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BTRX-335140 is a selective and orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively. Navacaprant endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats.
Orally administered BTRX-335140 (CYM-53093) showed robust efficacy in antagonizing KOR agonist-induced prolactin secretion and in tail-flick analgesia in mice.
| Molecular Weight | 453.55 |
| Formula | C25H32FN5O2 |
| CAS Number | 2244614-14-8 |
| Solubility (25°C) | DMSO ≥ 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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