Butenafine
目录号 : GC25181Butenafine is a synthetic benzylamine antifungal agent.
Cas No.:101828-21-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Butenafine is a synthetic benzylamine antifungal agent.
| Cas No. | 101828-21-1 | SDF | Download SDF |
| 分子式 | C23H27N | 分子量 | 317.47 |
| 溶解度 | DMSO: 63 mg/mL (198.44 mM);Water: Insoluble;Ethanol: 63 mg/mL (198.44 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1499 mL | 15.7495 mL | 31.499 mL |
| 5 mM | 0.63 mL | 3.1499 mL | 6.2998 mL |
| 10 mM | 0.315 mL | 1.575 mL | 3.1499 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Butenafine
Drugs 1998 Mar;55(3):405-12; discussion 413.PMID:9530545DOI:10.2165/00003495-199855030-00006.
Butenafine is a new antifungal agent with primary fungicidal activity against dermatophytes such as Trichophyton mentagrophytes, Microsporum canis and Trichophyton rubrum which cause tinea infections. 14C-labelled Butenafine (approximately 30 micrograms/g tissue) was found within guinea-pig dorsal skin 24 hours after topical application. Most of the drug was distributed into the epidermis including the horny layer. Small amounts were found in the dermis, probably transported via sebaceous glands and hair follicles. In vitro, the minimum concentration that completely inhibited growth of dermatophytes (MIC) and the minimum fungicidal concentrations (MFC) for Butenafine against T. mentagrophytes and M. canis were similar (0.012 to 0.05 mg/L) and were 4 to 130 times lower than those for naftifine, tolnaftate, clotrimazole and bifonazole. It also has greater activity against T. rubrum, M. gypseum and Epidermophyton floccosum when compared with naftifine, tolnaftate and clotrimazole; comparisons with bifonazole against these strains were not available. Assessment after 1 week's treatment in patients with tinea pedis revealed that mycological cure rates were greater in those who received twice-daily Butenafine for 1 week or once-daily Butenafine for 4 weeks than in placebo recipients. Mycological and overall cure rates were either further increased or maintained up to 5 weeks after treatment cessation compared with end-of-treatment values. In patients with tinea cruris or tinea corporis who received once-daily Butenafine 1% for 2 weeks, the mycological and overall cure rates continued to increase for up to 4 weeks after treatment cessation.
Butenafine hydrochloride: for the treatment of interdigital tinea pedis
Expert Opin Pharmacother 2000 Mar;1(3):467-73.PMID:11249531DOI:10.1517/14656566.1.3.467.
Butenafine, a derivative of benzylamine with potent fungicidal activity is a new generation of antimycotic compound that has shown to be extremely effective against experimentally-induced tinea pedis in the guinea-pig, a situation that resembles synergetic pathology similar to that of tinea pedis in humans. Butenafine, (N-4-tert-butylbenzyl-N-methyl-1-naphthalenemethyl-amine hydrochloride) with a chemical structure and mode of action similar to those of the allylamines, demonstrates superior fungicidal activity in vitro against dermatophytes and superior fungistatic activity toward Candida albicans that of naftifine and terbinafine. In vitro, pharmacodynamic data has shown that the geometric mean of minimum inhibitory concentration values for Butenafine were comparatively lower than those of naftifine and clotrimazole against clinical isolates for many dermatophytes. It inhibits sterol synthesis by blocking the squalene epoxidation stage in fungi. In phramacokinetic assessments Butenafine achieves and maintains high concentrations and long retention time in skin, with associated anti-inflammatory activity in vivo. In controlled clinical trials when applied topically, Butenafine appears to be well tolerated with a subjective mild burning sensation at the application site. There were no withdrawals from the study. Butenafine is sparingly soluble in water but readily soluble in methanol, ethanol, dichloromethane and chloroform. If incorporated properly in semisolid topical preparations, with a balanced vehicle, Butenafine hydrochloride potentially exhibits as a promising alternative antimycotic agent for the treatment of tinea pedis.
Nanoemulsified Butenafine for Enhanced Performance against Experimental Cutaneous Leishmaniasis
J Immunol Res 2021 Mar 31;2021:8828750.PMID:33880383DOI:10.1155/2021/8828750.
