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Luliconazole

SKU: orb1941063

Description

Luliconazole is a broad-spectrum antifungal drug.(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). Further, the MIC of luliconazole against Malassezia restricta is very low (MIC range: 0.004-0.016 μg/ml).\n(In Vivo):uliconazole (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).

Images & Validation

Key Properties

CAS Number187164-19-8
MW354.28
Purity>98% (HPLC)
FormulaC14H9Cl2N3S2
SMILESN#C/C(N1C=CN=C1)=C2SC[C@@H](C3=CC=C(Cl)C=C3Cl)S/2
TargetAntifungal
SolubilityEthanol: 5 mg/mL (14.11 mM); DMSO: 71 mg/mL (200.4 mM)

Bioactivity

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). Animal model: Male specific-pathogen-free (SPF) Hartley guinea pig models of tinea corporis and tinea pedis. Dosage: 0.02%-1%. Administration: Appliance on skin; 0.02%-1%; 7-14 days. Result: Was sufficiently potent for short-term treatment for dermatophytosis In vivo.
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). Further, the MIC of luliconazole against Malassezia restricta is very low (MIC range: 0.004-0.016 μg/ml).

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

NND-502

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Luliconazole (orb1941063)

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