Home Metabolism PGDS inhibitor AT-56 For research use only.

AT-56

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

AT-56 Chemical Structure

CAS: 162640-98-4

Purity & Quality Control

Batch: S967801 DMSO] 80 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 98.52%
98.52

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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
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]
Cell Research 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.
In Vivo
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]
Animal Research 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
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05102123 Not yet recruiting Smoking (Tobacco) Addiction|Smoking Cessation Population Health Research Institute December 1 2023 Phase 3
NCT05707208 Recruiting Chronic Pain Sustained Therapeutics Inc. March 21 2023 Phase 2
NCT04102800 Active not recruiting 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
NCT03005379 Terminated Clostridium Difficile Infection VA Office of Research and Development November 15 2018 Phase 2|Phase 3

Chemical lnformation & Solubility

Molecular Weight 397.52 Formula

C25H27N5
CAS No. 162640-98-4 SDF --
Smiles C1CN(CCC1=C2C3=CC=CC=C3C=CC4=CC=CC=C42)CCCCC5=NNN=N5
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 80 mg/mL ( (201.24 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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