RS 102895 Hydrochloride is a CKR-2B (CCR2)-selective chemokine receptor antagonist (IC|50|values are 0.36 and 17.8 μM for inhibition of human recombinant CKR-2B and CKR-1 (CCR2b and CCR1 receptors) respectively). Blocks MCP-1-stimulated calcium influx and chemotaxis with IC|50|values of 32 nM and 1.7 μM respectively. Inhibits α|1A|-AR, α|1D|-AR and SR-1A (α1A, α1D and 5-HT|1A|receptors).
Associated Targets(Human)
CCR2TchemC-C chemokine receptor type 2 (1 Activities)
1.Mirzadegan T, Diehl F, Ebi B, Bhakta S, Polsky I, McCarley D, Mulkins M, Weatherhead GS, Lapierre JM, Dankwardt J et al.. (2000) 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 Chem, 275 (33):(25562-71). [PMID:10770925][10.1021/op500134e]
2.Clark RD, Caroon JM, Kluge AF, Repke DB, Roszkowski AP, Strosberg AM, Baker S, Bitter SM, Okada MD. (1983) Synthesis and antihypertensive activity of 4'-substituted spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-ones.. J Med Chem, 26 (5):(657-61). [PMID:6842505][10.1021/op500134e]
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