化合物NKP608 TQ0087

Product Introduction
Bioactivity


英文名: NKP608

描述: NKP608 is a selective and potent antagonist at the neurokinin-1 (NK-1) receptor both in vitro(IC50: 2.6 nM) and in vivo.

体外活性: The binding of NKP608 to the bovine retina was characterized by an IC50 of 2.6 nM, whereas the compound's affinity to other receptor binding sites, including NK-2 and NK-3, was much lower. Species differences in IC50 values with NKP608 were less pronounced than with previously described NK-1 receptor antagonists, being 13 and 27 nM in gerbil midbrain and rat striatum, respectively.

体内活性: Using the hindfoot thumping model in gerbils, NKP608 exhibited a potent NK-1 antagonistic activity following oral administration (ID50: 0.23 mg/kg, 2 h pretreatment), supporting a central activity of NKP608.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : Insoluble
DMSO : 100 mg/mL (161.30 mM)


关键字: NKP 608 | NKP608 | NKP-608

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途