JNJ-41443532  (Synonyms: CCR2 antagonist 5)

JNJ-41443532 (CCR2 antagonist 5) is a selective, orally active hCCR2 inhibitor with good binding affinity (IC₅₀=37 nM) and potent functional antagonism (chemotaxis IC₅₀=30 nM). JNJ-41443532 displays a K_i of 9.6 µM for mCCR2 binding. JNJ-41443532 can be used in the research of inflammatory disease^[1].

JNJ-41443532 (compound 8d) dose-dependently inhibits the influx of leukocytes, monocytes/macrophages and T-lymphocytes into the peritoneal cavity with an ED₅₀ of 3 mg/kg p.o. bid in a thioglycollate-induced peritonitis (TG) model^[1].
JNJ-41443532 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].
JNJ-41443532 has amendable oral bioavailability in dogs and primates. Pharmacokinetic parameters (p.o.)^[1]:

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

482.52

C₂₂H₂₅F₃N₄O₃S

1228650-83-6

固体

White to off-white

Room temperature in continental US; may vary elsewhere.

• [1]. Zhang X, et al. Discovery of a 4-Azetidinyl-1-thiazoyl-cyclohexane CCR2 Antagonist as a Development Candidate. ACS Med Chem Lett. 2012 Oct 8;3(12):1039-44.  [Content Brief]