Naftopidil dihydrochloride

Names

[ Name ]:
Naftopidil dihydrochloride

[Synonym ]:
Avishot
Naftopidil DiHCl
KT-611 dihydrochloride
Naftopidildihydrochloride
RS-1-[4-(2-Methoxyphenyl)-1-piperazinyl]-3-(1-naphthoxy)-2-propanol
flivas dihydrochloride
1-(2-Methoxyphenyl)-4-[3-(naphth-1-yloxy)-2-hydroxypropyl]-piperazine
4-(2-Methoxyphenyl)-a-[(1-naphthalenyloxy)methyl]-1-piperazineethanol
S1387_Selleck
Flivas
1-[4-(2-Methoxyphenyl)-1-piperazinyl]-3-(1-naphthyloxy)-2-propanol
1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-(naphthalen-1-yloxy)propan-2-ol
1-Piperazineethanol, 4-(2-methoxyphenyl)-α-[(1-naphthalenyloxy)methyl]-
Naftopidil
1-[4-(2-Methoxyphenyl)piperazin-1-yl]-3-(1-naphthyloxy)propan-2-ol

Biological Activity

[Description]:

Naftopidil dihydrochloride (KT-611 dihydrochloride) is a selective alpha1-adrenoceptor antagonist, with antiproliferative effects. Naftopidil dihydrochloride can be used for the research of prostate hyperplasia[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

[Target]

α1-adrenoceptor[1]

[In Vitro]

Naftopidil dihydrochloride suppresses human prostate tumor growth by altering interactions between tumor cells and stroma[1]. Naftopidil dihydrochloride (10 μM for PCa cells; 0.1-10 Μm for PrSC) shows growth inhibitory effects on PrSC and PCa cells[1]. Naftopidil dihydrochloride (50 μM for E9 cells, 25 μM for PrSC; 48 hours) increased the level of cell-cycle regulatory protein p27 in E9 cells, but not PrSC[1]. Cell Proliferation Assay[1] Cell Line: PCa cells, PrSC Concentration: 10 μM (PCa cells); 0.1 μM, 1 μM, 10 μM (PrSC) Incubation Time: 3 days Result: Exhibited growth inhibitory effects on PCa cells, PrSC in dose-dependent manners. Western Blot Analysis[1] Cell Line: PCa cells, PrSC Concentration: 50 μM (E9 cells), 25 μM (PrSC) Incubation Time: 48 hours Result: Increased the level of cell-cycle regulatory protein p27 in E9 cells, but not PrSC.

[In Vivo]

Naftopidil dihydrochloride (10 mg/kg; p.o; daily, for 28 days) decreases microvessel density (MVD) in E9 + PrSC tumors mice model[1]. Male athymic mice(7-8 weeks), with E9 + PrSC xenograft [1] Animal Model: Male athymic mice(7-8 weeks), with E9 + PrSC xenograft [1] Dosage: 10 mg/kg Administration: Oral administration, daily, for 28 days Result: Decrease tumor weights.

[References]

[1]. 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.

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
602.8±55.0 °C at 760 mmHg

[ Melting Point ]:
212-213°

[ Molecular Formula ]:
C₂₄H₃₀Cl₂N₂O₃

[ Molecular Weight ]:
392.491

[ Flash Point ]:
318.3±31.5 °C

[ Exact Mass ]:
392.209991

[ PSA ]:
45.17000

[ LogP ]:
4.81

[ Vapour Pressure ]:
0.0±1.8 mmHg at 25°C

[ Index of Refraction ]:
1.619

[ Storage condition ]:
-20℃

[ Water Solubility ]:
methanol: >10 mg/mL

Safety Information

[ WGK Germany ]:
3

[ RTECS ]:
TL9336500

Related Compounds

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