Albendazole Sulfoxide

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Chemical Structure| 54029-12-8 同义名 : 阿苯达唑氧化物 ;Ricobendazole;Albendazole Oxide;RS 8852
CAS号 : 54029-12-8
货号 : A212431
分子式 : C12H15N3O3S
纯度 : 97%
分子量 : 281.331
MDL号 : MFCD00797922
存储条件:

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 25 mg/mL(88.86 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Albendazole oxide is a derivative of albendazole that inhibits the polymerization of tubulin into microtubules. It shows high inhibitory activity against E. intestinalis in vitro with an IC50 value of 3ng/mL, which is 1.7-fold more inhibitory than albendazole[3]. Albendazole oxide effectively inhibited the growth of Encephalitozoon hellem with IC90 of <10-4μg/mL. The IC90 values of albendazole oxide against Encephalitozoon cuniculi and Encephalitozoon intestinalis were 6×10-3 and 3.8×10-2μg/mL, respectively[4]. In rat hepatic microsomes, albendazole oxide reduces the activity of ethoxyresorufin O-deethylase (EROD) with an IC50 of 5µM[5].
作用机制 Albendazole oxide is a sulfoxide metabolite of albendazole that inhibits tubulin polymerization[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.55mL

0.71mL

0.36mL

17.77mL

3.55mL

1.78mL

35.55mL

7.11mL

3.55mL

参考文献

[1]Choi JS, Han JY, et al. Foetal outcomes after exposure to albendazole in early pregnancy. J Obstet Gynaecol. 2017 Aug 1:1-4.

[2]Fattahi Masoom SH, Lari SM, et al. Albendazole therapy in human lung and liver hydatid cysts: A 13-year experience. Clin Respir J. 2017 Mar 20.

[3]Katiyar SK, Edlind TD. In vitro susceptibilities of the AIDS-associated microsporidian Encephalitozoon intestinalis to albendazole, its sulfoxide metabolite, and 12 additional benzimidazole derivatives. Antimicrob Agents Chemother. 1997;41(12):2729-2732.

[4]Ridoux O, Drancourt M. In vitro susceptibilities of the microsporidia Encephalitozoon cuniculi, Encephalitozoon hellem, and Encephalitozoon intestinalis to albendazole and its sulfoxide and sulfone metabolites. Antimicrob Agents Chemother. 1998;42(12):3301-3303.

[5]Baliharová V, Velík J, Fimanová K, et al. Inhibitory effect of albendazole and its metabolites on cytochromes P450 activities in rat and mouflon in vitro. Pharmacol Rep. 2005;57(1):97-106.