680C91

SKU: orb1218684

Description

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

Key Properties

• CAS Number: 163239-22-3
• MW: 238.26
• Purity: >98% (HPLC)
• Formula: C₁₅H₁₁FN₂
• SMILES: C1=CC(=CN=C1)/C=C/C2=CNC3=C2C=CC(=C3)F
• Target: TDO
• Solubility: DMSO:48 mg/ml (201.46 mM); Ethanol:25 mg/ml (104.93 mM)

Bioactivity

• In Vivo:
  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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• In Vitro:
  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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

TDO