Home Metabolism PGDS inhibitor AT-56

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AT-56 PGDS inhibitor

Cat.No.S9678

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 PGDS inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 397.52

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 80 mg/mL (201.24 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 397.52 Formula

C25H27N5

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 162640-98-4 -- Storage of Stock Solutions

Synonyms N/A Smiles C1CN(CCC1=C2C3=CC=CC=C3C=CC4=CC=CC=C42)CCCCC5=NNN=N5

Mechanism of Action

Targets/IC50/Ki
L-PGDS
(Cell-free assay)
75 μM(Ki)
L-PGDS
(Cell-free assay)
95 μM
In vitro

AT-56 inhibits human and mouse L-PGDSs in a concentration (3–250 μm)-dependent manner. This compound inhibits the L-PGDS activity in a competitive manner against the substrate PGH2 (Km = 14 μm) with a Ki value of 75 μm. It 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.
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 this compound 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.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05102123 Recruiting
Smoking (Tobacco) Addiction|Smoking Cessation
Population Health Research Institute
 January 15 2024 Phase 3
NCT05707208 Recruiting
Chronic Pain
Sustained Therapeutics Inc.
 March 21 2023 Phase 2
NCT04102800 Completed
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

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