中文名 | Emodepside |
英文名 | Emodepside |
别名 | 艾德甙 哀默德斯 艾莫德丝 艾默德斯 EMODEPSIDE艾默德斯 (3S,6R,9S,12R,15S,18R,21S,24R)-3,9,15,21-四异丁基-4,6,10,16,18,22-六甲基-12,24-双(4-吗啉苄基)-1,7,13,19-四氧杂-4,10,16,22-四氮杂环二十四烷-2,5,8,11,14,17,20,23-八酮 |
英文别名 | QHT06 Emodepside PF 1022-221 Bay 44-4400 Cyclo(.alpha.R)-.alpha.-hydroxy-4-(4-morpholinyl)benzeneprop (3S,6R,9S,12R,15S,18R,21S,24R)-3,9,15,21-tetraisobutyl-4,6,10,16,18,22-hexamethyl-12,24-bis(4-morpholinobenzyl)-1,7,13,19-tetraoxa-4,10,16,22-tetraazacyclotetracosan-2,5,8,11,14,17,20,23-octaone Cyclo[(αR)-α-hydroxy-4-(4-morpholinyl)benzenepropanoyl-N-methyl-L-leucyl-(2R)-2-hydroxypropanoyl-N-methyl-L-leucyl-(αR)-α-hydroxy-4-(4-morpholinyl)benzenepropanoyl-N-methyl-L-leucyl-(2R)-2-hydroxypropanoyl-N-methyl-L-leucyl] Cyclo(.alpha.R)-.alpha.-hydroxy-4-(4-morpholinyl)benzenepropanoyl-N-methyl-L-leucyl-(2R)-2-hydroxypropanoyl-N-methyl-L-leucyl-(.alpha.R)-.alpha.-hydroxy-4-(4-morpholinyl)benzenepropanoyl-N-methyl-L-leucyl-(2R)-2-hydroxypropanoyl-N-methyl-L-leucyl |
CAS | 155030-63-0 |
化学式 | C60H90N6O14 |
分子量 | 1119.39 |
密度 | 1.104±0.06 g/cm3(Predicted) |
沸点 | 1219.3±65.0 °C(Predicted) |
溶解度 | DMSO: 31 mg/mL (27.69 mM)( < 1 mg/mL指产品微溶或不溶) |
酸度系数 | 5.34±0.40(Predicted) |
存储条件 | 2-8°C |
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. |
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 |
5 mM | 0.018 ml | 0.089 ml | 0.179 ml |
微信搜索化工百科或扫描下方二维码,添加化工百科小程序,随时随地查信息!