Naftopidil (dihydrochloride)

Naftopidil dihydrochloride (KT-611 dihydrochloride) is a selective alpha1-adrenoceptor antagonist, with K_is of 3.7 nM, 20 nM and 1.2 nM for the cloned human α_1a-, α_1b- and α_1d-adrenoceptor subtypes, respectively. Naftopidil dihydrochloride has antiproliferative effects. Naftopidil dihydrochloride can be used for the research of prostate hyperplasia^[1][2]. IC50 & Target: α1-adrenoceptor^[1] 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].