product name AZD1981
Description: AZD1981 is a potent, selective CRTh2 (DP2) 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.
References: Br J Pharmacol. 2013 Apr;168(7):1626-38; Bioorg Med Chem Lett. 2011 Nov 1;21(21):6288-92.
388.87
Formula
C19H17ClN2O3S
CAS No.
802904-66-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 11 mg/mL (28.3 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19423651
| In Vitro |
In vitro activity: AZD1981, as a potent antagonist in a disease relevant cell system, inhibits DK-PGD2-induced CD11b expression in human eosinophils with IC50 of 10 nM. AZD1981 blocks DP2-mediated shape change in human eosinophils and basophils in blood, as well as DP2-mediated chemotaxis of human Th2 cells and eosinophils. Moreover, AZD1981 also blocks the binding of [3H]PGD2 to mouse, rat, guinea pig, rabbit and dog recombinant DP2. Kinase Assay: Cell Assay: AZD1981 could block chemotaxis of DP2+ T-cell lines with a pIC50 value of 7.5±0.1. AZD1981 has been demonstrated to inhibit PGD2 binding to mouse, rat, rabbit, dog, guinea pig and human DP2. AZD1981 could inhibit shape change induced by DP2 in dog and guinea pig granulocytes as well as in human eosinophils and basophils in blood. |
|---|---|
| In Vivo | AZD1981 has high oral bioavailability in male sprague dawley rats. In guinea pig hind limb model, AZD1981 (100 nM) completely inhibits DK-PGD2-induced eosinophil mobilization. |
| Animal model | |
| Formulation & Dosage | |
| References | Br J Pharmacol. 2013 Apr;168(7):1626-38; Bioorg Med Chem Lett. 2011 Nov 1;21(21):6288-92. |
