Home Metabolism IDO/TDO inhibitor 680C91 For research use only.

680C91

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

680C91 Chemical Structure

680C91 Chemical Structure

CAS: 163239-22-3

Selleck's 680C91 has been cited by 3 publications

Purity & Quality Control

Batch: S899701 DMSO] 48 mg/mL] false] Ethanol] 25 mg/mL] false] Water] Insoluble] false Purity: 99.64%
99.64

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Biological Activity

Description 680C91 is a potent and selective inhibitor of TDO with Ki of 51 nM.
Targets
TDO [1]
(Cell-free assay)
51 nM(Ki)
In vitro
In vitro

68OC91 is a potent (Ki = 51 nM) and selective TDO inhibitor with no inhibitory activity against indoleamine 2,3-dioxygenase (EC 1.13.11.17), monoamine oxidase A and B, 5-HT uptake and 5-HT1A,1D,2A and 2c receptors at a concentration of 10 μM. 68OC91 has no effect on the binding of tryptophan to serum albumin in plasma and inhibited TDO competitively with respect to its substrate tryptophan. 68OC91 inhibits the catabolism of tryptophan by rat liver cells and rat liver perfused in situ.[1]
Cell Research Cell lines rat liver cells
Concentrations 0.1 μM, 0.5 μM, 2 μM
Incubation Time 0 min - 120 min
Method

The combined concentration of the L-[ring-2-14C]-tryptophan and non-labelled L-tryptophan used in the assays is 20 μM and is added either with or without 68OC91 at time zero.
In Vivo
In vivo

The catabolism of L-[ring-2-14C]-tryptophan and a load dose of tryptophan (100 mg/kg) in vivo are inhibited by prior administration of 68OC91. Administration of 68OC91 alone produces marked increases in brain tryptophan, 5-HT and 5-HIAA. A load dose of tryptophan (100 mg/kg), producing increases in brain tryptophan 4-fold greater than that seen with 68OC91, does not increase brain 5-HT and 5-HIAA to levels greater than those seen with 68OC91 and produces a shorter-lasting increase in these parameters.[1]
Animal Research Animal Models Male Wistar rats
Dosages 15 mg/kg
Administration Oral gavage

Chemical Information & Solubility

Molecular Weight 238.26 Formula

C15H11FN2
CAS No. 163239-22-3 SDF --
Smiles C1=CC(=CN=C1)C=CC2=CNC3=C2C=CC(=C3)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 48 mg/mL ( (201.46 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 25 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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