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CAS No.: 155030-63-0

Emodepside/埃莫德塞德 Catalog No. CSN25255

Synonyms: Bay 44-4400

Emodepside is an antiparasitic that is effective against a number of gastrointestinal nematodes, used in cat.

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实验方案

技术信息

生物活性

描述Emodepside, a cyclooctadepsipeptide, is a modern anthelmintic that has a novel mode of action involving a Ca-activated K channel (SLO-1) in Caenorhabditis elegans, sometimes mediated by a latrophilin (LAT) receptor. Emodepside produced a slow time-dependent (20 min), 4-aminopyridine sensitive, concentration-dependent hyperpolarization and increase in voltage-activated K currents^[1]. 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^[2]. Incubation of oocytes with 1-10 µM emodepside caused significantly increased currents over a wide range of step potentials in the absence of experimentally increased intracellular Ca2+, suggesting that emodepside directly opens C. elegans Slo-1a^[3]. Moreover, continuous exposure of wild-type C. elegans to emodepside throughout the life-cycle from egg onwards, slows worm development, an effect that is emodepside concentration-dependent. Emodepside interferes with signalling 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^[4].
参考文献

[1] Buxton SK, Neveu C, Charvet CL, Robertson AP, Martin RJ. On the mode of action of emodepside: slow effects on membrane potential and voltage-activated currents in Ascaris suum. Br J Pharmacol. 2011;164(2b):453-470
[2] Harder A, Holden-Dye L, Walker R, Wunderlich F. Mechanisms of action of emodepside. Parasitol Res. 2005;97 Suppl 1:S1-S10
[3] Kulke D, von Samson-Himmelstjerna G, Miltsch SM, 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;8(12):e3401. Published 2014 Dec 18
[4] Bull K, Cook A, Hopper NA, Harder A, Holden-Dye L, Walker RJ. Effects of the novel anthelmintic emodepside on the locomotion, egg-laying behaviour and development of Caenorhabditis elegans. Int J Parasitol. 2007;37(6):627-636

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 0.8933 mL
- 4.4667 mL
- 8.9334 mL
- 5 mM
- 0.1787 mL
- 0.8933 mL
- 1.7867 mL
- 10 mM
- 0.0893 mL
- 0.4467 mL
- 0.8933 mL

技术信息

CAS号

155030-63-0

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C60H90N6O14

运输

蓝冰

分子量

1119.39

别名

Bay 44-4400

溶解度

DMSO	98.0 mg/mL (87.5 mM)
Water	Insoluble
Ethanol	18.0 mg/mL (16.1 mM)

动物实验配方

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