AT-56

Catalog No.S9678

For research use only.

AT-56 is an orally active and selective inhibitor of lipocalin-type prostaglandin (PG) D synthase (L-PGDS) with Ki of 75 μM and IC50 of 95 μM.

AT-56 Chemical Structure

CAS No. 162640-98-4

Purity & Quality Control

Choose Selective PGDS Inhibitors

Biological Activity

Description AT-56 is an orally active and selective inhibitor of lipocalin-type prostaglandin (PG) D synthase (L-PGDS) with Ki of 75 μM and IC50 of 95 μM.
Targets
L-PGDS [1]
(Cell-free assay)
L-PGDS [1]
(Cell-free assay)
75 μM(Ki) 95 μM
In vitro

AT-56 inhibits human and mouse L-PGDSs in a concentration (3–250 μm)-dependent manner. AT-56 inhibits the L-PGDS activity in a competitive manner against the substrate PGH2 (Km = 14 μm) with a Ki value of 75 μm. AT-56 inhibits the production of PGD2 by L-PGDS-expressing human TE-671 cells after stimulation with Ca2+ ionophore (5 μm A23187) with an IC50 value of about 3 μm without affecting their production of PGE2 and PGF2α.[1]

In vivo

Orally administered AT-56 (<30 mg/kg body weight) decreases the PGD2 production to 40% in the brain of H-PGDS-deficient mice after a stab wound injury in a dose-dependent manner without affecting the production of PGE2 and PGF2α and also suppresses the accumulation of eosinophils and monocytes in the bronco-alveolar lavage fluid from the antigen-induced lung inflammation model of human L-PGDS-transgenic mice.[1]

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: TE-671 cells, MEG-01S cells
  • Concentrations: 0 - 100 μM
  • Incubation Time: 10 min
  • Method:

    TE-671 (1×106 cells/well) and MEG-01S (5×105 cells/well) are seeded into multiplates and cultured in Dulbecco's modified Eagle's medium supplemented with 10% heat-inactivated fetal bovine serum, 4 mM L-glutamine, 4.5 g/liter glucose, 100 units/ml penicillin, and 100 μg/ml streptomycin sulfate under a 5% CO2 atmosphere at 37 ℃. MEG-01S cells are caused to differentiate by treatment with 12-O-tetradecanoylphorbol-13-acetate to express H-PGDS and COX-1. After the cells have been cultured for 1 day, AT-56 is added to them at different doses ranging from 0 to 100 μM, and the cells are then incubated at 37 ℃ for 10 min. Thereafter, they are stimulated with a calcium ionophore, A23187 (5 μM), at 37 ℃ for 15 min. The culture media were harvested and centrifuged at 10,000 × g for 5 min to remove the cells, and the supernatant is removed and stored at 80 ℃ until the measurements of PGs can be made.

Animal Research:

[1]

  • Animal Models: H-PGDS KO mice (14–16-week-old males or females weighing 25–30 g, C57BL/6 strain)
  • Dosages: 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg
  • Administration: Oral gavage

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 397.52
Formula

C25H27N5

CAS No. 162640-98-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CN(CCC1=C2C3=CC=CC=C3C=CC4=CC=CC=C42)CCCCC5=NNN=N5

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04102800 Recruiting Drug: Benralizumab Asthma NHS Greater Glasgow and Clyde|University of Glasgow|AstraZeneca|Queen''s University Belfast|Bosch Healthcare Solutions GmbH|InHealthcare|University of Leicester|University of Plymouth|Vitalograph September 30 2019 Phase 4
NCT02494479 Completed Drug: Prurisol|Drug: Placebo Plaque Psoriasis Cellceutix Corporation August 2015 Phase 2
NCT02195232 Completed Drug: Isoquercetin Thromboembolism of Vein VTE in Colorectal Cancer|Thromboembolism of Vein in Pancreatic Cancer|Thromboembolism of Vein in Non-small Cell Lung Cancer Jeffrey Zwicker MD|Quercegen Pharmaceuticals|National Heart Lung and Blood Institute (NHLBI)|Dana-Farber Cancer Institute January 2015 Phase 2|Phase 3
NCT01925417 Completed Biological: RBX2660 (microbiota suspension) Recurrent Clostridium Difficile Infection Rebiotix Inc. August 2013 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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