BX471 is a potent, selective non-peptide CCR1 antagonist (Ki=1nM for human CCR1); exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.
信号通路
Immunology/Inflammation; GPCR & G Protein
靶点
CCR1
-
-
-
-
IC50
1nM(Ki)
-
-
-
-
体外研究
BX471 inhibits MIP-α/CCL3-induced intracellular Ca2+ mobilization. BX471 is orally active; effectively reduces disease severity in a rat model of multiple sclerosis. Decreases renal fibrosis in a mouse model of obstructive nephropathy.
体内研究
N/A
临床实验
N/A
特征
N/A
相关实验数据(此数据来自于公开文献,信裕生物并不保证其有效性):
酶活性检测实验
方法
N/A
细胞实验
细胞系
N/A
浓度
N/A
处理时间
N/A
方法
N/A
动物实验
动物模型
N/A
配制
N/A
剂量
N/A
给药方式
N/A
参考文献: 1. Liang M, et al. J Biol Chem. 2000 Jun 23, 275(25), 19000-8.
2. Anders HJ, et al. J Clin Invest. 2002 Jan, 109(2), 251-9.
3. Furuichi K, et al. J Immunol. 2008 Dec 15, 181(12), 8670-6.
包装清单: