中文名 | HPGDS inhibitor 1 |
英文名 | HPGDS inhibitor 1 |
别名 | 6-(3-氟苯基)-N-(1-(2,2,2-三氟乙基)哌啶-4-基)烟酰胺 6-(3-氟苯基)-N-[1-(2,2,2-三氟乙基)-4-哌啶基]-3-吡啶羧酰胺 6-(3-氟苯基)-N-[1-(2,2,2-三氟乙基)-4-哌啶基]-3-吡啶甲酰胺 |
英文别名 | CS-1438 MDK36122 HPGDS inhibitor 1 Prostaglandin D Synthase (hematopoietic-type) Inhibitor I 6-(3-fluorophenyl)-N-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)nicotinaMide 6-(3-Fluorophenyl)-N-[1-(2,2,2-trifluoroethyl)-4-piperidinyl]-3-pyridinecarboxamide 3-PYRIDINECARBOXAMIDE, 6-(3-FLUOROPHENYL)-N-[1-(2,2,2-TRIFLUOROETHYL)-4-PIPERIDINYL]- |
CAS | 1033836-12-2 |
化学式 | C19H19F4N3O |
分子量 | 381.37 |
溶解度 | 10毫米DMSO |
存储条件 | 2-8°C |
体外研究 | HPGDS inhibitor 1 has equal potency against purified HPGDS from human, rat, dog, and sheep (IC 50 , 0.5-2.3 nM). |
体内研究 | 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 |
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