| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| Other Sizes |
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| ln Vitro |
In vitro, terbinafine predominantly acts as a fungicidal agent against a variety of fungal diseases, such as filamentous, dimorphic, and dermatophytes. At the squalene epoxidation site, terbinafine selectively inhibits the formation of fungal ergosterol. The ultimate byproduct of the mechanism, ergosterol, is absent from treated fungal cells, which instead quickly accumulate the intermediate squalene [1].
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|---|---|
| ln Vivo |
Terbinafine has been shown to be particularly effective against experimental dermatophytosis both when applied topically and when taken orally. Skin temperature in guinea pigs afflicted with fungus decreased significantly during the fourth terbinafine therapy [2].
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| References | |
| Additional Infomation |
Terbinafine hydrochloride is a hydrochloride obtained by reaction of terbinafine with one molar equivalent of hydrogen chloride. It has a role as an EC 1.14.13.132 (squalene monooxygenase) inhibitor and a P450 inhibitor. It is a hydrochloride and an allylamine antifungal drug. It contains a terbinafine(1+).
Terbinafine Hydrochloride is a synthetic allylamine derivative structurally related to naftifine, antifungal Terbinafine Hydrochloride blocks ergosterol biosynthesis by inhibition of squalene epoxidase, part of the sterol synthesis pathway for the fungal cell membrane. Highly lipophilic, it tends to accumulate in skin, nails, and fatty tissues. Terbinafine is active against dermatophytes. (NCI04) A naphthalene derivative that inhibits fungal SQUALENE EPOXIDASE and is used to treat DERMATOMYCOSES of the skin and nails. See also: Terbinafine (broader). Drug Indication Treatment of onychomycosis Treatment of onychomycosis |
| Molecular Formula |
C21H26CLN
|
|---|---|
| Molecular Weight |
327.8908
|
| Exact Mass |
327.175
|
| CAS # |
78628-80-5
|
| Related CAS # |
Terbinafine;91161-71-6;Terbinafine-d3 hydrochloride;1310012-15-7;Terbinafine lactate;335276-86-3
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| PubChem CID |
5282481
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| Appearance |
White to off-white solid powder
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| Density |
1.007g/cm3
|
| Boiling Point |
417.9ºC at 760 mmHg
|
| Melting Point |
204-208°C
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| Flash Point |
183.7ºC
|
| Index of Refraction |
1.586
|
| LogP |
5.679
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| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
1
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
23
|
| Complexity |
428
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC(C)(C)C#C/C=C/CN(C)CC1=CC=CC2=CC=CC=C21.Cl
|
| InChi Key |
BWMISRWJRUSYEX-SZKNIZGXSA-N
|
| InChi Code |
InChI=1S/C21H25N.ClH/c1-21(2,3)15-8-5-9-16-22(4)17-19-13-10-12-18-11-6-7-14-20(18)19;/h5-7,9-14H,16-17H2,1-4H3;1H/b9-5+;
|
| Chemical Name |
(E)-N,6,6-trimethyl-N-(naphthalen-1-ylmethyl)hept-2-en-4-yn-1-amine;hydrochloride
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~60 mg/mL (~182.99 mM)
H2O : ~1 mg/mL (~3.05 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.62 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 (7.62 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 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 (7.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 13.75 mg/mL (41.93 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0498 mL | 15.2490 mL | 30.4980 mL | |
| 5 mM | 0.6100 mL | 3.0498 mL | 6.0996 mL | |
| 10 mM | 0.3050 mL | 1.5249 mL | 3.0498 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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