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CCR2 antagonist 5

Catalog No. T27682Cas No. 1228650-83-6
Alias JNJ-41443532 Free Base, JNJ-41443532, JNJ41443532, JNJ 41443532

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 binds mCCR2 with a Ki of 9.6 µM, which can be used to study inflammatory diseases and diabetes. diseases and diabetes.

CCR2 antagonist 5

CCR2 antagonist 5

Purity: 98.79%
Catalog No. T27682Alias JNJ-41443532 Free Base, JNJ-41443532, JNJ41443532, JNJ 41443532Cas No. 1228650-83-6
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 binds mCCR2 with a Ki of 9.6 µM, which can be used to study inflammatory diseases and diabetes. diseases and diabetes.
Pack SizePriceAvailabilityQuantity
1 mg$100In Stock
5 mg$247In Stock
10 mg$372In Stock
25 mg$668In Stock
50 mg$949In Stock
100 mg$1,290In Stock
200 mg$1,730In Stock
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Purity:98.79%
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Product Introduction

Bioactivity
Description
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 binds mCCR2 with a Ki of 9.6 µM, which can be used to study inflammatory diseases and diabetes. diseases and diabetes.
Targets&IC50
CCR2 (human):37 nM (IC50), CCR2 (mouse):9.6 μM (Ki)
In vivo
CCR2 antagonist 5 (compound 8d) 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 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]
CCR2 antagonist 5 has amendable oral bioavailability in dogs and primates.[1]
AliasJNJ-41443532 Free Base, JNJ-41443532, JNJ41443532, JNJ 41443532
Chemical Properties
Molecular Weight482.52
FormulaC22H25F3N4O3S
Cas No.1228650-83-6
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 50 mg/mL (103.62 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0725 mL10.3623 mL20.7245 mL103.6226 mL
5 mM0.4145 mL2.0725 mL4.1449 mL20.7245 mL
10 mM0.2072 mL1.0362 mL2.0725 mL10.3623 mL
20 mM0.1036 mL0.5181 mL1.0362 mL5.1811 mL
50 mM0.0414 mL0.2072 mL0.4145 mL2.0725 mL
100 mM0.0207 mL0.1036 mL0.2072 mL1.0362 mL

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