Shelf life (days): 1460.0
Formulation: A solid
Formal Name: 4-(4-(4-(4-(((2R,4S)-2-((1H-1,2,4-triazol-1-yl)methyl)-2-(2,4-dichlorophenyl)-1,3-dioxolan-4-yl)methoxy)phenyl)piperazin-1-yl)phenyl)-2-(butan-2-yl-3,3,4,4,4-d5)-2,4-dihydro-3H-1,2,4-triazol-3-one
Purity: ≥99% deuterated forms (d1-d5)
Formula Markup: C35H33Cl2D5N8O4
Formula Weight: 710.66344
CAS Number: 1217510-38-7
Notes: Itraconazole-d5 is intended for use as an internal standard for the quantification of itraconazole (Item No. 13288) by GC- or LC-MS. Itraconazole is an antifungal agent and inhibitor of hedgehog signaling (IC50 = 800 nM).{36692,19161} It binds to 14-α sterol demethylase/CYP51 isoform B (AF51B; Kd = 31 nM for A. fumigatus enzyme expressed in E. coli) and inhibits ergosterol biosynthesis in C. neoformans (IC50 = 6 nM after a 16-hour incubation).{36692,25587} It inhibits the growth of C. neoformans by 50% when used at a concentration of 3.2 nM. Itraconazole inhibits hedgehog signaling, reducing accumulation of Smoothened induced by sonic hedgehog (Shh) in primary cilia of NIHT-3T3 cells.{19161} It suppresses growth of medulloblastomas in a Ptch+/-p53-/- mouse allograft model when administered at a dose of 100 mg/kg twice daily. Itraconazole (1.25-100 µM) also reduces viral titers of several enteroviruses, including human rhinovirus 17, in infected cells, effects that can be reversed by overexpression of OSBP, the gene encoding oxysterol-binding protein (OSBP).{45895}
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