Luliconazole|187164-19-8|-陌孚医药/Medlife

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Luliconazole

目录号: PL03987 纯度: ≥99%

CAS No. :187164-19-8

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中文名称	Luliconazole
中文别名	卢立康唑;4-(2,4-二氯苯基)-1,3-二硫戊环-2-叉-1-咪唑基乙腈;(R)-2-氯-1-(4-甲氧基苯基)乙醇;卢利康唑;鲁利康;美罗培南;(2E)-2-[(4R)-4-(2,4-二氯苯基)-1,3-二硫戊环-2-亚基]-2-(1H-咪唑-1-基)乙腈;卢立康唑, 4-(2,4-二氯苯基)-1,3-二硫戊环-2-叉-1-咪唑基乙腈
英文名称	Luliconazole
英文别名	Luliconazole;4-(2,4-Dichlorophenyl)-1,3-dithiolan-2-ylidene-1-imidazolylacetonitrile;(2E)-2-[(4R)-4-(2,4-Dichlorophenyl)-1,3-dithiolan-2-ylidene]-2-imidazol-1-ylacetonitrile;NND 502;NND-502;PR-2699;(αE)-α-[(4R)-4-(2,4-Dichlorophenyl)-1,3-dithiolan-2-ylidene]-1H-imidazole-1-acetonitrile;[R-(E)]-α-[4-(2,4-Dichlorophenyl)-1,3-dithiolan-2-ylidene]-1H-imidazole-1-acetonitrile;(2E)-2-[(4R)-4-(2,4-Dichlorophenyl)-1,3-dithiolan-2-ylidene]-2-(1H-imidazol-1-yl)acetonitrile;C13478;Lulicon;Luliconazole (This product is only available in Japan.);(R,E)-2-(4-(2,4-DICHLOROPHENYL)-1,3-DITHIOLAN-2-YLIDENE)-2-(1H-IMIDAZOL-1-YL)ACETONITRILE;1H-Imidazole-1-acetonitrile,a-[(4R)-4-(2,4-dichlorophenyl)-1,3-dithiolan-2-ylidene]-,(aE)-;Luzu;RE91AN4S8G;(2E)-2-[(4R)-4-(2,4-dichlorophenyl)-1,3-dithiolan-2-ylidene]-2-imidazol-1-yl-acetonitrile;DSSTox_RID_82805;(R,E)-2-(4-(2,4-dichlorophenyl)-1,3-dithiolan-2-ylidene)-2-(1H-imidazol-1-yl)aceton
Cas No.	187164-19-8
分子式	C₁₄H₉Cl₂N₃S₂
分子量	354.28
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Luliconazole (NND 502) 是一种咪唑类抗生素 (antibiotic)，具有广谱抗真菌活性。Luliconazole 可用于皮肤感染的研究，包括皮肤真菌病、体癣、足癣等的研究。

生物活性

Luliconazole (NND 502) is a topical antifungal imidazole antibiotic with broad-spectrum and potent antifungal activity. Luliconazole can be used for the research of skin infection, including dermatophytosis, tinea corporis, tinea pedis et al.

性状

Solid

体外研究(In Vitro)

The MICs of LLCZ against the organism measured by a standardized microdilution method using RPMI 1640 medium, were 0.002 μg/ml for T. mentagrophytes TIMM1189 and 0.002 μg/ml for TIMM2789.
The minimum inhibitory concentrations (MIC) of luliconazole against Trichophyton spp. ( T. rubrum , T. mentagrophytes and T. tonsurans ) and Candida albicans are measured by the standardized broth microdilution method.
Luliconazole demonstrates great potency against Trichophyton spp. (MIC range: 0.00012-0.002 μg/ml) than the reference agents, with T. rubrum being the most susceptible to it (MIC range: 0.00012-0.00024 μg/ml). Luliconazole is against T. mentagrophytes with MIC values ranging 0.00012-0.002 μg/ml. Luliconazole is also highly active against Candida albicans (MIC range: 0.031-0.13 μg/ml).

体内研究(In Vivo)

Luliconazole (subcutaneous injection; 1, 5 and 25 mg/kg/day) is administered from the beginning of organogenesis (gestation day 7) through the end of lactation (lactation day 20). Luliconazole at 25 mg/kg presents maternal toxicity and embryofetal toxicity (increased prenatal pup mortality, reduced live litter sizes and increased postnatal pup mortality). Luliconazole at 5 mg/kg exhibits no embryofetal toxicity. Additionally, at 25 mg/kg/day has no treatment effects on postnatal development in rats.
Luliconazole (appliance on skin; 0.02%-1%; 7-14 days) has dose-dependent therapeutic efficacy on skin, it exerts efficacy its even at a concentration of 0.02%, and its efficacy at 0.1% is equal to that of 1% bifonazole creama tinea corporis model (4- and 8-day treatment) and the tinea pedis model (7- and 14-day treatment).

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Hiroyasu Koga, et al. Short-term therapy with luliconazole, a novel topical antifungal imidazole, in guinea pig models of tinea corporis and tinea pedis. Antimicrob Agents Chemother. 2012 Jun;56(6):3138-43.
[2]. Hiroyasu Koga, et al. In vitro antifungal activities of luliconazole, a new topical imidazole. Med Mycol. 2009;47(6):640-7.

溶解度数据	In Vitro: DMSO : 50 mg/mL (141.13 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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