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Product Details

680C91 | Tryptophan 2,3-dioxygenase inhibitor

680C91 (163239-22-3) is a potent and selective inhibitor of tryptophan 2,3-dioxygenase (TDO) Ki=42 nM).1,2 Displays no activity against indoleamine 2,3-dioxygenase, MAO-A and B and does not effect serotonin uptake. Elevates CSF tryptophan by up to 260% and CSF serotonin by 170% of basal.2 TDO inhibition by 680C91 in glioma cells blocked the release of kynurenine (Cat.# 10-2666), an endogenous tumor promoting AHR ligand.4

References/Citations
1) Schwarcz and Pellicciari (2002), Manipulation of brain kynurenines: glial targets, neuronal effects, and clinical opportunities; J. Pharmacol. Exp. Therap., 303 1
2) Salter et al. (1995), The effects of a novel and selective inhibitor of tryptophan 2,3-dioxygenase on tryptophan and serotonin metabolism; Biochem. Pharmacol, 49 1435
3) Salter et al. (1995), 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, 34 217
4) Opitz et al. (2011), An endogenous tumour-promoting ligand of the human aryl hydrocarbon receptor; Nature, 478 197

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680C91 | 163239-22-3 | Structure | Supplier

Catalog#  10-1443

$68.00
Quantity
Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
163239-22-3
Catalog Number:
10-1443
Activity:
Tryptophan 2,3-dioxygenase inhibitor
Chemical Name:
6-Fluoro-3-[(1E)-2-(3-pyridinyl)ethenyl]-1H-indole
Molecular Weight:
238.27
Molecular Formula:
C15H11FN2
Solubility:
Soluble in DMSO (up to 20 mg/ml) or in Ethanol (up to 10 mg/ml)
Physical Properties:
Light brown solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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