, 10 μM) attenuates LPS-induced inflammatory markers in both C57BL/6J male and female mouse embryonic fibroblast (MEF) cells, primary pre-adipocytes and differentiated 3T3-L1 adipocytes in an ERα-dependent manner, and such effects are through decreased NFκB-p65 and increased ERα protein expression[2].
Alpha-Estradiol (17-alpha-estradiol, 0.01, 0.1, 1 μg) significantly reduces the percentage of central avascular/total retina area of the mouse pups. Alpha-Estradiol (1 μg) markedly decreasesmalondialdehyde (MDA) levels on postnatal days (PND) 9, 13, and 17 in retinas of hyperoxia-exposed pups. Alpha-Estradiol (1 μg) also decreases the number of NADPH-oxidase-positive cells, NADPH oxidase concentration and activity in retinas of the pups. In the 1.0-μg Alpha-Estradiol-treated pups, VEGF retinal concentrations are high on PND 9 but lower on PND 14 and 17. The best effect in retinas of 1.0-μg Alpha-Estradiol-treated pups is partly reversed by ICI182780 on PND 14 and 17[3].
References:
[1]. Schriefers H, et al. Inhibition of testosterone metabolism by 17-alpha-estradiol in rat liver slices. Arzneimittelforschung. 1991 Nov;41(11):1186-9.
[2]. Santos RS, et al. The effects of 17 alpha-estradiol to inhibit inflammation in vitro. Biol Sex Differ. 2017 Sep 6;8:30.
[3]. Zhang HB, et al. 17-Alpha-estradiol ameliorating oxygen-induced retinopathy in a murine model. Jpn J Ophthalmol. 2012 Jul;56(4):407-15.
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Cell experiment: |
Mouse embryonic fibroblast (MEF) cells are treated for the indicated time with Alpha-Estradiol (17 α-E2) or 17 β-E2 at 10 μM concentration. Inflammation is induced by LPS at a concentration of 10 ng/mL either alone or in combination with the respective estrogen[2]. |
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Animal experiment: |
Newborn mice are randomLy assigned to six groups according to the kind of treatment: room air with vehicle injection (control, group 1), hyperoxia with vehicle injection (control, group 2), hyperoxia with 0.01 μg Alpha-Estradiol injection (group 3), hyperoxia with 0.1 μg Alpha-Estradiol injection (group 4), hyperoxia with 1.0 μg Alpha-Estradiol injection (group 5), and hyperoxia with 1.0 μg Alpha-Estradiol and 10.0 μg ICI182780 injection (antagonist of estrogen receptor α and β) (group 6). The pups receive daily subcutaneous injections of either Alpha-Estradiol in vehicle [dissolved in ethanol and diluted in 0.05 mL/mouse of phosphate-buffered saline (PBS)] or vehicle alone from postnatal days (PND) 7-16. On PND 7, the pups in the hyperoxia and Alpha-Estradiol-treatment groups are exposed to hyperoxia (75 ± 2 % O2) for 5 days (PND 7-12) and then returned to normoxia (room air) for 5 days, along with the nursing mothers, whereas pups in the normoxia group are kept in normoxia from PND 7-17. The pups are humanely euthanized on PND 9, 13 (14), and 17[3]. |
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References: [1]. Schriefers H, et al. Inhibition of testosterone metabolism by 17-alpha-estradiol in rat liver slices. Arzneimittelforschung. 1991 Nov;41(11):1186-9. |
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| Cas No. | 57-91-0 | SDF | |
| 别名 | α-雌二醇; Alfatradiol; Epiestradiol; Epiestrol | ||
| 化学名 | (8R,9S,13S,14S,17R)-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diol | ||
| Canonical SMILES | O[C@H]1[C@]2(C)[C@@H](CC1)[C@H](CCC3=C4C=CC(O)=C3)[C@@H]4CC2 | ||
| 分子式 | C18H24O2 | 分子量 | 272.38 |
| 溶解度 | ≥ 13.15mg/mL in Ethanol | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.6713 mL | 18.3567 mL | 36.7134 mL |
| 5 mM | 0.7343 mL | 3.6713 mL | 7.3427 mL |
| 10 mM | 0.3671 mL | 1.8357 mL | 3.6713 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
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