1. Anti-infection
  2. Fungal
  3. Efinaconazole

Efinaconazole (Synonyms: KP-103)

Cat. No.: HY-15660 Purity: 99.79%
Handling Instructions

Efinaconazole(KP-103) is a novel triazole antifungal drug currently under development as a topical treatment for onychomycosis.

For research use only. We do not sell to patients.

Efinaconazole Chemical Structure

Efinaconazole Chemical Structure

CAS No. : 164650-44-6

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
5 mg USD 50 In-stock
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10 mg USD 70 In-stock
Estimated Time of Arrival: December 31
50 mg USD 190 In-stock
Estimated Time of Arrival: December 31
100 mg USD 290 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Efinaconazole(KP-103) is a novel triazole antifungal drug currently under development as a topical treatment for onychomycosis. IC50 value: 0.0039 ug/ml (MIC for T. mentagrophytes SM-110) [1] Target: antifungal agent in vitro: Efinaconazole was 4-fold more active than itraconazole against T. mentagrophytes SM-110 (MICs of 0.0039 and 0.016 μg/ml, respectively). Similarly, efinaconazole was 8-fold more active than clotrimazole against C. albicans ATCC 10231 (MICs of 0.00098 and 0.0078 μg/ml, respectively) [1]. In a comprehensive survey of 1,493 isolates, efinaconazole MICs against T. rubrum and T. mentagrophytes ranged from ≤ 0.002 to 0.06 μg/ml, with 90% of isolates inhibited (MIC90) at 0.008 and 0.015 μg/ml, respectively. Efinaconazole MICs against 105 C. albicans isolates ranged from ≤ 0.0005 to >0.25 μg/ml, with 50% of isolates inhibited (MIC50) by 0.001 and 0.004 μg/ml at 24 and 48 h, respectively [2]. in vivo: The therapeutic efficacy of KP-103, a triazole derivative, for 10 guinea pigs with interdigital tinea pedis or tinea corporis was investigated. Topical KP-103 solution (0.25 to 1%) was dose-dependently effective in treating both dermatophytoses. A 1% KP-103-treatment rendered all infected skins culture-negative on day-2 posttreatment [3].

Clinical Trial
Molecular Weight

348.39

Formula

C₁₈H₂₂F₂N₄O

CAS No.

164650-44-6

SMILES

C[[email protected]@H](N1CCC(CC1)=C)[[email protected]@](O)(C2=CC=C(F)C=C2F)CN3N=CN=C3

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
In Vitro: 

DMSO : ≥ 100 mg/mL (287.03 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8703 mL 14.3517 mL 28.7035 mL
5 mM 0.5741 mL 2.8703 mL 5.7407 mL
10 mM 0.2870 mL 1.4352 mL 2.8703 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.18 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.18 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.18 mM); Clear solution

*All of the co-solvents are provided by MCE.
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Product Name:
Efinaconazole
Cat. No.:
HY-15660
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