| Bioactivity | TIK-301 (PD-6735) is a chlorinated melatonin derivative and a potent, high-affinity and orally active melatonin MT1 and MT2 receptors agonist with Kis of 0.081 nM and 0.042 nM, respectively. TIK-301 is also a 5-HT2B/5-HT2C receptors antagonist with antidepressant action. TIK-301 has the potential for sleep disorders and other circadian rhythm disorders treatment[1][2][3]. |
| In Vivo | In male rats, TIK-301(at doses of 0.8 and 4.0 mg/kg/day) can reduce body weight, and without altering food intake[1][2].The Tmax and half-life of TIK-301 is 1.1 hour and 1 hour, respectively[1]. |
| Name | TIK-301 |
| CAS | 118702-11-7 |
| Formula | C14H17ClN2O2 |
| Molar Mass | 280.75 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Paulis L, et al. Cardiovascular effects of melatonin receptor agonists. Expert Opin Investig Drugs. 2012 Nov;21(11):1661-78. [2]. Rivara S, et al. Melatonin receptor agonists: SAR and applications to the treatment of sleep-wake disorders. Curr Top Med Chem. 2008;8(11):954-68. [3]. Carocci A, et al. Melatonergic drugs in development. Clin Pharmacol. 2014 Sep 18;6:127-37. |