INCB 3284

SKU: orb1709417

Description

INCB 3284 is a potent, selective, and orally bioavailable antagonist of the human CCR2 receptor, blocking its interaction with MCP-1. It is a valuable research tool for investigating CCR2-mediated pathways in inflammatory diseases and has been utilized in preclinical studies, including models of hemorrhagic shock.

Research Area

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

Key Properties

• CAS Number: 887401-92-5
• MW: 520.54
• Purity: 99.82% (May vary between batches)
• Formula: C₂₆H₃₁F₃N₄O₄
• SMILES: COc1ccc(cn1)[C@@]1(O)CC[C@@H](CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F
• Target: CCR
• Solubility: DMSO:60 mg/mL (115.26 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.84 mM);H2O:< 0.1 mg/mL (insoluble)

Bioactivity

• Target IC50:
  MCP-1-hCCR2:3.7 nM|K+ channel (hERG):84 μM
• In Vivo:
  INCB 3284 (1 mg/kg/day, intraperitoneal injection) or C021 significantly improved the neurological outcomes in AOM-treated mice, reduced microglial activation, decreased phosphorylation of ERK1/2, and attenuated the upregulation of cytokines induced by AOM.
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• In Vitro:
  INCB3284 exhibited an IC50 of 3.7 nM for antagonizing the binding of monocyte chemoattractant protein-1 to hCCR2, an IC50 of 4.7 nM for antagonizing chemotactic activity, and an IC50 of 84 μM for inhibiting hERG potassium currents.
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Storage & Handling

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

Alternative Names

INCB 3284, INCB3284, INCB-3284, MCP-1-hCCR2, CCR2

Compound Identifiers

PubChem CID

11527661