D2571
DPPE hydrochloride
≥98% (HPLC)
别名:
BMS-217380-01, N,N-Diethyl-2-[4-(phenylmethyl) phenoxy]ethanamine hydrochloride, Tesmilifene hydrochloride, YMB1002, [2-(4-Benzyl-phenoxy)-ethyl]-diethyl-amine hydrochloride
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关于此项目
经验公式（希尔记法）:
C19H25NO·HCl
化学文摘社编号:
分子量:
319.87
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
51111800
MDL number:
产品名称
DPPE hydrochloride, ≥98% (HPLC)
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
SMILES string
Cl.CCN(CC)CCOc1ccc(Cc2ccccc2)cc1
InChI key
TXLHNFOLHRXMAU-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white
solubility
H2O: 16 mg/mL
storage temp.
2-8°C
Quality Level
Features and Benefits
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.
Biochem/physiol Actions
DPPE is a potent, selective ligand of the microsomal anti-estrogen binding site.
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.
存储类别
11 - Combustible Solids
wgk
nwg
flash_point_f
Not applicable
flash_point_c
Not applicable
Fred Y Xu et al.
Proceedings of the Western Pharmacology Society, 50, 61-63 (2008-07-09)
N,N-Diethyl-2-[4-(phenylmethyl)phenoxy]ethanamine (DPPE, tesmilifene), a potent chemopotentiating drug currently in Phase III clinical trials of metastatic breast cancer, increases cytotoxicity of anthracyclines and taxanes in a variety of multi-drug resistance expressing (MDR+) tumor cell lines in vitro; inhibits binding of histamine
W C Cramer et al.
General pharmacology, 30(2), 195-200 (1998-03-21)
1. We have investigated the ability of several compounds to diminish both infarct area and volume induced by middle cerebral artery occlusion in the mouse. 2. Lifarizine, ipsapirone and N,N-diethyl-2-[4-(phenylmethyl)phenoxy]ethanamine HCl (DPPE) all reduced both infarct area and volume. Ifenprodil
N Szincsák et al.
Melanoma research, 12(3), 231-240 (2002-07-26)
Histamine is produced by many cells expressing histidine decarboxylase (HDC), the enzyme responsible for the synthesis of histamine. Since melanoma cells and tissue contain relatively large amounts of histamine, the functional significance of histamine was examined using specific antihistamines in
Peter J Ferguson et al.
Cancer letters, 274(2), 279-289 (2008-11-07)
N,N-diethyl-2-[4-(phenylmethyl)phenoxyl]ethanamine (tesmilifene), a tamoxifen derivative with antihistamine activity, greatly enhanced the survival of doxorubicin-treated, advanced stage breast cancer patients in a phase III trial. However, the molecular basis of tesmilifene action is not firmly established. The effects of tesmilifene on
L J Brandes et al.
Breast cancer research and treatment, 49(1), 61-68 (1998-08-07)
N,N-diethyl-2-[4-(phenylmethyl)phenoxy] ethanamine.HCl (DPPE) is a diphenylmethane analog of tamoxifen that antagonizes the intracellular binding of histamine to growth-regulatory sites, a proportion of which represents P450 enzymes, in microsomes and nuclei. We previously reported increased response rates and decreased myelotoxicity in
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