15-PGDH-IN-1

15-PGDH-IN-1 is a potent and orally active 15-PGDH inhibitior. 15-PGDH-IN-1 has inhibition activity against recombinant human 15-PGDH with an IC50 value of 3 nM. 15-PGDH-IN-1 can be used for the research of tissue repair and regeneration[1].

Signaling Pathways >> Metabolic Enzyme/Protease >> 15-PGDH

Research Areas >> Metabolic Disease

IC50: 3 nM (15-PGDH)[1]

15-PGDH-IN-1 (compound 49) has inhibition activity against recombinant human 15-PGDH with an IC50 value of 3 nM[1]. 15-PGDH-IN-1 (4, 20, 100, 500, 2500 nM) induces PGE2 in A549 cells at 20 nM[1].

15-PGDH-IN-1 (compound 49) (5, 10, 20, 40 mg/kg; IV, IP, PO) shows potent inhibition of 15-PGDH, good oral bioavailability, and protective activity in mouse models of ulcerative colitis and recovery from bone marrow transplantation[1]. Animal Model: CD1 Mice (female)[1] Dosage: 5, 10 mg/kg Administration: IV, IP, PO Result: Showed a low Cmax value when dosed orally versus IP, but the AUC was only reduced by half and had good oral bioavailability (63%). Animal Model: C57Bl/6 mice[1] Dosage: 5, 20, 40 mg/kg Administration: IP, Oral Result: Showed elevation of PGE2 levels in colon and lung inhibited 15-PGDH enzymatic activity in the colon. Animal Model: DSS model[1] Dosage: 10, 40 mg/kg Administration: IP (10 mg/kg BID) or PO (40 mg/kg BID) Result: Showed protection in the mouse DSS model of ulcerative colitis.