1(2H)-Isoquinolinone, 2-methyl-6-[7-(1-piperidinylcarbonyl)-2-quinoxalinyl]-

Description

CAY10795 is a 15-hydroxy prostaglandin dehydrogenase (15-PGDH) inhibitor (IC₅₀ = 3 nM).¹ It increases prostaglandin E₂ (PGE₂; ) levels greater than 3-fold in IL-1β-stimulated A549 human lung cells when used at a concentration of 500 nM. CAY10795 reduces 15-PGDH activity in the colon of mice when administered at a dose of 20 mg/kg and limits decreases in body weight and colon length and reduces colon ulceration in a mouse model of ulcerative colitis induced by dextran sodium sulfate (DSS; ) when administered at a dose of 40 mg/kg. It also accelerates recovery of circulating neutrophils following whole-body radiation and bone marrow transplant in mice when administered at a dose of 10 mg/kg twice per day.

References

1. Hu, B., Toda, K., Wang, X., et al. Orally bioavailable quinoxaline inhibitors of 15-prostaglandin dehydrogenase (15-PGDH) promote tissue repair and regeneration J. Med. Chem. 65(22),15327-15343(2022).