产品
编 号：F083457
分子式：C22H25F3N4O3S
分子量：482.52
分子式：C22H25F3N4O3S
分子量：482.52
产品类型
规格
价格
是否有货
1mg
询价
询价
结构图
CAS No: 1228650-83-6
产品详情
生物活性：
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.
体内研究：
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. Pharmacokinetic parameters (p.o.):SpeciesDose(mg/kg)Cmax(ng/mL)AUClast(h*ng/mL)Oral bioavailability(%)
dogs6.71617588770.2
non-human primates7.2740306125.4
mice107420419
rats1010041615.3
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.
体内研究：
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. Pharmacokinetic parameters (p.o.):SpeciesDose(mg/kg)Cmax(ng/mL)AUClast(h*ng/mL)Oral bioavailability(%)
dogs6.71617588770.2
non-human primates7.2740306125.4
mice107420419
rats1010041615.3
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