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Amorolfine

CAS# 67467-83-8

Amorolfine

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Chemical structure

Amorolfine

3D structure

Chemical Properties of Amorolfine

Cas No. 67467-83-8 SDF Download SDF
PubChem ID 54260 Appearance Powder
Formula C21H35NO M.Wt 317.5
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble in Chloroform,Dichloromethane,Ethyl Acetate,DMSO,Acetone,etc.
Chemical Name (2R,6S)-2,6-dimethyl-4-[2-methyl-3-[4-(2-methylbutan-2-yl)phenyl]propyl]morpholine
SMILES CCC(C)(C)C1=CC=C(C=C1)CC(C)CN2CC(OC(C2)C)C
Standard InChIKey MQHLMHIZUIDKOO-AYHJJNSGSA-N
Standard InChI InChI=1S/C21H35NO/c1-7-21(5,6)20-10-8-19(9-11-20)12-16(2)13-22-14-17(3)23-18(4)15-22/h8-11,16-18H,7,12-15H2,1-6H3/t16?,17-,18+
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Amorolfine Dilution Calculator

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Amorolfine Molarity Calculator

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Preparing Stock Solutions of Amorolfine

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.1496 mL 15.748 mL 31.4961 mL 62.9921 mL 78.7402 mL
5 mM 0.6299 mL 3.1496 mL 6.2992 mL 12.5984 mL 15.748 mL
10 mM 0.315 mL 1.5748 mL 3.1496 mL 6.2992 mL 7.874 mL
50 mM 0.063 mL 0.315 mL 0.6299 mL 1.2598 mL 1.5748 mL
100 mM 0.0315 mL 0.1575 mL 0.315 mL 0.6299 mL 0.7874 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on Amorolfine

Potential of Chemical and Physical Enhancers for Transungual Delivery of Amorolfine Hydrochloride.[Pubmed:30925734]

Materials (Basel). 2019 Mar 28;12(7). pii: ma12071028.

Topical monotherapy of nail infection is limited by poor drug permeability into the human nail plate. Numerous substances and methods are applied to improve the antifungal agent delivery across the nail plate. This work aimed to evaluate the effect of chemical and physical enhancers on the accumulation and permeation of Amorolfine hydrochloride through human nail clippings. Polymeric nail lacquers with Eudragit E100 were developed as a potentially suitable delivery system for Amorolfine hydrochloride. Incorporating thioglycolic acid and urea into formulations provided increased accumulation of antifungal agent in nail layers of up to 100% and 57%, respectively. Structural changes of nail barrier, induced by fractional CO(2) laser, were visualized by microscopy. The permeation of Amorolfine hydrochloride through the nail increased twofold when thioglycolic acid-containing formulation was applied and the nail was pretreated with a fractional CO(2) laser. The results suggest that this novel combination of enhancers has the potential to be an effective option for topical drug delivery through the nail, and increased the efficacy of treatment.

Daily Application of an Aqueous, Acidifying, Peelable Nail Polish versus Weekly Amorolfine for Topical Onychomycosis Treatment: A Prospective, Randomized, Blinded Trial.[Pubmed:30051298]

Dermatol Ther (Heidelb). 2018 Sep;8(3):463-473.

INTRODUCTION: Onychomycosis is a fungal nail infection, frequently caused by dermatophytes, which occurs in 2-14% of Western adults. The present study was set up to evaluate the efficacy and safety of a water-based, peelable nail polish (daily application), which acidifies the nail environment, versus a 5% Amorolfine nail lacquer (weekly application) for topical treatment of mild-to-moderate onychomycosis. METHODS: One hundred two adults were randomized in this open, prospective, blinded trial. Clinical efficacy was evaluated at baseline and days 30, 60, 120, and 180, respectively. All patients underwent microbiological testing (at baseline and study end). The primary objective of this trial was the change in the percentage of healthy nail surface at day 180. RESULTS: The percentage of healthy surface between baseline and day 180 increased with 11.8% in the test product group and 13.2% in the Amorolfine group, which were statistically comparable. Other onychomycosis-related parameters (dystrophy, discolouration, thickening, and healthy aspect, respectively) showed significant (p < 0.05) improvement after 180 days (versus baseline) with both treatments. Clinical performance was further confirmed by the frequency of patients showing onychomycosis improvement or success at the end of the study: 96.0% (test product) versus 79.6% (Amorolfine). Microbiological results and improved quality of life confirmed clinical performance. Both treatments were well tolerated and appreciated for their properties and efficacy. CONCLUSION: The present trial confirmed the clinical performance of daily acidification of the nail, as reflected by (1) a comparable increase of percentage of healthy nail surface following treatment with the test product versus Amorolfine, (2) the overall improvement of other onychomycosis-related parameters, (3) user convenience, and (4) absence of side effects. These data indicate that daily application of an aqueous, acetic acid-based, peelable solution can be a convenient, safe, and equally effective alternative for the topical management of onychomycosis. TRIAL REGISTRATION: ClinicalTrials.gov identifier; NCT03382717 FUNDING: Oystershell Laboratories.

