| Description | 680C91 is a potent and selective inhibitor of TDO, and its Ki is 51 nM. |
| In vitro | 68OC91是一种高效(Ki = 51 nM)且具有选择性的TDO抑制剂，在10 μM浓度下，对单胺氧化酶A和B、吲哚胺2,3-双加氧酶(EC 1.13.11.17)、5-HT摄取以及5-HT1A、5-HT1D、5-HT2A和5-HT2c受体均无抑制作用。68OC91不会影响色氨酸与血浆中白蛋白的结合，并以竞争方式针对其底物色氨酸抑制TDO。68OC91能抑制大鼠肝细胞和原位灌注的大鼠肝脏中色氨酸的代谢。[1] |
| In vivo | 68OC91的预先给药能够抑制L-[环-2-14C]-色氨酸的分解，并且在体内给予色氨酸的负荷剂量（100 mg/kg）。单独给予68OC91显著提高了大脑中的色氨酸、5-HIAA和5-HT的水平。与68OC91相比，色氨酸的负荷剂量（100 mg/kg）使大脑中色氨酸的增加达到前者的4倍，但不会将大脑中的5-HIAA和5-HT提高到超过68OC91所观察到的水平，并且这些参数的增加持续时间更短。[1] |
| Cell experiments | Cell lines: rat liver cells. Concentrations: 0.1 μM, 0.5 μM, 2 μM. Incubation Time: 0 min - 120 min. Method: The combined concentration of non-labelled L-tryptophan and the L-[ring-2-14C]-tryptophan used in the assays is 20 μM and is added either with or without 68OC91 at time zero. |
| Animal experiments | Animal Models: Male Wistar rats. Dosages: 15 mg/kg. Administration: Oral gavage |
| Target activity | TDO:51 nM(Ki) |
| molecular weight | 238.26 |
| Molecular formula | C15H11FN2 |
| CAS | 163239-22-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 50 mg/mL (209.85 mM) |
| References | 1. M Salter, et al. Biochem Pharmacol. 1995 May 17;49(10):1435-42. 2. Sophie Imbeault, et al. Acta Neuropsychiatr. 2020 Feb;32(1):43-53. |