CCR2-RA-[R]
产品说明书
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同义名 : | - |
| CAS号 : | 512177-83-2 | |
| 货号 : | A316281 | |
| 分子式 : | C18H19ClFNO3 | |
| 纯度 : | 99% | |
| 分子量 : | 351.8 | |
| MDL号 : | MFCD11616183 | |
| 存储条件： |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
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| 描述 | The chemokine receptor CCR2, a G protein-coupled receptor implicated in numerous chronic inflammatory diseases, has led to the development of various small molecule antagonists. CCR2-RA-[R] effectively displaces [125I]CCL2 from CCR2 with a pIC50 value of 6.1, while its pKD for CCR2 and CCR5 are 8.8±0.1 and 7.0±0.1 respectively[2]. CCR2-RA-[R] inhibits CCR2 non-competitively by preventing activation-associated conformational changes and the formation of the G protein-binding interface. The drug-binding pocket of CCR2-RA-[R] is notably enclosed and features a beneficial mix of hydrophobic and polar characteristics that enhance its "druggability"[3]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.84mL 0.57mL 0.28mL |
14.21mL 2.84mL 1.42mL |
28.43mL 5.69mL 2.84mL |
| 参考文献 |
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