Soclenicant
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Soclenicant (BNC210) is an orally active α7 nAChR negative alteration modulator (NAM) with no apparent side effects. Soclenicant exhibits acute anxiolytic activity in rodent models of anxiety. Soclenicant inhibits rat and human α7 nAChR currents (in stably transfected cell lines) induced by acetylcholine, nicotine, choline, and the a7-specific agonist PNU-282987 (HY-12560A) with IC50 values in the range of 1.2 to 3 μM. Soclenicant can be used in studies of anxiety, trauma, and stressor-related disorders.
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- Pureté: 99.75%
- CAS No.: 1020634-41-6
- Formule: C24H26N4O3
- Masse moléculaire:418.49
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Activité biologique
Mean pharmacokinetic parameters following oral administration of Soclenicant (BNC210) to male Sprague Dawley rats at doses of 0.5, 5 and 100 mg/kg[3]
| Parameter | Measured Dose (mg/kg) | Apparent thalf (h) | Cmax (μM) | Tmax (min) | AUC0-tlast (μM*min) | AUC0-inf (μM*min) | AUC0-inf/D (μM*min*kg/μmol) | Apparent BA (%) | % Dose in urine |
| 0.5 mg/kg | 0.55 | c.n.c. | 0.2 | 30 | 53.8 | c.n.c. | 41.4 | 66.7 | 1.6 |
| 5 mg/kg | 4.8 | 8.8 | 1.1 | 30/300/30 | 496.8 | 497.6 | 43.7 | 70.3 | 0.7 |
| 100 mg/kg | 102.4 | 6.3 | 5.7 | 150 | 3055.1 | 3062.9 | 12.5 | 13.2 | 0.2 |