CCR2 antagonist 5

SKU: orb1700276

Description

JNJ-41443532 is a potent, selective, and orally bioavailable antagonist of human CCR2 (IC₅₀=37 nM) with demonstrated efficacy in inhibiting monocyte chemotaxis. Its significant species selectivity makes it a valuable pharmacological tool for studying CCR2-mediated pathways in preclinical models of inflammation and metabolic disorders like diabetes.

Research Area

Immunology & Inflammation, Immunology & Inflammation; Pharmacology & Drug Discovery, Infectious Disease & Virology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1228650-83-6
• MW: 482.52
• Purity: 99.98% (May vary between batches)
• Formula: C₂₂H₂₅F₃N₄O₃S
• 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
• Target: CCR
• Solubility: DMSO:50 mg/mL (103.62 mM);10% DMSO+40% PEG300+5% Tween-80+45% Saline:2.5 mg/mL (5.18 mM)

Bioactivity

• Target 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. 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. CCR2 antagonist 5 has amendable oral bioavailability in dogs and primates.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

JNJ41443532, JNJ-41443532, JNJ-41443532 Free Base, JNJ 41443532, CCR2, CCR2 antagonist 5

Compound Identifiers

PubChem CID

46208367