680C91

680C91CAS号: 163239-22-3分子式: C15H11FN2分子量: 238.26描述纯度储存/保存方法可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述
680C91 is a potent and selective inhibitor of TDO, and its Ki is 51 nM.
纯度
98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性
DMSO:50 mg/mL (209.85 mM)
生物活性
靶点
TDO:51 nM(Ki)
In vitro(体外研究)
68OC91, a potent (Ki = 51 nM) and selective TDO inhibitor, has no inhibitory activity against monoamine oxidase A and B, indoleamine 2,3-dioxygenase (EC 1.13.11.17), 5-HT uptake and 5-HT1A,5-HT1D,5-HT2A and 5-HT2c receptors at a concentration of 10 μM. 68OC91 has no effect on the binding of tryptophan to albumin in plasma and inhibited TDO competitively with respect to its substrate tryptophan. 68OC91 inhibits the catabolism of tryptophan by rat liver cells and rat liver perfused in situ.[1]
In vivo(体内研究)
Prior administration of 68OC91 inhibits the catabolism of L-[ring-2-14C]-tryptophan and a load dose of tryptophan (100 mg/kg) in vivo. Administration of 68OC91 alone significantly increases brain tryptophan, 5-HIAA and 5-HT. A load dose of tryptophan (100 mg/kg), producing increases in brain tryptophan 4-fold greater than that seen with 68OC91, does not increase brain 5-HIAA and 5-HT to levels greater than those seen with 68OC91 and produces a shorter-lasting increase in these parameters.[1]