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化驗
≥98% (HPLC)
形狀
powder
顏色
white
溶解度
H2O: 16 mg/mL
儲存溫度
2-8°C
SMILES 字串
Cl.CCN(CC)CCOc1ccc(Cc2ccccc2)cc1
InChI
1S/C19H25NO.ClH/c1-3-20(4-2)14-15-21-19-12-10-18(11-13-19)16-17-8-6-5-7-9-17;/h5-13H,3-4,14-16H2,1-2H3;1H
InChI 密鑰
TXLHNFOLHRXMAU-UHFFFAOYSA-N
生化/生理作用
DPPE is a potent, selective ligand of the microsomal anti-estrogen binding site. DPPE is a tamoxifen derivataive that binds with high affinity to the anti-estrogen binding site, but unlike tamoxifen, does not bind to the estrogen receptor. DPPE sensitizes MDR tumor cells to chemotherapy and also inhibits histamine binding at the intracellular histamine site.
特點和優勢
This compound is featured on the Nuclear Receptors (Steroids) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
nwg
閃點(°F)
Not applicable
閃點(°C)
Not applicable
Japanese journal of cancer research : Gann, 88(10), 1003-1008 (1998-01-01)
In 5-day incubation of an estrogen receptor-negative human ovarian cancer cell line (KF) with N,N-diethyl-2-[4-(phenylmethyl)phenoxy]ethanamine-HCl (DPPE), the concentration of DPPE required for 50% inhibition of KF cell proliferation (IC50) was 1.7 microM. The IC50 of DPPE for inhibition of protein
The Journal of pharmacy and pharmacology, 62(8), 1084-1088 (2010-07-29)
It has been reported that docetaxel is a P-glycoprotein substrate and is metabolized via the cytochrome P450 (CYP) 3A subfamily in rats. Tesmilifene is a substrate of the CYP3A subfamily and is an inhibitor of P-glycoprotein. Thus, the effects of
Bioorganic & medicinal chemistry, 8(8), 2007-2016 (2000-09-26)
New compounds have been synthesized based on the structure of the anti-tumoral drug tamoxifen and its diphenylmethane derivative, N,N-diethyl-2-[(4-phenyl-methyl)-phenoxy]-ethanamine, HCl (DPPE). These new compounds have no affinity for the estrogen receptor (ER) and bind with various affinity to the anti-estrogen
Current medicinal chemistry, 9(14), 1349-1357 (2002-07-23)
Endogenous histamine regulates the haematopoiesis. Histidine decarboxylase inhibitor decreases the histamine level, and its intracellular antagonist decreases the histamine effect. The effect of histidine decarboxylase inhibitor (alpha-fluoromethyl histidine) and the intracellular antagonist of histamine [N'N-diethyl-2-4-(phenylmethyl) phenoxyethan-amine-HCl] was investigated on the
Journal of clinical oncology : official journal of the American Society of Clinical Oncology, 22(2), 269-276 (2004-01-15)
N,N-diethyl-2-[4-(phenylmethyl)phenoxy]ethanamine (DPPE; tesmilifene) is a novel agent that augments chemotherapy cytotoxicity in vitro and in vivo. A phase II trial combining DPPE and doxorubicin (DOX) in metastatic breast carcinoma showed increased response over that expected with DOX. We report a
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