產(chǎn)品目錄

規(guī)格	500 μg 1 mg
CAS	1217510-38-7
別名	N/A
化學名	N/A
分子式	C35H33Cl2D5N8O4
分子量	710.7
溶解度	Chloroform: Slightly Soluble,Methanol: Slightly Soluble
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

Itraconazole-d5 is intended for use as an internal standard for the quantification of itraconazole by GC- or LC-MS. Itraconazole is an antifungal agent and inhibitor of hedgehog signaling (IC50 = 800 nM).1,2 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).1,3 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.2 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).4

1.Vanden Bossche, H., Marichal, P., Le Jeune, L., et al.Effects of itraconazole on cytochrome P-450-dependent sterol 14α-demethylation and reduction of 3-ketosteroids in Cryptococcus neoformansAntimicrob. Agents Chemother.37(10)2101-2105(1993) 2.Kim, J., Tang, J.Y., Gong, R., et al.Itraconazole, a commonly used antifungal that inhibits Hedgehog pathway activity and cancer growthCancer Cell17(4)388-399(2010) 3.Warrilow, A.G., Melo, N., Martel, C.M., et al.Expression, purification, and characterization of Aspergillus fumigatus sterol 14-a demethylase (CYP51) isoenzymes A and BAntimicrob. Agents Chemother.54(10)4225-4234(2010) 4.Strating, J.R.P.M., van der Linden, L., Albulescu, L., et al.Itraconazole inhibits enterovirus replication by targeting the oxysterol-binding proteinCell Rep.10(4)600-615(2015)

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原創(chuàng)作者：上海莼試生物技術有限公司

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