Molecular Formula | C19H19F4N3O |
Molar Mass | 381.37 |
Solubility | 10 mM in DMSO |
Storage Condition | 2-8°C |
In vitro study | HPGDS inhibitor 1 has equal potency against purified HPGDS from human, rat, dog, and sheep (IC 50 , 0.5-2.3 nM). |
In vivo study | HPGDS inhibitor 1 (compound 8; 1 mg/kg) has excellent PK characteristics with 76% bioavailability, and the T 1/2 is 4.1 hours in rats. Rats dosed orally with 1 mg/kg and 10 mg/kg HPGDS inhibitor 1 (compound 8) are sacrificed at various times. Oral administration of HPGDS inhibitor 1 blocks PGD2 production in the rat spleen; inhibition of PGD2 is inversely correlated with the plasma concentration of HPGDS inhibitor 1 in a time- and dose-dependent manner. HPGDS inhibitor 1 (compound 8; 1 mg/mL) illustrates efficacy in an in vivo sheep model of asthma. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.622 ml | 13.111 ml | 26.221 ml |
5 mM | 0.524 ml | 2.622 ml | 5.244 ml |
10 mM | 0.262 ml | 1.311 ml | 2.622 ml |
5 mM | 0.052 ml | 0.262 ml | 0.524 ml |