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Itraconazole-d5

Names

[ CAS No. ]:
1217510-38-7

[ Name ]:
Itraconazole-d5

[Synonym ]:
[2H5]-Itraconazole

Biological Activity

[Description]:

Itraconazole-d5 (R51211-d5) is the deuterium labeled Itraconazole. Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects[1][2][3].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Stem Cell/Wnt >> Hedgehog
Research Areas >> Infection
Signaling Pathways >> Metabolic Enzyme/Protease >> Cytochrome P450
Signaling Pathways >> Anti-infection >> Fungal
Signaling Pathways >> Autophagy >> Autophagy

[In Vitro]

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

[References]

[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

[2]. Kim, J., et al., Itraconazole, a commonly used antifungal that inhibits Hedgehog pathway activity and cancer growth. Cancer Cell, 2010. 17(4): p. 388-99.

[3]. Chong, C.R., et al., Inhibition of angiogenesis by the antifungal drug itraconazole. ACS Chem Biol, 2007. 2(4): p. 263-70.

[4]. Pace JR, et al. Repurposing the Clinically Efficacious Antifungal Agent Itraconazole as an Anticancer Chemotherapeutic. J Med Chem. 2016 Apr 28;59(8):3635-49.

Chemical & Physical Properties

[ Molecular Formula ]:
C35H33Cl2D5N8O4

[ Molecular Weight ]:
710.66400

[ Exact Mass ]:
709.27100

[ PSA ]:
104.70000

[ LogP ]:
5.70730

Related Compounds