| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
sterol 14-alpha demethylase
Lanosterol 14α-demethylase (a cytochrome P450 enzyme, CYP51), which is involved in ergosterol biosynthesis in fungi. |
|---|---|
| ln Vitro |
Lanoconazole is a potent inhibitor of ergosterol biosynthesis, leading to the disruption of fungal cell membrane integrity. It exhibits broad-spectrum antifungal activity against dermatophytes, yeasts, and molds. Specific MIC values vary depending on the fungal species. The compound is effective in vitro against common pathogens such as Trichophyton, Microsporum, and Candida species.
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| ln Vivo |
In addition to inhibiting the production of neutrophil chemokines like keratinocyte-derived chemokines and macrophage inflammatory proteins-2, lanoconazole (treated ears; 0.3%–3%; 6 days) also dose-dependently prevents TPA-induced irritant dermatitis and prevents neutrophil infiltration into the inflammatory site [2]. In comparison to saline controls, lanoconazole (oral; 3, 10, or 30 mg/kg; once daily; 3 weeks) effectively inhibited Cryptococcus neoformans in normal mice. Moreover, it considerably inhibited Cryptococcus neoformans growth. neoformans in the MAIDS mice's brain and lungs [3].
In vivo, lanoconazole demonstrates potent antifungal activity in animal models of dermatophytosis and other superficial fungal infections. It is effective when applied topically, leading to rapid resolution of skin lesions. The compound has been evaluated in preclinical studies for its efficacy and safety. |
| Enzyme Assay |
Lanoconazole antifungal activity is assessed using in vitro susceptibility testing methods, such as broth microdilution or agar diffusion, to determine minimum inhibitory concentrations (MICs) against various fungal pathogens. The inhibition of ergosterol biosynthesis can be measured by analyzing the sterol composition of treated fungal cells.
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| Cell Assay |
Lanoconazole cellular activity is evaluated in cultures of pathogenic fungi. Fungal cells are treated with varying concentrations of the compound, and fungal growth is monitored by optical density or colony counting. The disruption of cell membrane integrity can be assessed by measuring the leakage of intracellular contents or by using fluorescent viability stains.
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| Animal Protocol |
Animal/Disease Models: balb/c (Bagg ALBino) mouse[2]
Doses: 0.3%-3% dosage Route of Administration: Treatment for ear Experimental Results: demonstrated an inhibition effect of LCZ on ear swelling induced by topical application of TPA in mice. Animal/Disease Models: Four week old C57BL /6 mice infected intraperitoneally with LP-BM5 murine leukaemia virus[3] Doses: 3, 10 or 30 mg/kg Route of Administration: Oral adminstration Experimental Results: Inhibited C. neoformans growth in both normal and C. neoformans -induced encephalitis MAIDS mice . In vivo efficacy is studied in animal models of dermatophytosis, such as guinea pigs or mice infected with Trichophyton or Microsporum species. Lanoconazole is applied topically at various concentrations, and the resolution of skin lesions is assessed clinically and by mycological culture. The compound's safety and tolerability are also evaluated in these models. |
| ADME/Pharmacokinetics |
Lanoconazole has a molecular weight of 319.83 g/mol and a molecular formula of C14H10ClN3S2. It is a light yellow crystalline solid with a melting point of 141.5°C. The compound is practically insoluble in water. Topical formulations are used for clinical applications.
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| Toxicity/Toxicokinetics |
Lanoconazole has a favorable safety profile in topical use. The oral LD50 values in mice are 3224 mg/kg for males and 2715 mg/kg for females. The dermal LD50 in rats is >5000 mg/kg. No significant systemic toxicity is observed with topical administration.
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| References |
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| Additional Infomation |
Lanoconazole is a type of lanoconazole antifungal drug and an imidazole antifungal drug.
Lanoconazole is an approved antifungal agent used clinically for the topical treatment of dermatophytosis, including tinea pedis, tinea corporis, and tinea cruris. It is marketed under the trade name Astat. The compound is a racemic mixture with the CAS name (E)-(±)-α-[4-(2-Chlorophenyl)-1,3-dithiolan-2-ylidene]-1H-imidazole-1-acetonitrile. |
| Molecular Formula |
C14H10CLN3S2
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|---|---|
| Molecular Weight |
319.82
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| Exact Mass |
319
|
| CAS # |
101530-10-3
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| Related CAS # |
(Z)-Lanoconazole;101529-65-1
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| PubChem CID |
3002820
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
477.6±55.0 °C at 760 mmHg
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| Melting Point |
141.50C
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| Flash Point |
242.6±31.5 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.725
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| LogP |
3.38
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
20
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| Complexity |
445
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1C(S/C(=C(\C#N)/N2C=CN=C2)/S1)C3=CC=CC=C3Cl
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| InChi Key |
ZRTQSJFIDWNVJW-WYMLVPIESA-N
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| InChi Code |
InChI=1S/C14H10ClN3S2/c15-11-4-2-1-3-10(11)13-8-19-14(20-13)12(7-16)18-6-5-17-9-18/h1-6,9,13H,8H2/b14-12+
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| Chemical Name |
(2E)-2-[4-(2-chlorophenyl)-1,3-dithiolan-2-ylidene]-2-imidazol-1-ylacetonitrile
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| Synonyms |
NND-318 Astat TJN318NND318 Lanoconazole
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~312.67 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.82 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (7.82 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.82 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1268 mL | 15.6338 mL | 31.2676 mL | |
| 5 mM | 0.6254 mL | 3.1268 mL | 6.2535 mL | |
| 10 mM | 0.3127 mL | 1.5634 mL | 3.1268 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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