An antifungal agent and hedgehog pathway inhibitor; inhibits hedgehog signaling (IC50 = 0.8 μM); binds to 14-α sterol demethylase/CYP51 isoform B (Kd = 31 nM for A. fumigatus enzyme expressed in E. coli); inhibits ergosterol biosynthesis in C. neoformans (IC50 = 6 nM after 16 hours); inhibits C. neoformans growth by 50% at 3.2 nM; suppresses growth of medulloblastomas in a Ptch+/-p53-/- mouse allograft model at 100 mg/kg twice daily; reduces viral titers of several enteroviruses in infected cells from 1.25-100 µM

Itraconazole – 250 mg

Brand:
Cayman
CAS:
84625-61-6
Storage:
-20
UN-No:
Non-Hazardous - /

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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Description

An antifungal agent and hedgehog pathway inhibitor; inhibits hedgehog signaling (IC50 = 0.8 μM); binds to 14-α sterol demethylase/CYP51 isoform B (Kd = 31 nM for A. fumigatus enzyme expressed in E. coli); inhibits ergosterol biosynthesis in C. neoformans (IC50 = 6 nM after 16 hours); inhibits C. neoformans growth by 50% at 3.2 nM; suppresses growth of medulloblastomas in a Ptch+/-p53-/- mouse allograft model at 100 mg/kg twice daily; reduces viral titers of several enteroviruses in infected cells from 1.25-100 µM

Formal name: 4-[4-[4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]-2,4-dihydro-2-(1-methylpropyl)-3H-1,2,4-triazol-3-one

Synonyms: 

Molecular weight: 705.6

CAS: 84625-61-6

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Antifungals|Triazoles||Product Type|Biochemicals|Antivirals||Product Type|Biochemicals|Small Molecule Inhibitors|Cytochrome P450||Product Type|Biochemicals|Small Molecule Inhibitors|Demethylases||Product Type|Biochemicals|Small Molecule Inhibitors|Sterol Biosynthesis||Research Area|Cancer|Cell Signaling|Hedgehog Signaling||Research Area|Cell Biology|Cell Signaling|Hedgehog Signaling||Research Area|Immunology & Inflammation||Research Area|Infectious Disease|Fungal Diseases|Aspergillosis||Research Area|Infectious Disease|Viral Diseases|Rhinoviruses

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