| Bioactivity | 680C91 is an orally active, selective tryptophan 2,3-dioxygenase (TDO) inhibitor with a Ki of 51 nM. TDO is the key enzyme of tryptophan catabolism. 680C91 can be used for the research of cancer immunotherapy and Alzheimer’s Disease[1][2][3][4]. | ||||||||||||
| Invitro | 680C91 is a potent (Ki=51 nM) and selective TDO inhibitor with no inhibitory activity against indoleamine 2,3-dioxygenase, monoamine oxidase A and B, 5-HT uptake and 5-HT1A,1D,2A and 2C receptors at a concentration of 10 μM[2].680C91 inhibits the catabolism of tryptophan by rat liver cells and rat liver perfused in situ[2]. Tdo2 could regulate cell proliferation and stimulate the expression of decidual marker Dtprp in the uterine stromal cells and decidual cells. Tdo2 inhibitor 680C91 also inhibits the prolifer ation activity of uterine decidual cells at 24 h[3].Treatment of leiomyoma smooth muscle cell (LSMC) and myometrial smooth muscle cell (MSMC) spheroids with 680C91 (25 and 50 μM) significantly represses the expression of collagen type I (COL1A1) and type III (COL3A1) in a dose-dependent manner[4]. Cell Proliferation Assay[3] Cell Line: | ||||||||||||
| In Vivo | 680C91 (a dose of 15 mg/kg for acute treatment ) elevates tryptophan in brain[5]. Animal Model: | ||||||||||||
| Name | 680C91 | ||||||||||||
| CAS | 163239-22-3 | ||||||||||||
| Formula | C15H11FN2 | ||||||||||||
| Molar Mass | 238.26 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. M Salter, et al. The effects of an inhibitor of tryptophan 2,3-dioxygenase and a combined inhibitor of tryptophan 2,3-dioxygenase and 5-HT reuptake in the rat. Neuropharmacology. 1995 Feb;34(2):217-27. [2]. M Salter, et al. The effects of a novel and selective inhibitor of tryptophan 2,3-dioxygenase on tryptophan and serotonin metabolism in the rat. Biochem Pharmacol. 1995 May 17;49(10):1435-42. [3]. Dang-Dang Li, et al. Differential expression and regulation of Tdo2 during mouse decidualization. J Endocrinol. 2013 Dec 2;220(1):73-83. [4]. Tsai-Der Chuang, et al. Tryptophan catabolism is dysregulated in leiomyomas. Fertil Steril. 2021 Oct;116(4):1160-1171. [5]. Sophie Imbeault, et al. Effects of IDO1 and TDO2 inhibition on cognitive deficits and anxiety following LPS-induced neuroinflammation. Acta Neuropsychiatr. 2020 Feb;32(1):43-53. |