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| 5mg |
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Purity: ≥98%
Naminidil (BMS 234303-01) is a novel and potent cyanoguanidine KATP opener (ATP-Sensitive Potassium Channel Vasodilator). It can be used for the treatment of hair loss.
| Targets |
The target of Naminidil is not explicitly specified with IC₅₀, Ki, or EC₅₀ values in the specified patent. However, it is indicated to act on hair follicles by promoting hair growth, extending the anagen phase of the hair growth cycle, and inhibiting follicular miniaturization, which are consistent with the mechanisms of anti-alopecia agents targeting hair follicle proliferation and survival pathways [1]
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| ln Vitro |
Through potassium (K) channels, nanodil functions [1].
1. Hair follicle organ culture assay: Isolated human scalp hair follicles were cultured in vitro with Naminidil at concentrations of 0.1%, 0.5%, and 1.0% (w/v) for 14 days. The hair follicles treated with 0.5% and 1.0% Naminidil showed a significant increase in hair shaft elongation compared to the vehicle control: 0.5% concentration induced a 35% increase in hair shaft length, and 1.0% concentration induced a 52% increase. Additionally, the anagen phase duration of the cultured follicles was prolonged by 4–6 days in the Naminidil-treated groups, while the vehicle control follicles entered catagen phase earlier [1] 2. Dermal papilla cell (DPC) proliferation assay: Human dermal papilla cells were treated with Naminidil at concentrations of 0.01%, 0.1%, 0.5%, and 1.0% for 72 hours. The 0.1%–1.0% Naminidil concentrations significantly promoted DPC proliferation, with the maximum proliferation rate (168% of the vehicle control) observed at 0.5% concentration. No cytotoxicity was detected even at the highest concentration (1.0%) [1] |
| ln Vivo |
1. Mouse alopecia model (cyclophosphamide-induced): Male C57BL/6 mice were intraperitoneally injected with cyclophosphamide (150 mg/kg) to induce alopecia. Starting 3 days after cyclophosphamide injection, Naminidil was topically applied to the shaved dorsal skin of the mice at doses of 0.5% and 1.0% (w/w) in a cream formulation, once daily for 21 days. The 1.0% Naminidil group showed 85% hair regrowth rate on day 21, compared to 30% in the vehicle control group. Histological analysis of the dorsal skin revealed that Naminidil-treated mice had a higher density of anagen-phase hair follicles (72 follicles/mm²) than the vehicle control (38 follicles/mm²) [1]
2. Rat androgenetic alopecia model: Male Sprague-Dawley rats with androgenetic alopecia-like symptoms were topically administered 0.5% Naminidil solution once daily for 8 weeks. Compared to the vehicle control, the Naminidil-treated group showed a 40% increase in hair density and a 30% reduction in follicular miniaturization (assessed by follicle diameter measurement). The average hair shaft thickness also increased by 25% in the treated group [1] |
| Cell Assay |
1. Dermal papilla cell (DPC) proliferation assay: Human dermal papilla cells were isolated from healthy scalp hair follicles and cultured in Dulbecco's modified Eagle's medium (DMEM) supplemented with fetal bovine serum. The cells were seeded into 96-well plates at a density of 5×10³ cells per well and allowed to adhere overnight. Serial dilutions of Naminidil (0.01%–1.0% w/v) were added to the wells, with vehicle (culture medium containing the same excipients without Naminidil) as a control. The cells were incubated at 37°C with 5% CO₂ for 72 hours. A cell proliferation assay kit was used to measure the absorbance at 450 nm, and the proliferation rate was calculated relative to the vehicle control [1]
2. Hair follicle organ culture assay: Human scalp hair follicles were isolated under sterile conditions and placed into 24-well plates containing Williams' E medium supplemented with antibiotics and growth factors. Naminidil was added to the medium at final concentrations of 0.1%, 0.5%, and 1.0% (w/v), and the follicles were cultured at 37°C with 5% CO₂. The hair shaft length was measured every 2 days using a microscope, and the phase of the hair growth cycle (anagen, catagen, telogen) was determined by morphological observation on day 14 [1] |
| Animal Protocol |
1. Cyclophosphamide-induced alopecia mouse model: Male C57BL/6 mice (6–8 weeks old) were randomly divided into three groups (n=10 per group): vehicle control, 0.5% Naminidil cream, and 1.0% Naminidil cream. Alopecia was induced by a single intraperitoneal injection of cyclophosphamide (150 mg/kg) on day 0. On day 3 (when alopecia was evident), the dorsal hair of the mice was shaved, and the test formulations were topically applied to the shaved area (0.1 mL per mouse) once daily for 21 days. Hair regrowth was visually scored every 3 days (0 = no regrowth, 4 = complete regrowth). On day 21, the mice were euthanized, and dorsal skin samples were collected for histological analysis (hematoxylin and eosin staining) to count anagen-phase hair follicles [1]
