CCR2-RA-[R]

SKU: orb1941037

Description

A potent, selective, allosteric CCR2 antagonist with IC50 of 103 nM.

Key Properties

• CAS Number: 512177-83-2
• MW: 351.802
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₉ClFNO₃
• SMILES: O=C1N(C2=CC=C(Cl)C=C2F)[C@H](C3CCCCC3)C(C(C)=O)=C1O
• Target: Chemokine Receptor
• Solubility: DMSO : ≥ 125 mg/mL 355.32 mM; H2O : < 0.1 mg/mL

Bioactivity

• In Vitro:
  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. 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. CCR2-RA-[R] inhibits CCR2 non-competitively by blocking activation-associated conformational changes and formation of the G protein-binding interface. 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: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CCR2-RA [R]

Quick Database Links

Gene Symbol

Chemokine Receptor