Emodepside-Bay-44-4400-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEEmodepsideCat. No.: HY-101476CAS No.: 155030-63-0Synonyms: Bay 44-4400分式: CHNO分量: 1119.39作靶點(diǎn): Parasite作通路: Anti-infection儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 31 mg/mL (27.69 mM)*

2、 means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 0.8933 mL 4.4667 mL 8.9334 mL5 mM 0.1787 mL 0.8933 mL 1.7867 mL10 mM 0.0893 mL 0.4467 mL 0.8933 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Emodepside (PF 1022-221)具有譜驅(qū)活性的環(huán)庚三烯肽。體外研究Emod

3、epside is a semisynthetic derivative of PF1022A, which contains a morpholine attached in para positionat each of both D-phenyllactic acids. Emodepside is efficacious against a variety of gastrointestinalnematodes. Emodepside binds to a presynaptic latrophilin receptor in nematodes 1. Emodepside prod

4、uces1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEa slow time-dependent (20 min), 4-aminopyridine sensitive, concentration-dependent hyperpolarization andincrease in voltage-activated K currents. Emodepside has an inhibitory effect on spiking. Emodepsidesignificantly inhibits the ryanodine increa

5、se in spike frequency between the 20 and 35 min period by 9.8spikes/min 2. In the presence of emodepside, highly increased currents are observed without depolarizationup to a threshold of 0 mV and without any additional stimuli to artificially increase Ca 2+i levels. These novelfindings confirm that

6、 Slo-1 is a direct target of emodepside 3.體內(nèi)研究 Emodepside interferes with signaling at the neuromuscular junction on the body-wall muscles, pharynx andegg-laying muscles and thus inhibits three important physiological functions: locomotion, feeding andreproduction 4.REFERENCES1. Harder A, et al. Mec

7、hanisms of action of emodepside. Parasitol Res. 2005 Oct;97 Suppl 1:S1-10.2. Buxton SK, et al. On the mode of action of emodepside: slow effects on membrane potential and voltage-activated currents in Ascarissuum. Br J Pharmacol. 2011 Sep;164(2b):453-70.3. Kulke D, et al. Characterization of the Ca2

8、+-gated and voltage-dependent K+-channel Slo-1 of nematodes and its interaction withemodepside. PLoS Negl Trop Dis. 2014 Dec 18;8(12):e3401.4. Bull K, et al. Effects of the novel anthelmintic emodepside on the locomotion, egg-laying behaviour and development of Caenorhabditiselegans. Int J Parasitol. 2007 May;37(6):627-36.McePdfHeightCaution: Product has not been fully validated for medical application