AZD2423是一种有效的、选择性的、口服生物利用的、非竞争性的CCR2趋化因子受体负向变构调节剂。AZD2423对CCR2Ca2+通量的IC50为1.2nM。
AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator. AZD2423 has an IC50 of 1.2 nM for CCR2 Ca2+ flux [1][2][3].
AZD2423 inhibits MCP-1 induced calcium mobilization and chemotaxis of THP-1 cell line with an IC50 of 4 nM[1].
[1]. AZD2423. [2]. John G. Cumming. CCR2 antagonists for the treatment of neuropathic pain: The discovery and development of AZD2423. [3]. Kalliom?ki J, et al. A randomized, double-blind, placebo-controlled trial of a chemokine receptor 2 (CCR2) antagonist in posttraumatic neuralgia. Pain. 2013 May;154(5):761-7.
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