Home Microbiology Fungal inhibitor Efinaconazole

research use only

Efinaconazole Fungal inhibitor

Cat.No.S5025

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 Fungal inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 348.39

Jump to

Quality Control

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

Solubility

In vitro
Batch:

DMSO : 69 mg/mL (198.05 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 69 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg
g
μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO
%
% Tween 80
% ddH2O
% DMSO
+
%

Calculation results:

Working concentration: mg/ml;

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.

Chemical Information, Storage & Stability

Molecular Weight 348.39 Formula

C18H22F2N4O

 Storage (From the date of receipt)
CAS No. 164650-44-6 -- Storage of Stock Solutions

Synonyms KP-103 Smiles CC(C(CN1C=NC=N1)(C2=C(C=C(C=C2)F)F)O)N3CCC(=C)CC3

Mechanism of Action

Targets/IC50/Ki
14 alpha-demethylase
In vitro
In in vitro antifungal susceptibility tests, efinaconazole shows lower minimum inhibitory concentration (MIC) than terbinafine, ciclopirox, itraconazole and amorolfine.
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. This compound is metabolized extensively through oxidative and reductive processes resulting in a sole H3 metabolite. It may also undergo glucuronidation. This chemical does not have significant interactions with CYP450 enzymes in the liver. CYP2C8, CYP2C9, CYP2C19 and CYP3A4 are inhibited by this compound at concentrations higher than the systemic concentrations achieved clinically.
References

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.