CXCR4 antagonist 5

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CXCR4 antagonist 5 

CXCR4 antagonist 5 (compound 23) 是一种高效的 CXCR4 拮抗剂,IC50 为 8.8 nM。CXCR4 antagonist 5 可抑制 CXCL12 诱导的胞质钙离子增加 (IC50 = 0.02 nM),也能抑制 CXCR4/CXLC12 介导的趋化作用。CXCR4 antagonist 5 具有良好的理化性质和体外安全性,轻度或中度抑制 CYP 同工酶和 hERG。

CXCR4 antagonist 5

CXCR4 antagonist 5 Chemical Structure

CAS No. : 2304749-86-6

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生物活性

CXCR4 antagonist 5 (compound 23) is a highly potent CXCR4 antagonist with an IC50 value of 8.8 nM. CXCR4 antagonist 5 can inhibit CXCL12-induced cytosolic calcium increase (IC50 = 0.02 nM) and inhibits CXCR4/CXLC12-mediated chemotaxis. CXCR4 antagonist 5 has good physicochemical properties and in vitro safety profiles, inhibiting CYP isozymes and hERG marginally or moderately[1].

IC50 & Target[1]

CXCR4

8.8 nM (IC50)

分子量

366.50

Formula

C21H30N6

CAS 号

2304749-86-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Zhu F, et al. Structural optimization of aminopyrimidine-based CXCR4 antagonists. Eur J Med Chem. 2020;187:111914.

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