CCR2-RA-[R]

SKU: orb1308479

Description

CCR2-RA-[R] is a potent allosteric antagonist of the C-C chemokine receptor type 2 (CCR2), exhibiting an IC50 of 103 nM. This small molecule inhibitor is a valuable research tool for studying CCR2-mediated pathways in vitro and for exploring its role in inflammatory and autoimmune disease models in vivo.

Research Area

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

Key Properties

• CAS Number: 512177-83-2
• MW: 351.8
• Purity: 99.70% (May vary between batches)
• Formula: C₁₈H₁₉ClFNO₃
• SMILES: CC(=O)C1=C(O)C(=O)N([C@@H]1C1CCCCC1)c1ccc(Cl)cc1F
• Target: CCR
• Solubility: DMSO:125 mg/mL (355.32 mM);H2O:< 0.1 mg/mL (insoluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (9.38 mM)

Bioactivity

• Target IC50:
  CCR2:103 nM (in U2OS-CCR2 cells)
• In Vitro:
  CCR2-RA-[R] inhibits CCR2 non-competitively by blocking activation-associated conformational changes and formation of the G protein-binding interface. CCR2-RA-[R] displaces [125I]CCL2 from CCR2 with an pIC50 value of 6.1. The pKD of CCR2-RA-[R] for CCR2 and CCR5 is 8.8±0.1 and 7.0±0.1, respectively. The chemokine receptor CCR2 is a G protein-coupled receptor that is involved in many diseases characterized by chronic inflammation, and therefore a large variety of CCR2 small molecule antagonists has been developed. The binding pocket of CCR2-RA-[R] is highly enclosed and possesses a balanced combination of hydrophobic and polar features, all of which favors pocket “druggability”.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CC chemokine receptor, CCR2 RA [R], CCR2RA[R], CCR-2-RA-[R], CCR2-RA-[R], CCR, CCR2, inhibit, Inhibitor

Compound Identifiers

PubChem CID

12093170