S83575 |
Emodepside |
源叶(MedMol) | 98% |
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- 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
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)