CCR2 antagonist 5

Research use only, not for human use.

CCR2 antagonist 5 (JNJ-41443532) is a selective and orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM).

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 Ki of 9.6 μM for mCCR2 binding. JNJ-41443532 can be used in the research of inflammatory disease.

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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.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.JNJ-41443532 has amendable oral bioavailability in dogs and primates.

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Autophagy

CCR

CCR

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1228650-83-6

482.52

C22H25F3N4O3S

>98% (HPLC)

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N(C(CNC(=O)C1=CC(C(F)(F)F)=CC=C1)=O)C2CN([C@@H]3CC[C@@](O)(CC3)C4=CN=CS4)C2

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(-20℃)

With Ice Pack

≥ 2 years