| Description | TCS-OX2-29 is a potent and selective OX2 receptor antagonist (IC50: 40 nM). It displays >250-fold selectivity for OX2 over OX1. |
| In vitro | TCS-OX2-29 对离子通道和转运蛋白表现出选择性，[十]μM浓度下对这些蛋白的抑制率低于30%，这包括了与食物摄取相关的G蛋白偶联受体，如galanin和neuropeptide Y[1]。在转染了OX2受体的CHO细胞中，TCS-OX2-29 抑制了orexin A诱导的IP3积累和ERK1/2的磷酸化[2]。 |
| Target activity | OX2 receptor:40 nM |
| molecular weight | 397.51 |
| Molecular formula | C23H31N3O3 |
| CAS | 372523-75-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 9 mg/mL (22.64 mM) |
| References | 1. Hirose M et al. N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: the first orexin-2 receptor selective non-peptidicantagonist. Bioorg Med Chem Lett, 2003 Dec 15, 13(24):4497-9. 2. R Mould et al. Binding kinetics differentiates functional antagonism of orexin-2 receptor ligands. Br J Pharmacol. 2014 Jan; 171(2): 351-363. |