[CAS NO. 101530-10-3] Lanoconazole
PRODUCTS SPECIFICATIONS [101530-10-3]
DESCRIPTION [101530-10-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 319.83 |
| Molecular Formula | C14H10ClN3S2 |
| SMILES | N#C/C(N1C=CN=C1)=C2SC(C(C=CC=C3)=C3Cl)CS\2.[(E)] |
Summary
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] .
IC50 & Target
IC50: antifungal [1]
In Vivo
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | BALB/c mice [2] |
| Dosage: | 0.3%-3% dosage |
| Administration: | Treatment for ear |
| Result: | Exhibited an inhibition effect of LCZ on ear swelling induced by topical application of TPA in mice. |
| Animal Model: | Four week old C57BL/6 mice infected intraperitoneally with LP-BM5 murine leukaemia virus [3] |
| Dosage: | 3, 10 or 30 mg/kg |
| Administration: | Oral adminstration |
| Result: | Inhibited C. neoformans growth in both normal and C. neoformans -induced encephalitis MAIDS mice . |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 312.67 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
References
- [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.
Synonyms