155030-63-0
基本信息
哀默德斯
EMODEPSIDE艾默德斯
Emodepside
Bay 44-4400
PF 1022-221
Cyclo(.alpha.R)-.alpha.-hydroxy-4-(4-morpholinyl)benzeneprop
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
物理化学性质
| 沸点 | 1219.3±65.0 °C(Predicted) |
| 密度 | 1.104±0.06 g/cm3(Predicted) |
| 储存条件 | Sealed in dry,2-8°C |
| 溶解度 | DMSO : ≥ 31 mg/mL (27.69 mM) |
| 酸度系数(pKa) | 5.34±0.40(Predicted) |
| 形态 | Solid |
| 颜色 | White to off-white |
安全数据
| 危险性符号(GHS) |   GHS08,GHS09 |
| 警示词 | 警告 |
| 危险性描述 | H372-H410 |
| 防范说明 | P260-P264-P270-P314-P501-P273-P391-P501 |
常见问题列表
| Target | Value |
|
Ca-dependent SLO-1-like K channels
() |
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.
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.