Biological descriptionSelective CCR2 receptor antagonist (IC50 values are 360 nM and 17.8 μM at CCR2 and CCR1 receptors, respectively). Inhibits MCP-1 and MCP-3 stimulated calcium influx (IC50 values are 32 and 130 nM, respectively). Active in vivo.
Chemical name1'-[2-[4-(Trifluoromethyl)phenyl]ethyl]spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one hydrochloride
Storage instructionsStore at Room Temperature. Store under desiccating conditions. The product can be stored for up to 12 months.
Solubility overviewSoluble in DMSO to 50 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
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Rehni AK & Singh TG Involvement of CCR-2 chemokine receptor activation in ischemic preconditioning and postconditioning of brain in mice. Cytokine60:83-9 (2012).
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Mirzadegan T et al. Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists: binding to a common chemokine receptor motif within the helical bundle. J Biol Chem275:25562-71 (2000).
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