680C91

Catalog No.S8997 Batch:S899701

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Technical Data

Formula

C15H11FN2
Molecular Weight 238.26 CAS No. 163239-22-3
Solubility (25°C)* In vitro DMSO 48 mg/mL (201.46 mM)
Ethanol 25 mg/mL (104.92 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

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 Assay:

[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 Study:

[1]
  • Animal Models

    Male Wistar rats

  • Dosages

    15 mg/kg

  • Administration

    Oral gavage

Selleck's 680C91 has been cited by 3 publications

Targeting Tryptophan Catabolism in Ovarian Cancer to Attenuate Macrophage Infiltration and PD-L1 Expression [ Cancer Res Commun, 2024, 4(3):822-833] PubMed: 38451784
Serotonin reduction in post-acute sequelae of viral infection [ Cell, 2023, 186(22):4851-4867.e20] PubMed: 37848036
Identification and Characterization of a Novel Dual Inhibitor of Indoleamine 2,3-dioxygenase 1 and Tryptophan 2,3-dioxygenase [ Int J Tryptophan Res, 2022, 15:11786469221138456] PubMed: 36467776

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.