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155030-63-0

中文名稱 艾默德斯
英文名稱 Emodepside
CAS 155030-63-0
分子式 C60H90N6O14
分子量 1119.39
MOL 文件 155030-63-0.mol
更新日期 2024/12/18 15:29:09
155030-63-0 結(jié)構(gòu)式 155030-63-0 結(jié)構(gòu)式

基本信息

中文別名
艾默德斯
哀默德斯
EMODEPSIDE艾默德斯
英文別名
QHT06
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
所屬類別
化學(xué)農(nóng)藥原藥:殺蟲劑

物理化學(xué)性質(zhì)

沸點(diǎn)1219.3±65.0 °C(Predicted)
密度1.104±0.06 g/cm3(Predicted)
儲存條件Sealed in dry,2-8°C
溶解度DMSO : ≥ 31 mg/mL (27.69 mM)
酸度系數(shù)(pKa)5.34±0.40(Predicted)
形態(tài)Solid
顏色White to off-white

安全數(shù)據(jù)

危險(xiǎn)性符號(GHS)GHS hazard pictogramsGHS hazard pictograms
GHS08,GHS09
警示詞警告
危險(xiǎn)性描述H372-H410

常見問題列表

生物活性
Emodepside (QHT06, BAY 44-4400, PF 1022-221) 是一種PF1022A的半合成衍生物,是一種具有廣譜的驅(qū)蟲活性的環(huán)八肽。 Emodepside 可激活 Ca-dependent SLO-1-like K channels。
靶點(diǎn)
TargetValue
Ca-dependent SLO-1-like K channels
()
體外研究

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.

體內(nèi)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.

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