产品
编 号:F013159
分子式:C26H26Cl2N2O7S
分子量:581.46
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
AMG-009 is a potent antagonist of prostaglandin D2, with IC50 of 3 nM and 12 nM for CRTH2 and DP receptors, respectively.

体内研究:
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 Kb of 82 nM.

体外研究:
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).
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