Emodepside

Research use only, not for human use.

A semisynthetic derivative of PF1022A, and novel cyclo-depsipeptide anthelmintic which is efficacious against a variety of gastrointestinal nematodes.

A semisynthetic derivative of PF1022A, and novel cyclo-depsipeptide anthelmintic which is efficacious against a variety of gastrointestinal nematodes; causes parasitic nematode muscle relaxation, inhibition of muscle contraction elicited by either ACh or the neuropeptide AF2; elicits a Ca(++)-dependent hyperpolarization of muscle cells.Parasite Infection Phase 1 Clinical.

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.

PF 1022-221 | PF1022-221 | BAY 44-4400 | BAY44-4400

Microbiology/Virology

Parasite

Parasite

Infection

Parasite Infection

155030-63-0

1119.3884

C60H90N6O14

>98% (HPLC)

DMSO: ≥ 31 mg/mL

O=C([C@H](CC(C)C)N(C)C([C@@H](C)OC([C@H](CC(C)C)N(C)C([C@@H](CC1=CC=C(N2CCOCC2)C=C1)OC([C@H](CC(C)C)N(C)C([C@@H](C)OC([C@H](CC(C)C)N3C)=O)=O)=O)=O)=O)=O)O[C@H](CC4=CC=C(N5CCOCC5)C=C4)C3=O

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]

(-20℃)

With Ice Pack

≥ 2 years