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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 | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $100 | In Stock | In Stock | |
| 5 mg | $247 | In Stock | In Stock | |
| 10 mg | $372 | In Stock | In Stock | |
| 25 mg | $668 | In Stock | In Stock | |
| 50 mg | $949 | In Stock | In Stock | |
| 100 mg | $1,290 | In Stock | 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 (mouse):9.6 μM (Ki), CCR2 (human):37 nM (IC50) |
| 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] |
| Synonyms | 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/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 50 mg/mL (103.62 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2.5 mg/mL (5.18 mM), Sonication is recommeded. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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