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Description: AZD1981 is a novel potent and selective CRTh2 (Chemoattractant receptor-homologous molecule expressed on TH2 cells; DP2-Prostaglandin D2 receptor 2, ) receptor antagonist with IC50 of 4 nM, it displayed > 1000-fold selectivity over more than 340 other enzymes and receptors, including DP1. AZD1981 has shown to inhibit eosinophil migration with a pIC50 value of 7.6+/-0.1. It could block chemotaxis of DP2+ T-cell lines with a pIC50 value of 7.5+/-0.1. AZD1981 inhibited PGD2 by binding to mouse, rat, rabbit, dog, guinea pig and human DP2. AZD1981 is currently being developed for the treatment of asthma.
References: Br J Pharmacol. 2013 Apr; 168(7):1626-38; Bioorg Med Chem Lett. 2011 Nov 1; 21(21):6288-92.
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