|雌酮硫酸酯哌嗪|CsnPharm

CAS No.: 7280-37-7

Estropipate/雌酮硫酸酯哌嗪 Catalog No. CSN10938

Synonyms: Piperazine estrone sulfate;Estrone sulfate piperazine salt;Harmogen

Estropipate, deriving from estrogen, is used to treat symptoms of menopause and to prevent osteoporosis.

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生物活性

描述Estropipate (EPP) is a form of estrogen, used to treat symptoms of menopause, also used to prevent osteoporosis. EPP and its free-base form (i.e., estrone sulfate) showed a potent and high degree of selectivity in inhibiting the OATP1B1-mediated transport of rosuvastatin with an IC50 value averaging 0.05 ± 0.01 and 0.12 ± 0.07 μM for human and cynomolgus monkey OATP1B1, respectively, whereas weak inhibition was observed for human and monkey OATP1B3, OATP2B1, sodium-taurocholate cotransporting polypeptide (NTCP), organic anion transporter 2, and organic cation transporter 1 with IC50 values ranging from 8.6 to 64.0 μM^[2]. Estropipate (estrone-3-sulfate stabilized with piperazine) was the most selective OATP1B1 inhibitor (IC50 = 0.06 mM vs. 19.3 mM for OATP1B3)^[3]. All the estrogens exerted stimulatory effects in the postmenopausal specimens that were comparable to those observed in the premenopausal proliferative-phase specimens. Estropipate, subcutaneous estradiol, and conjugated estrogens had some hyperphysiologic effects^[4].
参考文献

[1] Bagdade JD, Subbaiah PV. Effects of estropipate treatment on plasma lipids and lipoprotein lipid composition in postmenopausal women. J Clin Endocrinol Metab. 1991 Feb;72(2):283-6.
[2] Zhang Y, Panfen E, Fancher M, Sinz M, Marathe P, Shen H. Dissecting the Contribution of OATP1B1 to Hepatic Uptake of Statins Using the OATP1B1 Selective Inhibitor Estropipate. Mol Pharm. 2019 Jun 3;16(6):2342-2353
[3] Gui C, Obaidat A, Chaguturu R, Hagenbuch B. Development of a cell-based high-throughput assay to screen for inhibitors of organic anion transporting polypeptides 1B1 and 1B3. Curr Chem Genomics. 2010 Mar 1;4:1-8
[4] Whitehead MI, Townsend PT, Pryse-Davies J, Ryder TA, King RJ. Effects of estrogens and progestins on the biochemistry and morphology of the postmenopausal endometrium. N Engl J Med. 1981 Dec 31;305(27):1599-605

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2906 mL
- 11.4531 mL
- 22.9061 mL
- 5 mM
- 0.4581 mL
- 2.2906 mL
- 4.5812 mL
- 10 mM
- 0.2291 mL
- 1.1453 mL
- 2.2906 mL

技术信息

CAS号

7280-37-7

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H32N2O5S

运输

蓝冰

分子量

436.56

别名

Piperazine estrone sulfate;Estrone sulfate piperazine salt;Harmogen;Ogen;雌酮硫酸酯哌嗪

溶解度

DMSO	215.0 mg/mL (492.5 mM)
Water	insoluble

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Estropipate/雌酮硫酸酯哌嗪 Catalog No. CSN10938

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