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Purity: ≥98%
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.
| Targets |
Alpha-1A adrenergic receptor ( Ki = 3.7 nM ); Alpha-1B adrenergic receptor ( Ki = 20 nM ); Alpha-1D adrenergic receptor ( Ki = 1.2 nM )
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| ln Vitro |
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| ln Vivo |
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| 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. |
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| Animal Protocol |
Male athymic mice (7-8 weeks), with E9+PrSC xenograft
10 mg/kg Oral administration, daily, for 28 days |
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| References |
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| Additional Infomation |
Naftopidil is a member of piperazines.
Naftopidil has been investigated for the treatment of Disorder of Urinary Stent. |
| Molecular Formula |
C24H28N2O3
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| Molecular Weight |
392.49
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| Exact Mass |
392.209
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| Elemental Analysis |
C, 73.44; H, 7.19; N, 7.14; O, 12.23
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| CAS # |
57149-07-2
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| Related CAS # |
Naftopidil dihydrochloride; 57149-08-3; Naftopidil hydrochloride; 1164469-60-6; Naftopidil-d5; 2747918-58-5
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| PubChem CID |
4418
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
602.8±55.0 °C at 760 mmHg
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| Melting Point |
127 °C
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| Flash Point |
318.3±31.5 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.619
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| LogP |
4.81
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
29
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| Complexity |
483
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O([H])C([H])(C([H])([H])OC1=C([H])C([H])=C([H])C2=C([H])C([H])=C([H])C([H])=C12)C([H])([H])N1C([H])([H])C([H])([H])N(C2=C([H])C([H])=C([H])C([H])=C2OC([H])([H])[H])C([H])([H])C1([H])[H]
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| InChi Key |
HRRBJVNMSRJFHQ-UHFFFAOYSA-N
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| 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
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| Chemical Name |
1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol
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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) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.37 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (6.37 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.37 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| 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.
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 |
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