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AT-56 is an orally active inhibitor of lipocalin-type prostaglandin D synthase (L-PGDS) (Ki = 75 μM, IC50 = 95 μM). AT-56 Inhibits the production of PGD2 from PGH2 in vitro, with no effect on PGE2 or PGF2α production. AT-56 inhibited human and mouse L-PGDSs in a concentration (3-250 microm)-dependent manner. AT-56 inhibits 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. AT-56 did not inhibit the binding of 13-cis-retinoic acid,which is a nonsubstrate lipophilic ligand, to L-PGDS.
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Source | BMC Gastroenterol (2015). Figure 7. AT-56 |
| Method | inflammatory | |
| Cell Lines | Primary culture of the rat ENS | |
| Concentrations | 95 μM | |
| Incubation Time | 24 h | |
| Results | LPS was used to induce an inflammatory stress. We showed that 1/ the ENS produced PGD2 in response to LPS, and 2/ at the IC50 concentration (95 μM) AT-56 reduced PGD2 production in response to LPS |
| Molecular Weight | 397.52 |
| Formula | C25H27N5 |
| CAS Number | 162640-98-4 |
| Solubility (25°C) | DMSO 10 mM |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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