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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 Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $100 | In Stock | |
5 mg | $247 | In Stock | |
10 mg | $372 | In Stock | |
25 mg | $668 | In Stock | |
50 mg | $949 | In Stock | |
100 mg | $1,290 | In Stock | |
200 mg | $1,730 | In Stock |
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] |
Alias | JNJ-41443532 Free Base, JNJ-41443532, JNJ41443532, JNJ 41443532 |
Molecular Weight | 482.52 |
Formula | C22H25F3N4O3S |
Cas No. | 1228650-83-6 |
Smiles | N(C(CNC(=O)C1=CC(C(F)(F)F)=CC=C1)=O)C2CN([C@@H]3CC[C@@](O)(CC3)C4=CN=CS4)C2 |
Relative Density. | 1.43 g/cm3 (Predicted) |
Storage | Powder: -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
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