Afoxolaner (CAS 1093861-60-9) – Chemical Properties & Overview
Property Description
IUPAC Name：4-[5-[3-Chloro-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)-4H-1,2-oxazol-3-yl]-N-[2-oxo-2-(2,2,2-trifluoroethylamino)ethyl]-1-naphthalenecarboxamide
Molecular Formula：C₂₆H₁₄ClF₆N₃O₃
Molecular Weight：553.85 g/mol
CAS Number：1093861-60-9
Appearance：White to pale yellow crystalline powder
Solubility：Insoluble in water; soluble in DMSO, ethanol
Melting Point：150–155°C
Chemical Class：Isoxazoline derivative
Mechanism of Action：GABA/glutamate-gated chloride channel inhibitor (arthropod-specific)
Primary Use：Veterinary ectoparasiticide (fleas & ticks)
Target Animals：Dogs (oral administration)
Commercial Products:NexGard® (Merial/Boehringer Ingelheim)
Regulatory Approvals:FDA (USA), EMA (EU), VICH guidelines
Key Benefits:Monthly oral treatment, rapid killing of parasites, low mammalian toxicity
Afoxolaner (CAS 1093861-60-9) - Quality Control Specification
| Parameter | Specification | Test Method |
|---|
| Appearance | White to pale yellow crystalline powder | Visual inspection |
| Identification | Complies (HPLC/IR vs. reference standard) | HPLC, IR spectroscopy |
| Purity (HPLC) | ≥ 98.0% | Reverse-phase HPLC |
| Water Content (KF) | ≤ 0.5% w/w | Karl Fischer titration |
| Residue on Ignition | ≤ 0.1% | USP <281> |
| Heavy Metals | ≤ 10 ppm (as Pb) | ICP-MS / USP <231> |
| Related Substances | Total impurities ≤ 2.0%
Any single impurity ≤ 0.5% | HPLC (area normalization) |
| Particle Size | 90% ≤ 100 µm (customizable) | Laser diffraction (if applicable) |
| Solubility | Insoluble in water;
Soluble in DMSO/ethanol | Solubility test |
| Microbial Limits | Total aerobic count ≤ 1000 CFU/g
Yeast/mold ≤ 100 CFU/g
No pathogens detected | USP <61>, <62> |
| Storage Conditions | 2-8°C (dry, protected from light) | Label requirement |
| Shelf Life | 24 months (unopened, under recommended storage) | Stability studies |
China
