Estropipate

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Chemical Structure| 7280-37-7 同义名 : Piperazine estrone sulfate; Estrone sulfate piperazine salt; Ogen; Harmogen; Pipestrone
CAS号 : 7280-37-7
货号 : A340804
分子式 : C22H32N2O5S
纯度 : 96%
分子量 : 436.56
MDL号 : MFCD00867399
存储条件：

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(240.51 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.29mL

0.46mL

0.23mL

11.45mL

2.29mL

1.15mL

22.91mL

4.58mL

2.29mL
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