Estradiol 3-sulfamate (Synonyms: 雌二醇 3-氨基磺酸; BLE 00084; E2MATE; ES-J 995)
目录号: PL08399 纯度: ≥99%
Estradiol 3-sulfamate (BLE 00084; E2MATE; ES-J 995) 是一种长效和有口服活性的类固醇硫酸酯酶 (steroid sulfatase) 抑制剂;抑制雌酮硫酸酯酶的 IC50 值为251 nM,Ki 值为133 nM。
CAS No. :172377-52-5
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中文名称
Estradiol 3-sulfamate
中文别名
雌二醇 3-氨基磺酸
英文名称
Estradiol 3-sulfamate
英文别名
Estradiol 3-sulfamate;BLE 00084;E2MATE;ES-J 995;[(8R,9S,13S,14S,17S)-17-Hydroxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthre
Cas No.
172377-52-5
分子式
C18H25NO4S
分子量
351.46
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Estradiol 3-sulfamate (BLE 00084; E2MATE; ES-J 995) 是一种长效和有口服活性的类固醇硫酸酯酶 (steroid sulfatase) 抑制剂;抑制雌酮硫酸酯酶的 IC50 值为251 nM,Ki 值为133 nM。
生物活性
Estradiol 3-sulfamate (BLE 00084; E2MATE; ES-J 995) is a potent, long-acting, and orally active steroid sulfatase inhibitor; inhibits estrone sulfatase with an IC 50 of 251 nM and a K i of 133 nM.
性状
Solid
IC50 & Target[1][2]
IC50: 251 nM (estrone sulfatase)
Ki: 133 nM (estrone sulfatase)
体外研究(In Vitro)
Introduction of a fluoro, chloro, or bromo moiety at the C-2 position of EMATE and Estradiol 3-sulfamate and that of a fluoro moiety at the C-4 position of the parent sulfamates markedly increase the estrone sulfatase inhibitory activity. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Estradiol 3-sulfamate is readily transformed and absorbed in the gut into its oxidative metabolite, EMATE, and both compounds have already been shown to be potent, long-acting, and orally active STS inhibitors. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Numazawa M, et al. Inhibition of estrone sulfatase by aromatase inhibitor-based estrogen 3-sulfamates. Steroids. 2006 May;71(5):371-9.
[2]. Pohl O, et al. Synergistic effects of E2MATE and norethindrone acetate on steroid sulfatase inhibition: a randomized phase I proof-of-principle clinical study in women of reproductive age. Reprod Sci. 2014 Oct;21(10):1256-65.
溶解度数据
In Vitro: DMSO : 62.5 mg/mL (177.83 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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