AMG-009,1027847-67-1

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AMG-009

CAS No. : 1027847-67-1

MCE 国际站：AMG-009

产品活性：AMG-009 是 prostaglandin D2 的有效拮抗剂，对 CRTH2 和 DP 受体的 IC₅₀ 值分别为 3 nM 和 12 nM。

研究领域：GPCR/G Protein

作用靶点：Prostaglandin Receptor

In Vitro: AMG-009 inhibits PGD2-induced down-modulation of CRTH2 on CD16 negative granulocytes (eosinophils) in human whole blood with a K_i of 1 nM. AMG 009 also inhibits PGD2-induced cAMP response mediated by DP in platelets in 80% human whole blood with a K_i 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 (K_i=131 nM).

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. In a guinea pig model of PGD2-induced airway constriction, AMG 009 significantly improves DP potency, with K_b of 82 nM.

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