680C91

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

680C91 是一种有效的选择性 TDO 抑制剂，其 Ki 为 51 nM。

680C91 is a potent and selective inhibitor of TDO, and its Ki is 51 nM.

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.680C91 inhibits the catabolism of tryptophan by rat liver cells and rat liver perfused in situ. 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.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. Cell Proliferation Assay Cell Line:Uterine stromal cells Concentration:0.01, 0.05, 0.1, 0.5, 1, 5, and 10?μM Incubation Time:24?hours Result:The proliferation activity of stromal cells was significantly decreased at 5 and 10?μM.Western Blot Analysis Cell Line:MSMC and LSMC.Incubation Time:48 hours Result:Significantly reduced the expression of COL1A1 and COL3A1 in LSMC spheroids with no significant effect on expression of these proteins in MSMC spheroids.

680C91 (a dose of 15 mg/kg for acute treatment ) elevates tryptophan in brain. Animal Model:Male C57Bl6/NCrl mice aged 13-18 weeks Dosage:15 mg/kg Administration:Administered per os Result:Caused a significant increase in brain tryptophan.

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Others

Other Targets

TDO

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163239-22-3

238.26

C15H11FN2

>98% (HPLC)

DMSO:48 mg/ml (201.46 mM); Ethanol:25 mg/ml (104.93 mM)

C1=CC(=CN=C1)/C=C/C2=CNC3=C2C=CC(=C3)F

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(-20℃)

With Ice Pack

≥ 2 years