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. |
