Cat. No.: HY-B0391

Naftopidil

(Synonyms: KT-611; BM-15275)

1 Cited Publications

Customer Review

Based on 1 publication(s) in Google Scholar

Naftopidil (KT-611) is 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 has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia.

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

Purity: 98.14%
CAS No.: 57149-07-2
Formula: C₂₄H₂₈N₂O₃
Molecular Weight:392.49

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Naftopidil Chemical Structure

CAS No.: 57149-07-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

Alpha-1A adrenergic receptor

3.7 nM (Ki)

Alpha-1B adrenergic receptor

20 nM (Ki)

Alpha-1D adrenergic receptor

1.2 nM (Ki)

All Adrenergic Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
786-0	IC₅₀	13.3 μM Compound: 1	Antiproliferative activity against human 786-O cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human 786-O cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31759851]
DU-145	IC₅₀	>50 μM Compound: 1	Cytotoxicity against human DU145 cells after 48 hrs by WST-8 assay Cytotoxicity against human DU145 cells after 48 hrs by WST-8 assay	[PMID: 25874333]
DU-145	IC₅₀	21.1 μM Compound: 1	Antiproliferative activity against human DU145 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human DU145 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31759851]
DU-145	IC₅₀	22.2 μM Compound: 1	Cytotoxicity against human DU145 cells Cytotoxicity against human DU145 cells	[PMID: 25874333]
DU-145	IC₅₀	34.58 μM Compound: Naftopidil	Cytotoxicity against human DU145 cells assessed as inhibition of cell viability after 24 hrs by CCK-8 assay Cytotoxicity against human DU145 cells assessed as inhibition of cell viability after 24 hrs by CCK-8 assay	[PMID: 25488843]
DU-145	IC₅₀	34.58 μM Compound: Naftopidil	Cytotoxicity against human DU145 cells assessed as growth inhibition after 24 hrs by CCK8 assay Cytotoxicity against human DU145 cells assessed as growth inhibition after 24 hrs by CCK8 assay	[PMID: 29615343]
DU-145	IC₅₀	34.58 μM Compound: Naftopidil	Antiproliferative activity against human DU145 cells after 24 hrs by CCK-8 assay Antiproliferative activity against human DU145 cells after 24 hrs by CCK-8 assay	[PMID: 30482547]
HEK293	IC₅₀	47.3 μM Compound: 1	Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31759851]
KK-47 cell line	IC₅₀	19 μM Compound: 1	Antiproliferative activity against human KK47 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human KK47 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31759851]
LNCaP	IC₅₀	>50 μM Compound: 1	Cytotoxicity against human LNCAP cells after 48 hrs by WST-8 assay Cytotoxicity against human LNCAP cells after 48 hrs by WST-8 assay	[PMID: 25874333]
LNCaP	IC₅₀	22.36 μM Compound: Naftopidil	Cytotoxicity against human LNCAP cells assessed as inhibition of cell viability after 24 hrs by CCK-8 assay Cytotoxicity against human LNCAP cells assessed as inhibition of cell viability after 24 hrs by CCK-8 assay	[PMID: 25488843]
LNCaP	IC₅₀	22.36 μM Compound: Naftopidil	Cytotoxicity against human LNCAP cells assessed as growth inhibition after 24 hrs by CCK8 assay Cytotoxicity against human LNCAP cells assessed as growth inhibition after 24 hrs by CCK8 assay	[PMID: 29615343]
LNCaP	IC₅₀	22.36 μM Compound: Naftopidil	Antiproliferative activity against human LNCAP cells after 24 hrs by CCK-8 assay Antiproliferative activity against human LNCAP cells after 24 hrs by CCK-8 assay	[PMID: 30482547]
PC-3	IC₅₀	>50 μM Compound: 1	Cytotoxicity against human PC3 cells after 48 hrs by WST-8 assay Cytotoxicity against human PC3 cells after 48 hrs by WST-8 assay	[PMID: 25874333]
PC-3	IC₅₀	31.2 μM Compound: 1	Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31759851]
PC-3	IC₅₀	33.2 μM Compound: 1	Cytotoxicity against human PC3 cells Cytotoxicity against human PC3 cells	[PMID: 25874333]
PC-3	IC₅₀	42.1 μM Compound: Naftopidil	Cytotoxicity against human PC3 cells assessed as inhibition of cell viability after 24 hrs by CCK-8 assay Cytotoxicity against human PC3 cells assessed as inhibition of cell viability after 24 hrs by CCK-8 assay	[PMID: 25488843]
PC-3	IC₅₀	42.1 μM Compound: Naftopidil	Cytotoxicity against human PC3 cells assessed as growth inhibition after 24 hrs by CCK8 assay Cytotoxicity against human PC3 cells assessed as growth inhibition after 24 hrs by CCK8 assay	[PMID: 29615343]
PC-3	IC₅₀	42.1 μM Compound: Naftopidil	Antiproliferative activity against human PC3 cells after 24 hrs by CCK-8 assay Antiproliferative activity against human PC3 cells after 24 hrs by CCK-8 assay	[PMID: 30482547]
PNT1A	IC₅₀	27 μM Compound: 1	Cytotoxicity against human PNT1A cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human PNT1A cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31759851]
RWPE-1	IC₅₀	>50 μM Compound: Naftopidil	Cytotoxicity against human RWPE1 cells assessed as inhibition of cell viability after 24 hrs by CCK-8 assay Cytotoxicity against human RWPE1 cells assessed as inhibition of cell viability after 24 hrs by CCK-8 assay	[PMID: 25488843]
RWPE-1	IC₅₀	>50 μM Compound: Naftopidil	Antiproliferative activity against human RWPE1 cells after 24 hrs by CCK-8 assay Antiproliferative activity against human RWPE1 cells after 24 hrs by CCK-8 assay	[PMID: 30482547]
T-24	IC₅₀	18.5 μM Compound: 1	Antiproliferative activity against human T24 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human T24 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31759851]

