MedChemExpress - Model Naftopidil dihydrochloride -57149-08-3

Naftopidil dihydrochloride (KT-611 dihydrochloride) is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil dihydrochloride has antiproliferative effects. Naftopidil dihydrochloride can be used for the research of prostate hyperplasia[1][2].

Naftopidil dihydrochloride

MCE China：Naftopidil dihydrochloride

Brand：MedChemExpress (MCE)

Cat. No.HY-B0391A

CAS：57149-08-3

Synonyms：KT-611 dihydrochloride; BM-15275 dihydrochloride

Storage：Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Naftopidil dihydrochloride (KT-611 dihydrochloride) is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil dihydrochloride has antiproliferative effects. Naftopidil dihydrochloride can be used for the research of prostate hyperplasia.

In Vitro：Naftopidil dihydrochloride suppresses human prostate tumor growth by altering interactions between tumor cells and stroma[2]. Naftopidil dihydrochloride (10 μM for PCa cells, 0.1-10 μM for PrSC; 3 days) shows growth inhibitory effects on PCa cells and PrSC[2]. Naftopidil dihydrochloride (50 μM for E9 cells, 25 μM for PrSC; 48 hours) increases the level of cell-cycle regulatory protein p27 in E9 cells, but not PrSC[2].

In Vivo：Naftopidil dihydrochloride (10 mg/kg; p.o; daily; for 28 days) decreases microvessel density (MVD) in E9+PrSC tumors mice model[2].

IC50 & Target：Alpha-1A adrenergic receptor 3.7 nM (Ki) Alpha-1B adrenergic receptor 20 nM (Ki) Alpha-1D adrenergic receptor 1.2 (Ki)

References：

[1]. R Takei, et al. Naftopidil, a novel alpha1-adrenoceptor antagonist, displays selective inhibition of canine prostatic pressure and high affinity binding to cloned human alpha1-adrenoceptors. Jpn J Pharmacol. 1999 Apr;79(4):447-54. [Content Brief]

[2]. Yasuhide Hori, et al. Naftopidil, a selective {alpha}1-adrenoceptor antagonist, suppresses human prostate tumor growth by altering interactions between tumor cells and stroma. Cancer Prev Res (Phila). 2011 Jan;4(1):87-96. [Content Brief]

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MedChemExpress - Model Naftopidil dihydrochloride -57149-08-3

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Naftopidil dihydrochloride