1. Immunology/Inflammation
  2. PGE synthase
  3. AT-56

AT-56 

Cat. No.: HY-13988
Handling Instructions

AT-56 is a potent, selective and orally active inhibitor of lipocalin-type prostaglandin D synthase (L-PGDS), with an IC50 of 95 μM and Ki of 75 μM. AT-56 could selectively suppress the drowsiness or pain reaction mediated by L-PGDS-catalyzed PGD2.

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AT-56 Chemical Structure

AT-56 Chemical Structure

CAS No. : 162640-98-4

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Description

AT-56 is a potent, selective and orally active inhibitor of lipocalin-type prostaglandin D synthase (L-PGDS), with an IC50 of 95 μM and Ki of 75 μM. AT-56 could selectively suppress the drowsiness or pain reaction mediated by L-PGDS-catalyzed PGD2[1].

IC50 & Target

IC50: 95 μM (L-PGDS); Ki: 75 μM (L-PGDS)[1]

In Vitro

AT-56 (1-30 μM; 10 minutes) dose-dependently inhibits the production of PGD2 in L-PGDS-expressing human medulloblastoma TE-671 cells with an IC50 of about 3 μM[1].

In Vivo

AT-56 ( 1-30 mg/kg; p.o.) suppresses the PGD2 production in the stab-wounded brain[1].
AT-56 (1-10 mg/kg; p.o.) suppresses the L-PGDS-mediated allergic airway inflammation in mice[1].
AT-56 (10 mg/kg; p.o.) exhibits Cmax (2.15 μg/ml), half-life (1.71 h) and high oral bioavailability (82%)[1].

Animal Model: H-PGDS KO mice (14-16weeks, 25-30 g, C57BL/6 strain) with a stab wound brain injury[1]
Dosage: 0, 1, 3, 10, 30 mg/kg
Administration: P.o. 1 h before the stab wound injury
Result: Inhibited the L-PGDS reaction in the brain.
Decreased the total amount of PGD2 in the brain to 40% with 30 mg/kg AT-56.
Animal Model: Human L-PGDS-overexpressing TG mice (males, 14-16 weeks, 25-30 g)[1]
Dosage:  0, 1, 10 mg/kg
Administration: P.o. 1 h before and 24 h after the antigen exposure
Result: Prevented the eosinophil infiltration by inhibiting transgened human L-PGDS.
Animal Model: Male C57BL/6 mice (7 weeks, 22-26 g)[1]
Dosage: 10 mg/kg for p.o. and 2 mg/kg for i.v. (Pharmacokinetic Analysis)
Administration: P.o. and i.v. administration
Result: Oral bioavailability (82%); Cmax (2.15 μg/ml); T1/2 (1.71 h, p.o.); T1/2 (2.35 h, i.v.).
Molecular Weight

397.52

Formula

C₂₅H₂₇N₅

CAS No.

162640-98-4

SMILES

N1(CCCCC2=NNN=N2)CC/C(CC1)=C3C4=CC=CC=C4C=CC5=CC=CC=C/35

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

AT-56AT56AT 56PGE synthaseProstaglandin E synthaseLipocalin-typeprostaglandinDsynthasePGL-PGDSdrowsinessinflammatoryInhibitorinhibitorinhibit

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