680C91 | Tryptophan 2,3-dioxygenase inhibitor

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 from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
Shipping Code:
RT

Available Options

size :PriceQuantity 
5 mg$68.00
25 mg$272.00

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, 478197

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 from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. 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