| Size | Price | Stock | Qty |
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Lanoconazole (Astat; TJN-318; NND-318) is a potent, imidazole -based and topical antifungal agent that can be potentially used for dermatophytosis and onychomycosis. It has a broad spectrum of activity against fungi in vitro and in vivo. Lanoconazole interferes with ergosterol biosynthesis by inhibiting sterol 14-alpha demethylase and blocking fungal membrane ergosterol biosynthesis.
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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].
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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 . |
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| Additional Infomation |
Lanoconazole is a conazole antifungal drug and an imidazole antifungal drug.
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| Molecular Formula |
C14H10CLN3S2
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|---|---|
| Molecular Weight |
319.82
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| Exact Mass |
319
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| 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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