AMG-009

Research use only, not for human use.

AMG-009 is a selective and potent dual antagonist of CRTH2 and DP, with an IC50 value of 3 nM for CRTH2 and 12 nM for DP receptors.

AMG-009 is a potent antagonist of prostaglandin D2, with IC50 of 3 nM and 12 nM for CRTH2 and DP receptors, respectively.

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).

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.

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Cell Cycle/DNA Damage

GPR

GPR | Prostaglandin Receptor

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1027847-67-1

581.47

C26H26Cl2N2O7S

>98% (HPLC)

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O=C(O)CC1=CC=C(OC2=CC=C(C=C2NS(=O)(=O)C3=CC=C(Cl)C=C3Cl)C(=O)NCCCC)C(OC)=C1

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(-20℃)

With Ice Pack

≥ 2 years