Oxfendazole

产品说明书

Print
Chemical Structure| 53716-50-0 同义名 : 奥芬哒唑 ;Oxfenbendazole;HOE 8105;Fenbendazole sulfoxide
CAS号 : 53716-50-0
货号 : A193817
分子式 : C15H13N3O3S
纯度 : 99%
分子量 : 315.347
MDL号 : MFCD00801063
存储条件：

Pure form Sealed in dry,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(95.13 mM)，配合低频超声，并水浴加热至45℃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 Oxfendazole, a veterinary medicine belonging to the benzimidazole family of anthelmintic drugs, has demonstrated substantial activity against the tissue stages of Taenia solium and has potential to be developed as an effective therapy for neurocysticercosis. Oxfendazole was rapidly absorbed with a mean plasma half-life ranging from 8.5 to 11 h. The renal excretion of oxfendazole was minimal[3]. Oxfendazole (OFZ) is effective against A. suum when used at a single high oral dose of 30 mg/kg[4]. The efficacy of oxfendazole in the reduction of O. lupi mfs was evaluated by microfilarial count and by assessing the percentage of mfs (microfilariae) reduction and mean microfilaricidal efficacy. The mean microfilaricidal efficacy of oxfendazole in the treatment of canine onchocercosis by O. lupi at D30, D90 and D180 was 41%, 81% and 90%, in G2 and 40%, 65% and 70%, in G3, respectively[5]. Oxfendazole also suppressed the cell growth of non‑small cell lung cancer (NSCLC) cells, and overexpression of c‑Src decreased the cytotoxicity of oxfendazole against NSCLC cells[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01584362 Tenia Solium Infection Phase 1 Withdrawn(study conducted unde... 展开 >>r Clinical Trials Agreement as NIAID registration NCT02234570) 收起 << - -
NCT03435718 Trichuris Infection Phase 2 Not yet recruiting October 2021 -
NCT02636803 Helminthiasis Phase 2 Not yet recruiting February 2020 -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.17mL

0.63mL

0.32mL

15.86mL

3.17mL

1.59mL

31.71mL

6.34mL

3.17mL
参考文献

[1]Dewa Y, Nishimura J, et al. Involvement of oxidative stress in hepatocellular tumor-promoting activity of oxfendazole in rats. Arch Toxicol. 2009 May;83(5):503-11.

[2]Gleizes C, Eeckhoutte C, et al. Inducing effect of oxfendazole on cytochrome P450IA2 in rabbit liver. Consequences on cytochrome P450 dependent monooxygenases. Biochem Pharmacol. 1991 Jun 15;41(12):1813-20.

[3]An G, Murry DJ, Gajurel K, et al. Pharmacokinetics, Safety, and Tolerability of Oxfendazole in Healthy Volunteers: a Randomized, Placebo-Controlled First-in-Human Single-Dose Escalation Study. Antimicrob Agents Chemother. 2019;63(4):e02255-18. Published 2019 Mar 27

[4]Ceballos L, Canton C, Cadenazzi G, et al. Oxfendazole kinetics in pigs: In vivo assessment of its pattern of accumulation in Ascaris suum. Exp Parasitol. 2019;199:52‐58

[5]Colella V, Maia C, Pereira A, et al. Evaluation of oxfendazole in the treatment of zoonotic Onchocerca lupi infection in dogs. PLoS Negl Trop Dis. 2018;12(1):e0006218. Published 2018 Jan 29

[6]Xu D, Tian W, Jiang C, Huang Z, Zheng S. The anthelmintic agent oxfendazole inhibits cell growth in non‑small cell lung cancer by suppressing c‑Src activation. Mol Med Rep. 2019;19(4):2921‐2926