Home Microbiology Fungal inhibitor Efinaconazole For research use only.

Efinaconazole

Synonyms: KP-103

Efinaconazole (KP-103) is an inhibitor of 14 alpha-demethylase which is involved in the biosynthesis of ergosterol, a constituent of fungal cell membranes.

Efinaconazole Chemical Structure

Efinaconazole Chemical Structure

CAS: 164650-44-6

Purity & Quality Control

Batch: S502501 DMSO] 69 mg/mL] false] Ethanol] 69 mg/mL] false] Water] Insoluble] false Purity: 99.97%
99.97

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Biological Activity

Description Efinaconazole (KP-103) is an inhibitor of 14 alpha-demethylase which is involved in the biosynthesis of ergosterol, a constituent of fungal cell membranes.
Targets
14 alpha-demethylase [1]
In vitro
In vitro In in vitro antifungal susceptibility tests, efinaconazole shows lower minimum inhibitory concentration (MIC) than terbinafine, ciclopirox, itraconazole and amorolfine[1].
In Vivo
In vivo Efinaconazole is a topical antifungal, so it has relatively low systemic accumulation. The plasma half-life after 10 days of administration is 29.9 h. It has high plasma protein-binding affinity from 95.8 to 96.5%; primarily to albumin, a1-acid glycoprotein and γ-globulin. Efinaconazole is metabolized extensively through oxidative and reductive processes resulting in a sole H3 metabolite. It may also undergo glucuronidation. Efinaconazole does not have significant interactions with CYP450 enzymes in the liver. CYP2C8, CYP2C9, CYP2C19 and CYP3A4 are inhibited by efinaconazole at concentrations higher than the systemic concentrations achieved clinically[1].

Chemical Information & Solubility

Molecular Weight 348.39 Formula

C18H22F2N4O
CAS No. 164650-44-6 SDF --
Smiles CC(C(CN1C=NC=N1)(C2=C(C=C(C=C2)F)F)O)N3CCC(=C)CC3
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 69 mg/mL ( (198.05 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 69 mg/mL

Water : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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