Oxiconazole (nitrate)
(Synonyms: 硝酸奥昔康唑; Ro 13-8996) 目录号 : GC17528
An antifungal agent
Cas No.:64211-46-7
Sample solution is provided at 25 µL, 10mM.
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Oxiconazole is a new imidazole derivative with a broad fungistatic spectrum against the agents of human mycoses in vitro. Subinhibitory concentrations of oxiconazole inhibited synthesis of DNA and decreased synthesis of RNA, protein and carbohydrate to a lesser extent. In trichophytosis in the guinea-pig and vaginal candidiasis in the rat, oxiconazole exhibited high topical activity. In dermal infection with T. mentagrophytes var. quinckeanum, systemic histoplasmosis, oxiconazole showed systemic oral activity. Oxiconazole was inactive in cryptococcosis and aspergillosis in the mouse [1].
In vitro: oxiconazole is highly effective against many dermatophytes, including Trichophyton rubrum, Trichophyton mentagrophytes, Trichophyton tonsurans, and Epidermophyton floccosum. After application to the skin, oxiconazole is rapidly absorbed into the stratum corneum, maximum concentrations often being attained within 100 minutes. Fungicidal concentrations are maintained in the epidermis, upper corium, and deeper corium for at least five hours, and levels exceeding the minimum inhibitory concentrations of susceptible fungi are present in the corneum, epidermis, upper corium, and the hair follicle for over 16 hours [2].
In patients with tinea pedis treated once daily for four weeks and patients with inea corporis, tinea cruris, and tinea versicolor treated once daily for two weeks, 1% oxiconazole cream produced mycologic and clinical cures in at least 80% of patients. In plantar-type tinea pedis caused primarily by T rubrum, once-daily oxiconazole cream resulted in a mycologic cure in 76% of patients [2].
References:
[1] Polak A. Oxiconazole, a new imidazole derivative. Evaluation of antifungal activity in vitro and in vivo[J]. Arzneimittel-Forschung, 1981, 32(1): 17-24.
[2] Jegasothy B V, Pakes G E. Oxiconazole nitrate: pharmacology, efficacy, and safety of a new imidazole antifungal agent[J]. Clinical therapeutics, 1990, 13(1): 126-141.
Cell experiment: | A total of 121 isolates of pathogenic fungi are tested. The three drugs (including Oxiconazole nitrate) are serially diluted in sterile saline. For each test plate, 2 mL of a solution of drug in sterile saline is added to an 18 mL blank of molten agar medium at 50°C and mixed well; the resulting mixtures are then poured into the plates and allowed to solidify. The resulting drug dilution sequences range from 128 to 0.063 μg/mL. Control plates are prepared in a similar manner using 2 mL blanks of sterile saline. The plates are then inoculated using a replicator. Incubation is at 30°C for a minimum of 96 hr. The Minimal Inhibitory Concentration (MIC) is defined as the lowest concentration of drug producing complete inhibition of growth[1]. |
Animal experiment: | Fifty adult rats are divided into 5 groups consisting of 10 animals each. Over 14 days, the rats in group I receive 0.1 mL of Oxiconazole nitrate-containing solution drops, group II receives 4% boric acid solution in alcohol drops, and groups III and IV receive gentamicin (40 mg/mL) and saline solutions, respectively. Group V receives no medication. Each solution used is given twice a day[2]. |
References: [1]. Shadomy S, et al. Further in vitro studies with oxiconazole nitrate. Diagn Microbiol Infect Dis. 1988 Apr;9(4):231-7. | |
| Cas No. | 64211-46-7 | SDF | |
| 别名 | 硝酸奥昔康唑; Ro 13-8996 | ||
| 化学名 | (1Z)-O-[(2,4-dichlorophenyl)methyl]oxime 1-(2,4-dichlorophenyl)-2-(1H-imidazol-1-yl)-ethanone, mononitrate | ||
| Canonical SMILES | ClC1=CC(Cl)=C(/C(CN2C=NC=C2)=N/OCC3=C(Cl)C=C(Cl)C=C3)C=C1.[O-][N+](O)=O | ||
| 分子式 | C18H13Cl4N3O • HNO3 | 分子量 | 492.1 |
| 溶解度 | ≥ 16.05mg/mL in DMSO | 储存条件 | Room temperature |
| 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 | 2.0321 mL | 10.1605 mL | 20.3211 mL |
| 5 mM | 0.4064 mL | 2.0321 mL | 4.0642 mL |
| 10 mM | 0.2032 mL | 1.0161 mL | 2.0321 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。
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
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