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BX471 hydrochloride

产品编号 T14845 CAS 288262-96-4

别名: ZK-811752 hydrochloride

BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist (Ki: 1 nM for human CCR1). It shows 250-fold selectivity for CCR1 over CCR2, CCR5, and CXCR4.

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BX471 hydrochloride, CAS 288262-96-4

规格	价格/CNY		货期	数量
2 mg	￥ 497		5日内发货
1 mL * 10 mM (in DMSO)	￥ 1,550		5日内发货

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BX471 hydrochloride 的其他形式现货产品:

BX471

其他形式的 BX471 hydrochloride:

BX471
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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist (Ki: 1 nM for human CCR1). It shows 250-fold selectivity for CCR1 over CCR2, CCR5, and CXCR4.
靶点活性	MIP-1α-CCR1:1 nM （ki）, MCP-3-CCR1:5.5 nM （ki）, RANTES-CCR1:2.8 nM （ki）
体外活性	BX471 is a potent functional antagonist based on its ability to inhibit a number of CCR1-mediated effects including Ca2+ mobilization, increase in extracellular acidification rate, CD11b expression, and leukocyte migration and it is also able to displace 125I-MIP-1α/CCL3 binding to mouse CCR1 in a concentration-dependent manner (Ki: 215 nM). BX471 demonstrates a greater than 10,000-fold selectivity for CCR1 compared with 28 G-protein-coupled receptors [1]. BX471 also inhibits the RANTES-mediated adhesion of T lymphocytes to activated endothelium [4]. BX471 (0.1-10 μM) shows dose-dependent inhibition of RANTES-mediated and shear-resistant adhesion on IL-1β-activated microvascular endothelium in shear flow in isolated blood monocytes. Increasing concentrations of BX471 inhibits the Ca2+ transients induced by MIP-1α/CCL3 in both human and mouse CCR1 (IC50s: 5.8 nM and 198 nM) [2].
体内活性	BX471 has a borderline significant effect on the number of CCR5-positive CD8 cells in the peripheral blood. BX471 reduces the amount of FSP1-positive cells by 65% in UUO kidneys as compared with vehicle control [2]. BX471 (4 mg/kg, p.o. or i.v.) is orally active with a bioavailability of 60% in dogs. Furthermore, BX471 effectively reduces disease in a rat experimental allergic encephalomyelitis model of multiple sclerosis [1]. BX471 (20 mg/kg, s.c.) reaches peak plasma levels of 9 μM by around 30 minutes, and this rapidly declines to approximately 0.4 μM after 2 hours. From 4 to 8 hours the drug plasma levels drop to 0.1 μM or lower. Mice treated with 20 mg/kg of BX471 for 10 days shows a reduction of interstitial CD45 positive leukocytes of approximately 55%. Pretreatment with BX471 reduces macrophage and neutrophil accumulation in the kidney after ischemia-reperfusion injury [3].

别名	ZK-811752 hydrochloride
分子量	471.35
分子式	C21H25Cl2FN4O3
CAS No.	288262-96-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 150 mg/mL (318.23 mM), Sonication is recommended.

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1216 mL	10.6078 mL	21.2157 mL	53.0391 mL
	5 mM	0.4243 mL	2.1216 mL	4.2431 mL	10.6078 mL
	10 mM	0.2122 mL	1.0608 mL	2.1216 mL	5.3039 mL
	20 mM	0.1061 mL	0.5304 mL	1.0608 mL	2.652 mL
	50 mM	0.0424 mL	0.2122 mL	0.4243 mL	1.0608 mL
	100 mM	0.0212 mL	0.1061 mL	0.2122 mL	0.5304 mL

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参考文献

1. Liang M, 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. Anders HJ, et al. A chemokine receptor CCR-1 antagonist reduces renal fibrosis after unilateral ureter ligation. J Clin Invest. 2002 Jan;109(2):251-9. 3. Furuichi K, et al. Chemokine receptor CCR1 regulates inflammatory cell infiltration after renal ischemia-reperfusion injury. J Immunol. 2008 Dec 15;181(12):8670-6. 4. Horuk R, 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.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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