In Vitro

Naftopidil suppresses human prostate tumor growth by altering interactions between tumor cells and stroma^[2].
Naftopidil (10 μM for PCa cells, 0.1-10 μM for PrSC; 3 days) shows growth inhibitory effects on PCa cells and PrSC^[2].
Naftopidil (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 (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.

Chemical Information

CAS No. 57149-07-2
Appearance Solid
Molecular Weight 392.49
Formula C₂₄H₂₈N₂O₃
Color White to off-white
SMILES

OC(CN1CCN(C(C=CC=C2)=C2OC)CC1)COC3=CC=CC4=CC=CC=C34
Synonyms

KT-611; BM-15275
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Journal Impact Factor

Phytomedicine

Stachydrine hydrochloride reduces NOX2 activity to suppress oxidative stress levels to improve cardiac insufficiency. [Abstract]

2025 May:140:156621. PMID: 40088741

Solvent & Solubility

In Vitro:

DMSO : 33.33 mg/mL (84.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5478 mL

12.7392 mL

25.4784 mL

5 mM

0.5096 mL

2.5478 mL

5.0957 mL

10 mM

0.2548 mL

1.2739 mL

2.5478 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (6.37 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5478 mL	12.7392 mL	25.4784 mL	63.6959 mL
	5 mM	0.5096 mL	2.5478 mL	5.0957 mL	12.7392 mL
	10 mM	0.2548 mL	1.2739 mL	2.5478 mL	6.3696 mL
	15 mM	0.1699 mL	0.8493 mL	1.6986 mL	4.2464 mL
	20 mM	0.1274 mL	0.6370 mL	1.2739 mL	3.1848 mL
	25 mM	0.1019 mL	0.5096 mL	1.0191 mL	2.5478 mL
	30 mM	0.0849 mL	0.4246 mL	0.8493 mL	2.1232 mL
	40 mM	0.0637 mL	0.3185 mL	0.6370 mL	1.5924 mL
	50 mM	0.0510 mL	0.2548 mL	0.5096 mL	1.2739 mL
	60 mM	0.0425 mL	0.2123 mL	0.4246 mL	1.0616 mL
	80 mM	0.0318 mL	0.1592 mL	0.3185 mL	0.7962 mL

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Naftopidil

GPCR/G Protein Compound Library

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Publications Citing Use of MedChemExpress (MCE) Naftopidil

All Adrenergic Receptor Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Naftopidil Related Classifications

Cat. No.: HY-B0391