化合物R121919 T16713

Product Introduction
Bioactivity


英文名: R121919

描述: R121919 (NBI30775) 是一种高效的促肾上腺皮质激素释放因子受体 1 （CRF1）小分子受体拮抗剂，具有抗抑郁和抗焦虑活性，抑制 CRF1 受体、 CRF2 受体和 CRF 结合蛋白。

体外活性: R121919是一种强效的小分子CRF1受体拮抗剂，对CRF1受体具有高亲和力，其Ki值在2-5 nM范围内。值得注意的是，其在CRF2受体、CRF结合蛋白和其他70种受体类型上的活性均弱1000倍以上[2]。

体内活性: In rats, R121919 demonstrates a dose-dependent reduction in adrenocorticotropic hormone and corticosterone responses to restraint stress. At a dose of 10 mg/kg R121919, peak plasma concentrations of adrenocorticotropic hormone and corticosterone are decreased by 9% and 25%, respectively[2].Moreover, R121919 exhibits anxiolytic effects in mice with a steep dose-response curve, leading to reduced anxiety levels. Some of the intracellular targets of the drug include molecules like GR (glucocorticoid receptor), MR (mineralocorticoid receptor), BAG-1 (Bcl-2-associated athanogene-1), and AP-1 (activator protein 1)[1].

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

溶解度: DMSO : 5 mg/mL(13.14 mM)
Ethanol : 80 mg/mL(210.23 mM)


关键字: R-121919 | NBI-30775 | R121919 | R 121919 | NBI 30775

相关库: Membrane Protein-targeted Compound Library | GPCR Compound Library

化合物R121919 T16713信息由TargetMol中国为您提供，如您想了解更多关于化合物R121919 T16713报价、型号、参数等信息，欢迎来电或留言咨询。

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