2. Androgenetic alopecia rat model: Male Sprague-Dawley rats (10 weeks old) with naturally occurring androgenetic alopecia-like symptoms were randomly divided into two groups (n=8 per group): vehicle control (ethanol:propylene glycol:water = 20:30:50 v/v/v) and 0.5% Naminidil solution. The test solutions were topically applied to the dorsal alopecic area (0.2 mL per rat) once daily for 8 weeks. Hair density was measured using a digital microscope every 2 weeks, and hair shaft thickness was determined by image analysis. At the end of the study, skin samples were collected to assess follicular miniaturization via histological sectioning [1] 3. Skin irritation test in rabbits: New Zealand white rabbits (n=3) were used for acute skin irritation testing. The dorsal skin of the rabbits was shaved and divided into two areas: one area was treated with 0.5% Naminidil cream (0.2 g) and covered with a gauze patch for 24 hours, and the other area was treated with vehicle cream as a control. After removing the patches, the skin was observed for erythema, edema, or other irritation signs at 1, 24, 48, and 72 hours. No irritation was observed in the Naminidil-treated area [1] |
| Toxicity/Toxicokinetics |
1. Acute skin toxicity: In rabbit skin irritation tests, topical application of 0.5% and 1.0% naphthidine preparations (cream or solution) did not cause skin erythema, edema, itching or corrosion within 72 hours, indicating no acute skin toxicity [1]. 2. Subchronic skin toxicity: In a 28-day subchronic toxicity study in rats, once-daily topical application of 1.0% naphthidine cream (the highest concentration tested) did not cause significant changes in body weight, food consumption or hematological/biochemical parameters (ALT, AST, BUN, creatinine). Histological examination of the skin and major organs (liver, kidney, heart) at the treatment site revealed no abnormalities [1]. 3. Plasma protein binding rate: No data on the plasma protein binding rate of Naminidil is provided in this patent [1].
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| References | |
| Additional Infomation |
1. Naminidil is a topical anti-hair loss drug used to treat androgenetic alopecia (male/female hair loss) and alopecia areata. Its core mechanism of action includes promoting the proliferation of dermal papilla cells, prolonging the anagen phase of the hair growth cycle, and inhibiting hair follicle atrophy, thereby stimulating hair regeneration and preventing further hair loss[1]. 2. This patent mainly relates to topical formulations of naminidil, including creams, gels, lotions, and solutions. The preferred formulation contains 0.1%–1.0% (w/w or w/v) namididil and adds excipients such as humectants, emulsifiers, penetration enhancers and preservatives to improve skin absorption and formulation stability [1]
3. Namididil is for external use only and has very little systemic absorption (not detected in plasma in animal studies), which reduces the risk of systemic side effects compared to oral anti-hair loss drugs [1] 4. The patent states that namididil has a synergistic effect when used in combination with other anti-hair loss drugs (such as minoxidil and finasteride) in a topical formulation, but does not provide specific data on the synergistic effect [1] |
| Molecular Formula |
C15H19N5
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| Molecular Weight |
269.34486
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| Exact Mass |
269.164
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| CAS # |
220641-11-2
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| PubChem CID |
158438
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| Appearance |
White to off-white solid powder
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| Vapour Pressure |
1.42E-06mmHg at 25°C
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| LogP |
3.295
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
20
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| Complexity |
434
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[C@H](C(C)(C)C)N=C(NC#N)NC1=CC=C(C=C1)C#N
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| InChi Key |
PGYDRGZVXVVZQC-LLVKDONJSA-N
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| InChi Code |
InChI=1S/C15H19N5/c1-11(15(2,3)4)19-14(18-10-17)20-13-7-5-12(9-16)6-8-13/h5-8,11H,1-4H3,(H2,18,19,20)/t11-/m1/s1
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| Chemical Name |
1-cyano-3-(4-cyanophenyl)-2-[(2R)-3,3-dimethylbutan-2-yl]guanidine
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| Synonyms |
BMS 234303-01; BMS 234303 01; BMS 23430301
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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 |
| 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) |
DMSO : ~125 mg/mL (~464.10 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.72 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 20.8 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: ≥ 2.08 mg/mL (7.72 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.8 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: ≥ 2.08 mg/mL (7.72 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 | 3.7128 mL | 18.5639 mL | 37.1278 mL | |
| 5 mM | 0.7426 mL | 3.7128 mL | 7.4256 mL | |
| 10 mM | 0.3713 mL | 1.8564 mL | 3.7128 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.
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