680C91

SKU:

10-1443-25mg

CAS Number:

163239-22-3

Extra Details:

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 basal2. TDO inhibition by 680C91 in glioma cells blocked the release of kynurenine, an endogenous tumor promoting AHR ligand4.

Molecular Weight:

238.27

Physical State:

Light brown solid

References:

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

Shipping Conditions:

Ambient

Storage Conditions:

-20°C

Supplier:

Focus Biomolecules

• Manufacturer's Data Sheet:

Purity:

98% by TLC, NMR (Conforms)

Chemical Name:

6-Fluoro-3-[(1E)-2-(3-pyridinyl)ethenyl]-1H-indole