(Z)-Lanoconazole
目录号 : GC60428(Z)-Lanoconazole是Lanoconazole的Z构型形式。Lanoconazole是一种强效口服咪唑类抗真菌(antifungal)试剂,具有广谱的体内外抗真菌活性。Lanoconazole通过抑制sterol14-alpha去甲基酶,阻断真菌膜上的ergosterol生物合成,从而干扰ergosterol的生物合成。Lanoconazole可用于皮肤真菌病和甲真菌病的研究。
Sample solution is provided at 25 µL, 10mM.
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- Purity: >99.00%
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(Z)-Lanoconazole is the Z configuration of Lanoconazole. Lanoconazole is a potent and orally active imidazole antifungal agent, shows a broad spectrum of activity against fungi in vitro and in vivo[1]. Lanoconazole interferes with ergosterol biosynthesis by inhibiting sterol 14-alpha demethylase and blocking fungal membrane ergosterol biosynthesis. Lanoconazole can be used for the investigation of dermatophytosis and onychomycosis[1][2].
Lanoconazole (treatment for ear; 0.3%-3%; 6 days) dose‐dependently suppressesTPA-induced irritant dermatitis, suppresses the production of neutrophil chemotactic factors such as keratinocyte‐derived chemokine and macrophage inflammatory protein-2, and inhibited neutrophil infiltration to the inflammation site[2].Lanoconazole (oral administration; 3, 10 or 30 mg/kg; once a day; 3 weeks) significantly inhibits C. neoformans compared with the saline control in normal mice. In addtion, it significantly reduces the growth of C. neoformans in the lungs and brains of MAIDS mice[3].
[1]. Shokoohi GR, et al. In Vitro Activities of Luliconazole, Lanoconazole, and Efinaconazole Compared with Those of Five Antifungal Drugs against Melanized Fungi and Relatives.Antimicrob Agents Chemother. 2017 Oct 24;61(11). pii: e00635-17. [2]. Nakamura A, et al. Anti-inflammatory effect of lanoconazole on 12-O-tetradecanoylphorbol-13-acetate- and 2,4,6-trinitrophenyl chloride-induced skin inflammation in mice.Mycoses. 2020 Feb;63(2):189-196. [3]. Furukawa K, et al. Lanoconazole, a new imidazole antimycotic compound, protects MAIDS mice against encephalitis caused by Cryptococcus neoformans.J Antimicrob Chemother. 2000 Sep;46(3):443-50.
Cas No. | SDF | ||
Canonical SMILES | N#C/C(N1C=CN=C1)=C2SCC(C3=CC=CC=C3Cl)S\2.[(Z)] | ||
分子式 | C14H10ClN3S2 | 分子量 | 319.83 |
溶解度 | 储存条件 | Store at -20°C | |
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1 mg | 5 mg | 10 mg | |
1 mM | 3.1267 mL | 15.6333 mL | 31.2666 mL |
5 mM | 0.6253 mL | 3.1267 mL | 6.2533 mL |
10 mM | 0.3127 mL | 1.5633 mL | 3.1267 mL |
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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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A sensitive and rapid bioanalytical method for the quantitative determination of luliconazole in rabbit eye tissues using UPLC-MS/MS assay
J Chromatogr B Analyt Technol Biomed Life Sci 2022 Apr 1;1194:123173.PMID:35219088DOI:10.1016/j.jchromb.2022.123173.
Luliconazole (LCZ) is a novel antifungal imidazole with broad-spectrum and high susceptibility of Aspergillus and Fusarium are the dominant species of fungal keratitis, may potentially be a new medical treatment option for ocular fungal infection. To evaluate LCZ distribution in ocular tissues after topical application for the development of ophthalmic delivery system, it is important to have a bioanalytical method for measuring the drug concentrations in different ocular tissues and aqueous humor (AH). A selective and sensitive ultrahigh performance liquid chromatography coupled with tandem mass spectrometry (UPLC-MS/MS) method was developed for the quantification of LCZ in rabbit ocular tissues, including conjunctiva, cornea, AH, iris, lens, vitreous humor (VH), retinal choroid and sclera, using lanoconazole as internal standard (IS). Chromatographic separation was achieved on a Xterra MS, C18 column (2.1 × 50 mm, 3.5 μm) using mobile phase with formic acid solution (0.2%, v/v): acetonitrile (50:50, v/v) at a flow rate of 0.2 ml/min, and the run time was 2.5 min. Detection was performed using the transitions 354.1 → 150.3 m/Z for LCZ and 320.1 → 150.3 m/Z for IS by positive ion electrospray ionization in multiple reaction monitoring (MRM) mode. Method validation was conducted in accordance with U.S. Food and Drug Administration's regulatory guidelines for bioanalytical method validation. The calibration curves were linear over the concentration range from 2.80 ng/ml to 2038 ng/ml for conjunctiva, cornea and sclera, 2.09 ng/ml to 1019 ng/ml for AH, 2.09 ng/ml to 509.5 ng/ml for iris, 2.09 ng/ml to 203.8 ng/ml for retinal choroid and VH, 2.04 ng/ml to 101.9 ng/ml for lens, with all the squared correlation coefficients (r2) more than 0.99. The accuracy of the method was within the acceptable limit of 89.34%∼112.78% at the lower limit of quantification and other concentrations, Inter-day and intra-day precision values, expressed in terms of RSD (%), in all tissues were within 15% at all concentrations. The mean recoveries of LCZ in rabbit ocular tissues was 84.85%∼100.52%. No interference was found due to matrix components. Luliconazole was stable during the stability studies, including autosampler stability, benchtop stability, freeze/thaw stability and long-term stability. The method was successfully applied to the ocular pharmacokinetic and tissues distribution studies of LCZ in rabbit after topical administration of LCZ ophthalmic drug delivery system.