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CAS No.: 288262-96-4

BX471 HCl Catalog No. CSN18182

Synonyms: ZK-811752 hydrochloride;ZK-811752 HCl

BX471 HCl is a potent, selective non-peptide CCR1 antagonist (Ki = 1 nM for human CCR1) and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.

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实验方案

技术信息

生物活性

描述The CC chemokine receptor 1 (CCR1) is a therapeutic target for the treatment of autoimmune diseases. BX471 HCl is a non-peptide CCR1 antagonist that displaces the CCR1 ligands, including MIP-1α, RANTES, and MCP-3, with high affinity (Ki = 1.0, 2.8, and 5.5 nM, respectively). It also dose-dependently inhibited Ca²⁺ mobilization induced by MIP-1α (30 nM), RANTES (300 nM), and MCP-3 (100 nM) with IC50 values of 5, 2, and 6 nM, respectively. The increase in the intracellular Ca²⁺ concentration by 30 nM MIP-1α was completed inhibited by BX471 HCl at a dosage of 300 nM. BX471 HCl at 1 μM inhibited MIP-1α-induced upregulation of CD11b in human blood^[3]. The treatment with 20 mg/kg BX471 HCl for 10 days resulted in 55% reduction of interstitial CD45 positive leukocytes in a mouse model of unilateral ureter obstruction (UUO). BX471 HCl-treated mice also showed significantly decreased CCR5-positive CD8 T cells in UUO kidneys as compared with the vehicle controls (44.2% vs. 64.3%). Additionally, BX471 HCl reduced the amount of FSP1-positive cells by 65% in UUO kidneys compared with the vehicle-treated group^[4].
作用机制BX 471 is a potent inhibitor of chemokine binding to CCR. It blocks CCR1 activation as depicted by the inhibition of Ca²⁺ mobilization, CD11b expression, extracellular acidification and cell migration^[3].
参考文献

[1] Furuichi K, Gao JL, et al. Chemokine receptor CCR1 regulates inflammatory cell infiltration after renal ischemia-reperfusion injury. J Immunol. 2008 Dec 15;181(12):8670-6.
[2] Horuk R, Clayberger C, et al. A non-peptide functional antagonist of the CCR1 chemokine receptor is effective in rat heart transplant rejection. J Biol Chem. 2001 Feb 9;276(6):4199-204.
[3] Liang M, Mallari C, Rosser M, et al. Identification and characterization of a potent, selective, and orally active antagonist of the CC chemokine receptor-1. J Biol Chem. 2000;275(25):19000‐19008. doi:10.1074/jbc.M001222200
[4] Anders HJ, Vielhauer V, Frink M, et al. A chemokine receptor CCR-1 antagonist reduces renal fibrosis after unilateral ureter ligation. J Clin Invest. 2002;109(2):251‐259. doi:10.1172/JCI14040

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1216 mL
- 10.6078 mL
- 21.2155 mL
- 5 mM
- 0.4243 mL
- 2.1216 mL
- 4.2431 mL
- 10 mM
- 0.2122 mL
- 1.0608 mL
- 2.1216 mL

技术信息

CAS号

288262-96-4

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H25Cl2FN4O3

运输

蓝冰

分子量

471.35

别名

ZK-811752 hydrochloride;ZK-811752 HCl

溶解度

DMSO	145.0 mg/mL (307.6 mM) warming

动物实验配方

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