| Bioactivity | 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]. | |||||||||
| Target | IC50: 95 μM (L-PGDS); Ki: 75 μM (L-PGDS) | |||||||||
| Invitro | 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: | |||||||||
| Name | AT-56 | |||||||||
| CAS | 162640-98-4 | |||||||||
| Formula | C25H27N5 | |||||||||
| Molar Mass | 397.52 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Irikura D, et, al. 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. |