BX471

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Chemical Structure| 217645-70-0 同义名 : ZK-811752; BAY 865047; SH T 04268H
CAS号 : 217645-70-0
货号 : A434794
分子式 : C21H24ClFN4O3
纯度 : 99%+
分子量 : 434.89
MDL号 : MFCD09859709
存储条件:

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 BX471 is a potent and selective non-peptide CCR1 (CC Chemokine Receptor-1). It competitively displaced the CCR1 ligands MIP-1α, RANTES and MCP-3 with Ki values ranging in 1-5.5nM. BX471 could inhibit a number of CCR1-mediated effects including MIP-1α-induced Ca2+ mobilization, increase in extracellular acidification rate, MIP-1α-inducedCD11b expression, and leukocyte and monocyte migration induced by MIP-1α and RANTES. It effectively reduced disease in a rat experimental allergic encephalomyelitis model of multiple sclerosis at doses of 20mg/kg and 50mg/kg[2].
作用机制 BX471 can display CCR1 ligands in a competitive manner.[2]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.30mL

0.46mL

0.23mL

11.50mL

2.30mL

1.15mL

22.99mL

4.60mL

2.30mL

参考文献

[1]Liang M, Mallari C, et al. Identification and characterization of a potent, selective, and orally active antagonist of the CC chemokine receptor-1. J Biol Chem. 2000 Jun 23;275(25):19000-8.

[2]Liang M, Mallari C, Rosser M, Ng HP, May K, Monahan S, Bauman JG, Islam I, Ghannam A, Buckman B, Shaw K, Wei GP, Xu W, Zhao Z, Ho E, Shen J, Oanh H, Subramanyam B, Vergona R, Taub D, Dunning L, Harvey S, Snider RM, Hesselgesser J, Morrissey MM, Perez HD. Identification and characterization of a potent, selective, and orally active antagonist of the CC chemokine receptor-1. J Biol Chem. 2000 Jun 23;275(25):19000-8. doi: 10.1074/jbc.M001222200. PMID: 10748002.