High affinity antagonist for CCR1 and CCR3 receptors, partial agonist at CCR2 and CCR5 receptors
UCB35625 is a high affinity antagonist for CCR1 and CCR3 receptors. Also both UCB35625 and its enantiomer J113863 exhibit low binding affinity toward CCR2 and CCR5 where they activate three Gi and two G0 protein isoforms. UCB35625 does not activate G12 protein isoform. J113863 binding to CCR2 and CCR5 induce the recruitment of b-arrestin 2 whereas UCB35625 did not. J113863 and UCB35625 are biased ligands for the chemokine receptors CCR2 and CCR5.
Código de clase de almacenamiento
11 - Combustible Solids
Clase de riesgo para el agua (WGK)
WGK 3
Punto de inflamabilidad (°F)
Not applicable
Punto de inflamabilidad (°C)
Not applicable
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The Journal of biological chemistry, 280(6), 4808-4816 (2004-11-19)
The chemokine receptor CCR1 and its principal ligand, CCL3/MIP-1alpha, have been implicated in the pathology of several inflammatory diseases including rheumatoid arthritis, multiple sclerosis, and asthma. As such, these molecules are the focus of much research with the ultimate aim
The Journal of biological chemistry, 292(2), 575-584 (2016-11-30)
Biased agonism at G protein-coupled receptors constitutes a promising area of research for the identification of new therapeutic molecules. In this study we identified two novel biased ligands for the chemokine receptors CCR2 and CCR5 and characterized their functional properties.
The Journal of biological chemistry, 275(34), 25985-25992 (2000-06-16)
We describe a small molecule chemokine receptor antagonist, UCB35625 (the trans-isomer J113863 published by Banyu Pharmaceutical Co., patent WO98/04554), which is a potent, selective inhibitor of CCR1 and CCR3. Nanomolar concentrations of UCB35625 were sufficient to inhibit eosinophil shape change
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