| Bioactivity | CCR2 antagonist 1 is a high-affinity and long-residence-time CCR2 antagonist, with a Ki of 2.4 nM. | ||||||||||||
| Invitro | The combination of SAR and SKR in the hit-to-lead process results in the discovery of a new higheaffinity and longeresidenceetime CCR2 antagonist (CCR2 antagonist 1 (compound 15a), Ki=2.4 nM; RT=714 min)[1]. | ||||||||||||
| Name | CCR2 antagonist 1 | ||||||||||||
| CAS | 1683534-96-4 | ||||||||||||
| Formula | C28H32BrF3N2O | ||||||||||||
| Molar Mass | 549.47 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Vilums M, et al. When structure-affinity relationships meet structure-kinetics relationships: 3-((Inden-1-yl)amino)-1-isopropyl-cyclopentane-1-carboxamides as CCR2 antagonists. Eur J Med Chem. 2015 Mar 26;93:121-34. |