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AT-56

Chemical Structure : AT-56

CAS No.: 162640-98-4

AT-56 (L-PGDS inhibitor AT-56)

Catalog No.: PC-38455Not For Human Use, Lab Use Only.

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

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Biological Activity

AT-56 is an orally active, selective inhibitor of lipocalin-type prostaglandin D synthase (L-PGDS) with Ki of 75 uM, IC50 of 95 uM.
AT-56 inhibited the L-PGDS activity in a competitive manner against the substrate PGH2 (Km = 14 μM) with a Ki value of 75 μM but did not inhibit the binding of 13-cis-retinoic acid, a nonsubstrate lipophilic ligand, to L-PGDS.
AT-56 occupied the catalytic pocket, but not the retinoid-binding pocket, of L-PGDS.
AT-56 inhibited 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 3 uM.
Orally administered AT-56 (<30 mg/kg body weight) decreased the PGD2 production to 40% in the brain of H-PGDS-deficient mice, without affecting the production of PGE2 and PGF2α.
AT-56 also suppressed 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.

Physicochemical Properties

M.Wt 397.526
Formula C25H27N5
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-(5H-Dibenzo[a,d]cyclohepten-5-ylidene)-1-[4-(2H-tetrazol-5-yl)butyl]-piperidine

References

1. Daisuke Irikura, et al. J Biol Chem. 2009 Mar 20;284(12):7623-30.

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