Dapaconazole

Names

[ Name ]:
Dapaconazole

[Synonym ]:
1-[2-(2,4-Dichlorophenyl)-2-{[4-(trifluoromethyl)benzyl]oxy}ethyl]-1H-imidazole
dapaconazole
H2976538CX
1H-Imidazole, 1-[2-(2,4-dichlorophenyl)-2-[[4-(trifluoromethyl)phenyl]methoxy]ethyl]-
UNII:H2976538CX

Biological Activity

[Description]:

Dapaconazole, as an antifungal agent, inhibits sterol 14α-demethylase cytochrome P450 activity with an IC50 of 1.4 μM[1].

[Related Catalog]:

Research Areas >> Infection

Signaling Pathways >> Metabolic Enzyme/Protease >> Cytochrome P450

[Target]

Cytochrome P450 (CYP26):1.4 μM (IC50)

[In Vitro]

Dapaconazole inhibits sterol 14α-demethylase cytochrome P450 activity with an IC50 of 1.4 ± 0.3 μM[1].

[In Vivo]

Dapaconazole (20 mg/kg; p.o.) shows that the bioavailability is 97.3 %[1]. Animal Model: Male beagle dogs[1] Dosage: 20 mg/kg (Pharmacokinetic Analysis) Administration: P.o. Result: Showed that the bioavailability was 97.3 %.

[References]

[1]. Juliana SP, et al. Pharmacokinetics of Dapaconazole, A Novel Antifungal Agent, in Beagle Dogs and Inhibition of Cytochrome P450 Family 51. J Eur Acad Dermatol Venereol. 2018 Jun 10.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
512.8±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₉H₁₅Cl₂F₃N₂O

[ Molecular Weight ]:
415.236

[ Flash Point ]:
263.9±30.1 °C

[ Exact Mass ]:
414.051361

[ LogP ]:
5.30

[ Vapour Pressure ]:
0.0±1.3 mmHg at 25°C

[ Index of Refraction ]:
1.565

[ Storage condition ]:
2-8°C