EMODEPSIDE

中文名称:

EMODEPSIDE

中文同义词:

艾默德斯;EMODEPSIDE艾默德斯;哀默德斯

英文名称:

Emodepside

英文同义词:

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;Emodepside;Cyclo(.alpha.R)-.alpha.-hydroxy-4-(4-morpholinyl)benzeneprop;QHT06;PF 1022-221;Bay 44-4400;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]

CAS号:

155030-63-0

分子式:

C60H90N6O14

分子量:

1119.39

EINECS号:

相关类别:

科研原料;API

Mol文件:

155030-63-0.mol

沸点 

1219.3±65.0 °C(Predicted)

密度 

1.104±0.06 g/cm3(Predicted)

酸度系数(pKa)

5.34±0.40(Predicted)

生物活性

Emodepside (QHT06, BAY 44-4400, PF 1022-221) 是一种PF1022A的半合成衍生物，是一种具有广谱的驱虫活性的环八肽。 Emodepside 可激活 Ca-dependent SLO-1-like K channels。

靶点

Target Value Ca-dependent SLO-1-like K channels ()

Target

Value

Ca-dependent SLO-1-like K channels ()

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.