| Description | SHA 68 is a potent and selective non-peptide antagonist of neuropeptide S receptor (NPSR)(NPSR Asn107 and NPSR Ile107 with IC50s of 22.0 and 23.8 nM, respectively). |
| In vivo | SHA 68 (腹腔内注射；剂量为5和50mg/kg)能够降低NPS所引发的水平运动以及垂直攀爬[1]。SHA 68 (静脉注射；剂量为1mg/kg)的半衰期为0.74小时，清除率为4.29毫升/分钟/千克，稳态分布体积为2.53升/千克。SHA 68 (腹腔内注射；剂量为2.5mg/kg)的半衰期为0.43小时，清除率为4.56毫升/分钟/千克[1]。 |
| Target activity | Ile107:23.8 nM , Asn107:22 nM |
| molecular weight | 445.49 |
| Molecular formula | C26H24FN3O3 |
| CAS | 847553-89-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 250 mg/mL (561.18 mM), Sonication is recommended. |
| References | 1. Okamura N, et al. Synthesis and pharmacological in vitro and in vivo profile of 3-oxo-1,1-diphenyl-tetrahydro-oxazolo[3,4-a]pyrazine-7-carboxylic acid 4-fluoro-benzylamide (SHA 68), a selective antagonist of the neuropeptide S receptor.J Pharmacol Exp Ther. 2008 Jun;325(3):893-901. 2. Ensho T, et al. Neuropeptide S increases motor activity and thermogenesis in the rat through sympathetic activation.Neuropeptides. 2017 Oct;65:21-27. |