| 产品描述： | Emodepside (PF 1022-221) is a cyclooctadepsipeptide with broad-spectrum anthelmintic activity. |
| 靶点： |
Parasite |
| 体外研究： |
Emodepside is a semisynthetic derivative of PF1022A, which contains a morpholine attached in para position at each of both D-phenyllactic acids. Emodepside is efficacious against a variety of gastrointestinal nematodes. Emodepside binds to a presynaptic latrophilin receptor in nematodes. Emodepside produces a slow time-dependent (20 min), 4-aminopyridine sensitive, concentration-dependent hyperpolarization and increase in voltage-activated K currents. Emodepside has an inhibitory effect on spiking. Emodepside significantly inhibits the ryanodine increase in spike frequency between the 20 and 35 min period by 9.8 spikes/min. In the presence of emodepside, highly increased currents are observed without depolarization up to a threshold of 0 mV and without any additional stimuli to artificially increase [Ca 2+]i levels. These novel findings confirm that Slo-1 is a direct target of emodepside。 |
| 体内研究： |
Emodepside interferes with signaling at the neuromuscular junction on the body-wall muscles, pharynx and egg-laying muscles and thus inhibits three important physiological functions: locomotion, feeding and reproduction。 |
| 参考文献： |
1. Harder A, et al. Mechanisms of action of emodepside. Parasitol Res. 2005 Oct;97 Suppl 1:S1-10. 2. Buxton SK, et al. On the mode of action of emodepside: slow effects on membrane potential and voltage-activated currents in Ascaris suum. Br J Pharmacol. 2011 Sep;164(2b):453-70. 3. Kulke D, et al. Characterization of the Ca2+-gated and voltage-dependent K+-channel Slo-1 of nematodes and its interaction with emodepside. PLoS Negl Trop Dis. 2014 Dec 18;8(12):e3401. 4. Bull K, et al. Effects of the novel anthelmintic emodepside on the locomotion, egg-laying behaviour and development of Caenorhabditis elegans. Int J Parasitol. 2007 May;37(6):627-36. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20°C |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
0.893 ml |
4.467 ml |
8.933 ml |
| 5 mM |
0.179 ml |
0.893 ml |
1.787 ml |
| 10 mM |
0.089 ml |
0.447 ml |
0.893 ml |
| 50 mM |
0.018 ml |
0.089 ml |
0.179 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京