Randomized Clinical Trial to Evaluate the Efficacy and Safety of Combination Therapy with Short-Pulsed 1,064-nm Neodymium-Doped Yttrium Aluminium Garnet Laser and Amorolfine Nail Lacquer for Onychomycosis.[Pubmed:29200757]

Ann Dermatol. 2017 Dec;29(6):699-705.

Background: Onychomycosis is one of the most prevalent fungal diseases in the general population. However, treatment is of limited effectiveness and must be administered for long periods of time. Systemic antifungal agents are associated with adverse effects. Objective: We evaluated the clinical efficacy and safety of a 1,064-nm neodymium-doped yttrium aluminium garnet (Nd:YAG) laser with Amorolfine nail lacquer to treat onychomycosis. Methods: The 128 patients were randomly divided to 2 groups: 64 in the experimental group were treated with 1,064-nm Nd:YAG laser therapy and Amorolfine nail lacquer; the other 64 were in a control group treated with topical Amorolfine lacquer monotherapy. The laser treatment was 4 sessions at 4-week intervals and Amorolfine lacquer was applied once a week for 16 weeks. Efficacy was assessed as response rate from standardized photographs with ImagePro(R)Plus (Media Cybernetics, Inc., USA) analysis, microscopic examination, and subjective evaluation. Results: At 16 weeks, the experimental group showed a significantly higher cumulative cure rate than the control group (71.88% vs. 20.31%, p<0.0001). Clinical therapeutic effects were linked to patient satisfaction. The percent of "very satisfied" or "satisfied" responses was higher in the test group than the control group (81.25% vs. 23.44%). The treatment regimen was well tolerated, with transient discomfort observed in the test group. Conclusion: The 1,064-nm Nd:YAG laser with Amorolfine nail lacquer was effective and safe for treating onychomycosis. This therapy should be considered an alternative treatment, especially for patients with contraindications to systemic antifungal agents.

Patient-reported outcomes from two randomised studies comparing once-weekly application of amorolfine 5% nail lacquer to other methods of topical treatment in distal and lateral subungual onychomycosis.[Pubmed:28925059]

Mycoses. 2017 Dec;60(12):800-807.

Patient adherence is a key consideration in the choice of a topical regimen for the treatment of onychomycosis. The objective of this study was to investigate patient-reported outcomes (treatment utilisation, adherence and satisfaction) in onychomycosis treated with once-weekly Amorolfine 5% nail lacquer versus once-daily ciclopirox 8% nail lacquer (Study A) or once-daily urea 40% ointment/bifonazole 1% cream combination regimen (Study B). Study A: Subjects received Amorolfine and ciclopirox on opposite feet for 12 weeks. Study B: Subjects received Amorolfine and urea/bifonazole on opposite feet for 6-7 weeks. Assessments included subject adherence as per label, treatment preference and questionnaire. Study A: More subjects adhered to Amorolfine (85%) than to ciclopirox (60%) (P = .025). Overall, subjects were satisfied (95% vs 100%, respectively) and the treatments were balanced in terms of preference (50% vs 45%) at week 12. Study B: More subjects adhered to Amorolfine dosage (81.8%) than to the dosage of the urea/bifonazole combination regimen (59.1%) (P = .096). At the end of study, 85.7% of subjects preferred Amorolfine versus 14.3% for urea/bifonazole. Fewer subjects experienced local side effects with Amorolfine (4.5%) compared to urea (27.3%) and bifonazole (15%). Amorolfine 5% nail lacquer offers a simple and convenient treatment option, which may result in improved patient adherence and consequently lead to improved efficacy and patient satisfaction.

A New Kinetic Spectrophotometric Method for the Quantitation of Amorolfine.[Pubmed:28348920]

J Anal Methods Chem. 2017;2017:9812894.

Amorolfine (AOF) is a compound with fungicide activity based on the dual inhibition of growth of the fungal cell membrane, the biosynthesis and accumulation of sterols, and the reduction of ergosterol. In this work a sensitive kinetic and spectrophotometric method for the AOF quantitation based on the AOF oxidation by means of KMnO4 at 30 min (fixed time), pH alkaline, and ionic strength controlled was developed. Measurements of changes in absorbance at 610 nm were used as criterion of the oxidation progress. In order to maximize the sensitivity, different experimental reaction parameters were carefully studied via factorial screening and optimized by multivariate method. The linearity, intraday, and interday assay precision and accuracy were determined. The absorbance-concentration plot corresponding to tap water spiked samples was rectilinear, over the range of 7.56 x 10(-6)-3.22 x 10(-5) mol L(-1), with detection and quantitation limits of 2.49 x 10(-6) mol L(-1) and 7.56 x 10(-6) mol L(-1), respectively. The proposed method was successfully validated for the application of the determination of the drug in the spiked tap water samples and the percentage recoveries were 94.0-105.0%. The method is simple and does not require expensive instruments or complicated extraction steps of the reaction product.

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