1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor
  3. Naftopidil dihydrochloride

Naftopidil dihydrochloride  (Synonyms: KT-611 dihydrochloride; BM-15275 dihydrochloride)

Cat. No.: HY-B0391A
Handling Instructions

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.

For research use only. We do not sell to patients.

Naftopidil dihydrochloride Chemical Structure

Naftopidil dihydrochloride Chemical Structure

CAS No. : 57149-08-3

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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[1][2].

IC50 & Target[1]

Alpha-1A adrenergic receptor

3.7 nM (Ki)

Alpha-1B adrenergic receptor

20 nM (Ki)

Alpha-1D adrenergic receptor

1.2 (Ki)

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[2]

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 and PrSC in dose-dependent manners.

Western Blot Analysis[2]

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[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male athymic mice(7-8 weeks), with E9+PrSC xenograft[2]
Dosage: 10 mg/kg
Administration: Oral administration, daily, for 28 days
Result: Decreased tumor weights.
Clinical Trial
Molecular Weight

465.41

Formula

C24H30Cl2N2O3

CAS No.
SMILES

[H]Cl.[H]Cl.OC(CN1CCN(C(C=CC=C2)=C2OC)CC1)COC3=CC=CC4=CC=CC=C34

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Naftopidil dihydrochloride
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HY-B0391A
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