AT-56

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Chemical Information

Product name：AT-56	Purity：98% min
CAS NO：162640-98-4	Solubility：
Molecular Formula：C₂₅H₂₇N₅	Package：Package according to customer requirements
Molecular Weight：397.515	Storage：Store at -20℃

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Remarks

AT-56 is a selective, competitive, and highly bioavailable inhibitor of lipocalin-type prostaglandin D synthase (L-PGDS) with a Ki value of 75 µM. AT-56 inhibited human and mouse L-PGDSs in a concentration (3-250 microm)-dependent manner but did not affect the activities of hematopoietic PGD synthase (H-PGDS), cyclooxygenase-1 and -2, and microsomal PGE synthase-1. AT-56 inhibited the L-PGDS activity in a competitive manner against the substrate PGH(2) (K(m) = 14 microm) with a K(i) value of 75 microm but did not inhibit the binding of 13-cis-retinoic acid, a nonsubstrate lipophilic ligand, to L-PGDS.

References

1: Irikura D, Aritake K, Nagata N, Maruyama T, Shimamoto S, Urade Y. Biochemical, functional, and pharmacological characterization of AT-56, an orally active and selective inhibitor of lipocalin-type prostaglandin D synthase. J Biol Chem. 2009 Mar 20;284(12):7623-30. doi: 10.1074/jbc.M808593200. PubMed PMID: 19131342; PubMed Central PMCID: PMC2658056.

2: Le Loupp AG, Bach-Ngohou K, Bourreille A, Boudin H, Rolli-Derkinderen M, Denis MG, Neunlist M, Masson D. Activation of the prostaglandin D2 metabolic pathway in Crohn's disease: involvement of the enteric nervous system. BMC Gastroenterol. 2015 Sep 4;15:112. doi: 10.1186/s12876-015-0338-7. PubMed PMID: 26338799; PubMed Central PMCID: PMC4558965.