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Lotilaner

Names

[ CAS No. ]:
1369852-71-0

[ Name ]:
Lotilaner

Biological Activity

[Description]:

Lotilaner is a parasiticide, acts as a potent non-competitive antagonist of insects GABACl receptors, with an IC50 of 23.84 nM for Drosophila melanogaster GABA receptor. No effect on a dog GABAA receptor[1].

[Related Catalog]:

Signaling Pathways >> Anti-infection >> Parasite
Research Areas >> Infection
Signaling Pathways >> Membrane Transporter/Ion Channel >> GABA Receptor
Signaling Pathways >> Neuronal Signaling >> GABA Receptor

[Target]

IC50: 23.84 nM (DmS-GABA), 38.25 nM (DmR2-GABA), 52.40 nM (Ls-GABA1), 36.79 nM (Rm-GABA)[1]


[In Vitro]

Lotilaner shows IC50s of 38.25 ± 3.75, 52.40 ± 4.54, 36.79 ± 4.39 nM for Drosophila melanogaster dieldrin/fipronil-resistant forms (DmR2), Lepeophtheirus salmonis (Ls) and Rhipicephalus microplus (Rm) GABACl receptors, respectively[1].

[References]

[1]. Lotilaner, et al. The novel isoxazoline ectoparasiticide lotilaner (Credelio™): a non-competitive antagonist specific to invertebrates γ-aminobutyric acid-gated chloride channels (GABACls). Parasit Vectors. 2017 Nov 1;10(1):530.

Chemical & Physical Properties

[ Molecular Formula ]:
C20H14Cl3F6N3O3S

[ Molecular Weight ]:
596.76

[ Exact Mass ]:
594.97300

[ PSA ]:
108.03000

[ LogP ]:
6.22460


Related Compounds

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