产品
编 号:F750248
分子式:C24H22N4O2
分子量:398.46
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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生物活性:
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.

体内研究:
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.Animal Model:CD1 Mice (female)
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
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
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.

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