LAS191859

Description: LAS191859 is a CRTH2/DP2 antagonist with IC50 values of 7.6, 9.58, 14 and 15.5nM for recombinant guinea pig, human, rat and mouse CRTH2/DP2 receptors, respectively. LAS191859 has a residence time half-life of 21h at CRTh2 that translates into a long-lasting in vivo efficacy that is independent of plasma levels. Target: Others. Smiles: C(N(C(=O)C1CC1)CC)C2=C(N3C=4C(C(CC(O)=O)=C3)=CC=C(C)N4)C=CC(C(F)(F)F)=C2. References: Calbet M, Andrés M, Armengol C, Bravo M, Eichhorn P, López R, García-González V, Roberts R, Miralpeix M. Pharmacological characterization of CRTh2 antagonist LAS191859: Long receptor residence time translates into long-lasting in vivo efficacy. Pharmacol Res. 2016 Sep,111:208-216. doi: 10.1016/j.phrs.2016.06.014. Epub 2016 Jun 16. PubMed PMID: 27317944.