| 产品描述: | Tribendimidine is an orally active, broad-spectrum anthelmintic agent, with particularly high activity against A. lumbricoides and N. americanus. Tribendimidine is also an L-type nicotinic acetylcholine receptor (nAChR) agonist |
| 靶点: |
nAChR;AChR |
| 体外研究: |
Tribendimidine (100 μg/mL; 24 h) shows intoxication of C. elegans. Tribendimidine (0-100 μg/mL; 6 days) shows toxicity with an LC50 value (concentration at which half the animals are dead) of 54.4 μg/mL. Tribendimidine (0-200 μg/mL; 64 h)-induced sterility is resisted by trb mutant hermaphrodites, and Levamisole-resistant mutants are resistant to Tribendimidine. |
| 体内研究: |
Tribendimidine (75 and 150 mg/kg; p.o.; once) shows inhibition activity against C. sinensis in rats, and shows inhibition against O. viverrini at 400 mg/kg in hamsters. Animal Model: C. sinensis infected Female Wistar rats Dosage: 75 mg/kg and 150 mg/kg Administration: Oral administration, once Result: A 99.1% worm burden reduction was achieved at 150 mg/kg, and the worm burden reduction was still significant (68.9%) at 75 mg/kg. |
| 动物实验: |
Ba/F3, H1975, H3255GR and H3255DR cells were treated with increasing concentrations of inhibitors for 72 hours and growth or the inhibition of growth was assessed by MTS assay according to previously established methods. |
| 参考文献: |
1. Xiao SH, et al. Tribendimidine: a promising, safe and broad-spectrum anthelmintic agent from China. Acta Trop. 2005 Apr;94(1):1-14. 2. Keiser J, et al. Evaluation of the in vivo activity of tribendimidine against Schistosoma mansoni, Fasciola hepatica, Clonorchis sinensis, and Opisthorchis viverrini. Antimicrob Agents Chemother. 2007 Mar;51(3):1096-8. 3. Hu Y, et al. The new anthelmintic tribendimidine is an L-type (levamisole and pyrantel) nicotinic acetylcholine receptor agonist. PLoS Negl Trop Dis. 2009 Aug 11;3(8):e499. |
| 溶解性: |
soluble in DMSO |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.21 ml |
11.048 ml |
22.095 ml |
| 5 mM |
0.442 ml |
2.21 ml |
4.419 ml |
| 10 mM |
0.221 ml |
1.105 ml |
2.21 ml |
| 50 mM |
0.044 ml |
0.221 ml |
0.442 ml |
|
| 注意: |
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