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MDK36122 selectively blocks HPGDS (IC50s = 0.7 and 32 nM in enzyme and cellular assays, respectively) with little activity against the related human enzymes L-PGDS, mPGES, COX-1, COX-2, and 5-LOX.
Oral administration of HPGDS inhibitor 1 blocked PGD2 production in the rat spleen; inhibition of PGD2 was inversely correlated with the plasma concentration of HPGDS inhibitor 1 in a time and dose-dependent manner. Spleen PGD2 levels fall as HPGDS inhibitor 1 plasma levels increase over time; PGD2 levels return to baseline levels as HPGDS inhibitor 1 plasma levels decline.
| Molecular Weight | 381.37 |
| Formula | C19H19F4N3O |
| CAS Number | 1033836-12-2 |
| Form | Solid |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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| SAR191801
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