CCR2 antagonist5 is a selective, orally activehCCR2inhibitor with good binding affinity (IC₅₀=37 nM) and potent functional antagonism (chemotaxis IC₅₀=30 nM).CCR2 antagonist5 displays a K_iof 9.6 μM for mCCR2 binding.CCR2 antagonist5 can be used in the research of inflammatory disease^[1].

CCR2 antagonist 5 (compound 8d) dose-dependently inhibits the influx of leukocytes, monocytes/macrophages and T-lymphocytes into the peritoneal cavity with an ED₅₀of 3 mg/kg p.o. bid in a thioglycollate-induced peritonitis (TG) model^[1].
CCR2 antagonist 5 has good CV safety profile. It does not induce dose-dependent or notable effects on most cardiohemodynamic, functional respiratory and electrophysiological parameters up to 10 mg/kg (i.v.) with plasma level at 70 μM in an anesthetized dog^[1].
CCR2 antagonist 5 has amendable oral bioavailability in dogs and primates. Pharmacokinetic parameters (p.o.)^[1]:

482.52

C₂₂H₂₅F₃N₄O₃S

1228650-83-6

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