化合物CCR2-RA-[R] T14900

Product Introduction
Bioactivity


英文名: CCR2-RA-[R]

描述: CCR2-RA-[R] 是一种 C-C 趋化因子受体 2 型 (CCR2) 变构拮抗剂，IC50值为103 nM。

体外活性: 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[2]. 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”[3].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : < 0.1 mg/mL (insoluble)
DMSO : 125 mg/mL (355.32 mM)


关键字: CCR | CCR2-RA-[R] | Inhibitor | inhibit | CCR-2-RA-[R] | CC chemokine receptor | CCR2RA[R] | CCR2 RA [R]

相关产品: AZD-5672 | Leronlimab | GSK2239633A | YM022 | Bindarit | CCR8 antagonist 1 | INCB3344 | CCR4 antagonist 3-1 | TAK-779 | PF-04634817

相关库: Cytokine Inhibitor Library | Immuno-Oncology Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Chemokine Inhibitor Library | NO PAINS Compound Library | Covalent Inhibitor Library | Bioactive Compound Library

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