Naftopidil

Alias: KT-611; BM-15275; KT611; BM 15275; KT 611; BM15275; KT611; Flivas

Cat No.:V1113 Purity: ≥98%

COA Product Data Instructions for use SDS

Naftopidil (BM-15275; KT611; BM15275; KT611; Flivas) is a selective α1-adrenergic receptor antagonist that has been approved for the treatment of BPH-benign prostatic hyperplasia.

Naftopidil Chemical Structure CAS No.: 57149-07-2
Product category: Adrenergic Receptor

This product is for research use only, not for human use. We do not sell to patients.

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Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

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Nature 597, 119–125 (2021)

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Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

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Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

NMR

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information

Product Description

Naftopidil (BM-15275; KT611; BM15275; KT611; Flivas) is a selective α1-adrenergic receptor antagonist that has been approved for the treatment of BPH-benign prostatic hyperplasia. Naftopidil possesses a Kis of 3.7 nM, 20 nM, and 1.2 nM for α1a, α1b, and α1d adrenoceptor inhibition, respectively.

Biological Activity I Assay Protocols (From Reference)

Targets

Alpha-1A adrenergic receptor ( Ki = 3.7 nM ); Alpha-1B adrenergic receptor ( Ki = 20 nM ); Alpha-1D adrenergic receptor ( Ki = 1.2 nM )

ln Vitro

In vitro activity: Naftopidil inhibits the growth of human prostate tumors by changing the way that tumor cells and stroma interact[2].
Naftopidil (10 μM for PCa cells, 0.1-10 μM for PrSC; 3 days) exhibits growth-inhibiting properties on PCa cells and PrSC[2].
Naftopidil (50 μM for E9 cells, 25 μM for PrSC; 48 hours) raises the expression of the cell-cycle regulatory protein p27, but not of PrSC in E9 cells[2].

ln Vivo

Naftopidil (10 mg/kg; p.o; daily; for 28 days) reduces microvessel density (MVD) in the mouse model of E9+PrSC tumors[2].

Cell Assay

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.

Animal Protocol

Male athymic mice (7-8 weeks), with E9+PrSC xenograft
10 mg/kg
Oral administration, daily, for 28 days

References

[1]. 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.

[2]. 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.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C24H28N2O3

Molecular Weight

392.49

Exact Mass

392.21

Elemental Analysis

C, 73.44; H, 7.19; N, 7.14; O, 12.23

CAS #

57149-07-2

Related CAS #

Naftopidil dihydrochloride; 57149-08-3; Naftopidil hydrochloride; 1164469-60-6; Naftopidil-d5; 2747918-58-5

Appearance

Solid powder

SMILES

COC1=CC=CC=C1N2CCN(CC2)CC(COC3=CC=CC4=CC=CC=C43)O

InChi Key

HRRBJVNMSRJFHQ-UHFFFAOYSA-N

InChi Code

InChI=1S/C24H28N2O3/c1-28-24-11-5-4-10-22(24)26-15-13-25(14-16-26)17-20(27)18-29-23-12-6-8-19-7-2-3-9-21(19)23/h2-12,20,27H,13-18H2,1H3

Chemical Name

1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol

Synonyms

KT-611; BM-15275; KT611; BM 15275; KT 611; BM15275; KT611; Flivas

HS Tariff Code

2934.99.9001

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: 33.3~79 mg/mL (84.9~201.3 mM)

Water: <1 mg/mL

Ethanol: <1 mg/mL

Preparing Stock Solutions		1 mg	5 mg	10 mg
	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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

Calculate Reset

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculate Reset

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

Calculate Reset

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT00967772	Completed	Drug: Naftopidil	Healthy	Dong-A ST Co., Ltd.	September 2009	Phase 1
NCT01959074	Completed	Drug: Naftopidil Drug: Placebo for Naftopidil	Disorder of Urinary Stent	Seoul National University Hospital	May 2014	Phase 3
NCT01952314	Completed	Drug: Naftopidil 75mg Drug: Placebo for Naftopidil	Ureter Stones	Seoul National University Hospital	May 2014	Phase 3
NCT01922375	Completed	Drug: Naftopidil	Lower Urinary Tract Symptoms Associated With Benign Prostatic Hyperplasia	Dong-A Pharmaceutical Co., Ltd.	December 2011	Phase 4
NCT02034604	Completed	Drug: Naftofidil Drug: Tamsulosin	Neurogenic Lower Urinary Tract Dysfunction	Samsung Medical Center	December 2013	Phase 4