680C91

Catalog No.S8997

For research use only.

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

680C91 Chemical Structure

CAS No. 163239-22-3

Purity & Quality Control

Choose Selective IDO/TDO Inhibitors

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

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]

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]

Protocol (from reference)

Cell Research:

[1]

  • 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.

Animal Research:

[1]

  • Animal Models: Male Wistar rats
  • Dosages: 15 mg/kg
  • Administration: Oral gavage

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 238.26
Formula

C15H11FN2

CAS No. 163239-22-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC(=CN=C1)C=CC2=CNC3=C2C=CC(=C3)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy 680C91 | 680C91 supplier | purchase 680C91 | 680C91 cost | 680C91 manufacturer | order 680C91 | 680C91 distributor