The production of ergosterol lipid involves the activity of different enzymes and is a crucial event for the Leishmania membrane homeostasis. Such enzymes can be blocked by azoles and allylamines drugs, such as the antifungal Butenafine chloride. This drug was active on parasites that cause cutaneous and visceral leishmaniasis. Based on the leishmanicidal activity of Butenafine chloride and considering the absence of reports about the therapeutic potential of this drug in cutaneous leishmaniasis, the present work is aimed at analyzing the efficacy of Butenafine formulated in two different topical delivery systems, the self-nanoemulsifying drug delivery systems (BUT-SNEDDS) and in a SNEDDS-based nanogel (BUT-SNEDDS gel) as well as in the free form in experimental cutaneous leishmaniasis. Physical studies showed that both formulations were below 300 nm with low polydispersity (<0.5) and good colloidal stability (around -25 mV). Increased steady-state flux was reported for nanoenabled Butenafine formulations with reduced lag time in Franz cell diffusion assays across Strat-M membranes. No toxic or inflammatory reactions were detected in animals treated with BUT-SNEDDS, BUT-SNEDDS gel, or Butenafine. Animals topically treated with Butenafine (free or nanoformulated) showed small dermal lesions and low tissue parasitism. Furthermore, BUT-SNEDD gel and Butenafine presented similar efficacy than the standard drug Glucantime given by the intralesional route. Increased levels of IFN-γ were observed in animals treated with BUT-SNEDDS gel or Butenafine. Based on these data, the antifungal drug Butenafine chloride can be considered an interesting repurposed drug for the treatment of cutaneous leishmaniasis.
Diagnosis and management of tinea infections
Am Fam Physician 2014 Nov 15;90(10):702-10.PMID:25403034doi
Tinea infections are caused by dermatophytes and are classified by the involved site. The most common infections in prepubertal children are tinea corporis and tinea capitis, whereas adolescents and adults are more likely to develop tinea cruris, tinea pedis, and tinea unguium (onychomycosis). The clinical diagnosis can be unreliable because tinea infections have many mimics, which can manifest identical lesions. For example, tinea corporis can be confused with eczema, tinea capitis can be confused with alopecia areata, and onychomycosis can be confused with dystrophic toenails from repeated low-level trauma. Physicians should confirm suspected onychomycosis and tinea capitis with a potassium hydroxide preparation or culture. Tinea corporis, tinea cruris, and tinea pedis generally respond to inexpensive topical agents such as terbinafine cream or Butenafine cream, but oral antifungal agents may be indicated for extensive disease, failed topical treatment, immunocompromised patients, or severe moccasin-type tinea pedis. Oral terbinafine is first-line therapy for tinea capitis and onychomycosis because of its tolerability, high cure rate, and low cost. However, kerion should be treated with griseofulvin unless Trichophyton has been documented as the pathogen. Failure to treat kerion promptly can lead to scarring and permanent hair loss.
Butenafine and superficial mycoses: current status
Expert Opin Drug Metab Toxicol 2008 Jul;4(7):999-1005.PMID:18624686DOI:10.1517/17425255.4.7.999.
Background: Butenafine hydrochloride, a benzylamine derivative, exhibits potent fungicidal activity particularly against dermatophytes, aspergilli, dimorphic and dematiaceous fungi. Objective: To review pharmacokinetics, mechanism of actions and clinical efficacy of Butenafine against various dermatophytic and other superficial fungal infections. Methods: Medline search was made using keyword Butenafine. All English language articles were considered for this review. For inclusion in clinical efficacy section when ever available randomized controlled trials were considered a priority over other trials. Results/conclusions: The drug has excellent penetration into the epidermis and a prolonged retention time following topical application, conferring residual therapeutic activity after treatment cessation. Butenafine possess anti-inflammatory activity too. Topical Butenafine 1% cream has been reported to be efficacious for tinea pedis, tinea corporis and tinea cruris in many randomized clinical trials when used for shorter duration. Its efficacy against pityriasis versicolor, seborrheic dermatitis and as anticandidal agent is not yet fully established.