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Tesmilifene

Antagonist of intracellular histamine
 
BML-EI401-0010 10 mg 76.00 USD
 
BML-EI401-0050 50 mg 302.00 USD
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Tesmilifene is a novel agent that augments cytotoxicity of various chemotherapeutic agents both in vitro and in vivo. It binds selectively to the high-affinity microsomal antiestrogen binding site (Ki=50nm) but has no affinity for estrogen receptors. Inhibits concanavalin-A-induced histamine release in mast cells and acts as a novel antagonist of intracellular histamine.

Product Specification

Alternative Name:DPPE, N,N-Diethyl-2-[4-(phenylmethyl)phenoxy]ethanamine . HCl
 
Formula:C19H25NO . HCl
 
MW:283.4 . 36.5
 
CAS:92981-78-7
 
MI:14: 9178
 
Purity:≥99% (TLC)
 
Appearance:Off-white solid.
 
MeltingPoint:150-152°C
 
Solubility:Soluble in water (4mg/ml) or DMSO (3mg/ml).
 
Shipping:Ambient
 
Long Term Storage:Ambient
 
Use/Stability:Stable for at least 1 year after receipt when stored at -20°C.Stock solutions are stable for up to 3 months at -20°C.
 
BML-EI401 structure
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BML-EI401 structure

Product Literature References

Enhancement of cytotoxicity of natural product drugs against multidrug resistant variant cell lines of human head and neck squamous cell carcinoma and breast carcinoma by tesmilifene.: P. J. Ferguson, et al.; Cancer Lett. 274, 279 (2009), Abstract;
Phase III study of N,N-diethyl-2-[4-(phenylmethyl) phenoxy]ethanamine (BMS-217380-01) combined with doxorubicin versus doxorubicin alone in metastatic/recurrent breast cancer: National Cancer Institute of Canada Clinical Trials Group St: L. Reyno, et al.; J. Clin. Oncol. 22, 269 (2004), Abstract;
Synergy between tamoxifen and cisplatin in human melanoma cells is dependent on the presence of antiestrogen-binding sites.: J.A. Jones, et al.; Cancer Res. 57, 2657 (1997), Abstract;
Influence of DPPE on histamine release from isolated rat mast cells.: N. Grosman; Agents Actions 41, 1 (1994), Abstract;
Histamine is an intracellular messenger mediating platelet aggregation.: S.P: Saxena, et al.; Science 243, 1596 (1989), Abstract;

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