Lotilaner is a gamma-aminobutyric acid (GABA)-gated chloride channel inhibitor that is highly selective against mites. It has antiparasitic activity with an IC50 value of 23.84 nM against the Drosophila GABA receptor and can be used in studies related to helminth mite blepharitis.
| Molecular Weight | 596.76 |
| Formula | C20H14Cl3F6N3O3S |
| CAS Number | 1369852-71-0 |
| Form | Solid |
| Solubility (25°C) | DMSO >100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Yahiya Y Syed. Drugs. Lotilaner Ophthalmic Solution 0.25%: First Approval
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