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BX471 HCl {[allProObj[0].p_purity_real_show]}

货号:A151361 同义名: ZK-811752 hydrochloride;BX471 hydrochloride

BX471 HCl是一种强效、选择性的非肽类 CCR1 拮抗剂(Ki = 1 nM 对人 CCR1),并对 CCR2、CCR5 和 CXCR4 的选择性为 250 倍。

BX471 HCl 化学结构 CAS号:288262-96-4
BX471 HCl 化学结构
CAS号:288262-96-4
BX471 HCl 3D分子结构
CAS号:288262-96-4
BX471 HCl 化学结构 CAS号:288262-96-4
BX471 HCl 3D分子结构 CAS号:288262-96-4
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BX471 HCl 纯度/质量文件 产品仅供科研

货号:A151361 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 CCR 其他靶点 纯度
Maraviroc ++

MIP-1α, IC50: 3.3 nM

MIP-1β, IC50: 5.2 nM

99%+
DAPTA +++

gp120 Bal-CCR5, IC50: 0.06 nM

CM235-CCR5, IC50: 0.32 nM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

BX471 HCl 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].

BX471 HCl 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

BX471 HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.12mL

0.42mL

0.21mL

10.61mL

2.12mL

1.06mL

21.22mL

4.24mL

2.12mL

BX471 HCl 技术信息

CAS号288262-96-4
分子式C21H25Cl2FN4O3
分子量 471.353
别名 ZK-811752 hydrochloride;BX471 hydrochloride
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere,2-8°C

溶解方案

DMSO: 115 mg/mL(243.98 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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