CH0076989 

CH0076989 is a specific CCR3 agonist. CH0076989 activates eosinophils and transfectants expressing both wild-type CCR3 and a CCR1:CCR3 chimaeric receptor lacking the CCR3 amino-terminus. CH0076989 has a direct interaction with the transmembrane helices of CCR3, supported by the complete loss of its activity due to mutations of the residues Y41, Y113 and E287. CH0076989 can be used for the study of inflammation and allergic diseases (such as asthma)^[1].

CH0076989 (0.01-10 μM, 4 min) induces eosinophil shape change in a dose dependent manner^[1].
CH0076989 (0.0001-10 μM, 5 h) elicits chemotaxis in CCR3-transfected L1.2 cells with an optimal concentration of 1 μM, but has no effect on CCR1-transfected cells^[1].
CH0076989 (10 μM, 20 min) induces CCR3 internalization in CCR3-transfected L1.2 cells, which is dose-dependently inhibited by cis-J-113863 (UCB35625) (HY-103360A)^[1].
CH0076989 (0.0001-10 μM, 5 h) induces chemotaxis in L1.2 cells transfected with the CCR1:CCR3 chimeric receptor (Chi-1)^[1].
CH0076989 (0.0001-10 μM, 5 h) fails to induce chemotaxis in L1.2 cells transfected with Y41A, Y113A, or E287Q mutant CCR3^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

530.25

C₂₄H₂₂Br₂N₂O₂

954371-52-9

BrC1=CC(NC(CC2=C3C=COC3=CC=C2)=O)=CC=[N+]1CCCC4=CC=CC=C4.[Br-]

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• [1]. Wise EL, et al. Small molecule receptor agonists and antagonists of CCR3 provide insight into mechanisms of chemokine receptor activation. J Biol Chem. 2007 Sep 21;282(38):27935-43.  [Content Brief]