Name | 2-[4-[4-(butylcarbamoyl)-2-[(2,4-dichlorophenyl)sulfonylamino]phenoxy]-3-methoxyphenyl]acetic acid |
---|---|
Synonyms | amg-009 |
Description | AMG-009 is a potent antagonist of prostaglandin D2, with IC50 of 3 nM and 12 nM for CRTH2 and DP receptors, respectively. |
---|---|
Related Catalog | |
Target |
CRTH2/DP2 Receptor:3 nM (IC50) |
In Vitro | AMG-009 inhibits PGD2-induced down-modulation of CRTH2 on CD16 negative granulocytes (eosinophils) in human whole blood with a Ki of 1 nM. AMG 009 also inhibits PGD2-induced cAMP response mediated by DP in platelets in 80% human whole blood with a Ki of 148 nM. AMG 009 inhibits guinea pig CRTH2 receptors (IC50=3 nM) and a PGD2-induced cAMP response assay with cells expressing the guinea pig DP receptors (Ki=131 nM)[1]. |
In Vivo | AMG 009 (3, 10 or 30 mg/kg, s.c.) results in a dose dependent decrease in airway resistance provoked by PGD2 aerosol in an acute guinea pig model[1]. In a guinea pig model of PGD2-induced airway constriction, AMG 009 significantly improves DP potency, with Kb of 82 nM[2]. |
References |
Molecular Formula | C26H26Cl2N2O7S |
---|---|
Molecular Weight | 581.46500 |
Exact Mass | 580.08400 |
PSA | 142.90000 |
LogP | 7.48070 |