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Emodepside (Bay 44-4400)

رقم الكتالوجGC33940

Emodepside (Bay 44-4400) (PF 1022-221) عبارة عن ببتيد حلقي حلقي مع نشاط طارد للديدان واسع الطيف.

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Emodepside (Bay 44-4400) التركيب الكيميائي

Cas No.: 155030-63-0

الحجم السعر المخزون الكميّة
1mg
57٫00
متوفر
5mg
126٫00
متوفر
10mg
198٫00
متوفر
10mM (in 1mL DMSO)
244٫00
متوفر
25mg
329٫00
متوفر
50mg
477٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of Emodepside (Bay 44-4400)

Emodepside (PF 1022-221) is a cyclooctadepsipeptide with broad-spectrum anthelmintic activity.

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[1]. 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[2]. 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[3].

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[4].

[1]. Harder A, et al. Mechanisms 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 Ascaris suum. Br J Pharmacol. 2011 Sep;164(2b):453-70. [3]. Kulke D, et al. Characterization of the Ca2+-gated and voltage-dependent K+-channel Slo-1 of nematodes and its interaction with emodepside. 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 Caenorhabditis elegans. Int J Parasitol. 2007 May;37(6):627-36.

Chemical Properties of Emodepside (Bay 44-4400)

Cas No. 155030-63-0 SDF
Canonical SMILES O=C(N([C@H](C(O[C@](C(N([C@H](C(O[C@H](CC1=CC=C(N2CCOCC2)C=C1)C(N(C)[C@H](CC(C)C)C(O[C@H](C)C(N(C)[C@@H](CC(C)C)C3=O)=O)=O)=O)=O)CC(C)C)C)=O)([H])C)=O)CC(C)C)C)[C@H](O3)CC4=CC=C(N5CCOCC5)C=C4
Formula C60H90N6O14 M.Wt 1119.39
الذوبان DMSO : ≥ 31 mg/mL (27.69 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Emodepside (Bay 44-4400)

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 0.8933 mL 4.4667 mL 8.9334 mL
5 mM 0.1787 mL 0.8933 mL 1.7867 mL
10 mM 0.0893 mL 0.4467 mL 0.8933 mL
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In vivo Formulation Calculator (Clear solution) of Emodepside (Bay 44-4400)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 2 reference(s) in Google Scholar.)

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