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Purity: ≥98%
Naftopidil 2HCl (BM-15275; KT-611; BM15275; KT611; Flivas), the dihydrochloride salt of Naftopidil, is a potent and selective α1-adrenergic receptor antagonist with antihypertensive effects. It has a Kis of 3.7 nM, 20 nM, and 1.2 nM for α1a, α1b, and α1d adrenergic receptor inhibition, respectively. Benign prostatic hyperplasia, or BPH, may now be treated with naftopidil. When compared to the alpha1a- and alpha1b-adrenoceptor subtypes, naptopidil has a selectivity for the alpha1d-adrenoceptor that is roughly 3- and 17-fold higher, respectively. In human prostate cancer cell lines that are both androgen-sensitive and -insensitive, naftopidil inhibits the growth of the cells.
| Targets |
Alpha-1A adrenergic receptor ( Ki = 3.7 nM ); Alpha-1B adrenergic receptor ( Ki = 20 nM ); Alpha-1D adrenergic receptor ( Ki = 1.2 )
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| Cell Assay |
Flow cytometry is used to analyze cell cycles. After treating the cells for 24 hours with either 20 μM Naftopidil (LNCaP), 40 μM Naftopidil (PC-3), or vehicle (0.1% DMSO), the cells are trypsinized, once again cleaned with phosphate-buffer saline (PBS), fixed in 70% ethanol, and kept at 4 °C for the purpose of cell cycle analysis. After fixed cells are rinsed with PBS, they are incubated for 30 minutes at 37 °C in PBS containing 20 μg/mL RNaseA and 0.3% NP-40. Afterwards, they are stained for 30 minutes at 4 홈 in the dark with 50 μg/mL propidium iodide (PI). One FACS Caliburflow cytometer is used to analyze the DNA content of one million stained cells. Using Cell Quest software, the fractions of cells in the G0/G1, S, and G2/M phases are computed.
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| References |
| Molecular Formula |
C24H30CL2N2O3
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| Molecular Weight |
465.41
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| Exact Mass |
464.16
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| Elemental Analysis |
C, 61.94; H, 6.50; Cl, 15.23; N, 6.02; O, 10.31
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| CAS # |
57149-08-3
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| Related CAS # |
Naftopidil; 57149-07-2; Naftopidil hydrochloride; 1164469-60-6
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| Appearance |
Solid powder
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| SMILES |
COC1=CC=CC=C1N2CCN(CC2)CC(COC3=CC=CC4=CC=CC=C43)O.Cl.Cl
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| InChi Key |
HZVCEQMJXMUXJF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H28N2O3.2ClH/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;2*1H
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| Chemical Name |
1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol;dihydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1486 mL | 10.7432 mL | 21.4864 mL | |
| 5 mM | 0.4297 mL | 2.1486 mL | 4.2973 mL | |
| 10 mM | 0.2149 mL | 1.0743 mL | 2.1486 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.
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.
(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.
| 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 |
Products are for research use only; We do not sell to patients
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