Powder: -20°C for 3 years | In solvent: -80°C for 1 year
INCB 3284, a potent and selective human CCR2 antagonist with an oral bioavailability, is utilized in the study of acute liver failure. It effectively inhibits the binding of monocyte chemoattractant protein-1 (MCP-1) to hCCR2, demonstrating an IC50 of 3.7 nM.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 312 | 现货 | ||
5 mg | ¥ 595 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 913 | 现货 |
产品描述 | INCB 3284, a potent and selective human CCR2 antagonist with an oral bioavailability, is utilized in the study of acute liver failure. It effectively inhibits the binding of monocyte chemoattractant protein-1 (MCP-1) to hCCR2, demonstrating an IC50 of 3.7 nM. |
靶点活性 | MCP-1-hCCR2:3.7 nM |
体外活性 | INCB 3284 also causes an IC50 of 4.7 nM in antagonism of chemotaxis activity, an IC50 of 84 μM in inhibition of the hERG potassium current. However, INCB 3284 has no effec on CCR1, CCR3, CCR5, CXCR3, and CXCR5, or additional GPCRs at a concentration of 1 μM. Moreover,INCB 3284 is a pentent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC50 of 3.7 nM. INCB 3284 potently inhibits CCR2-mediated signaling events such as intracellular calcium mobilization and ERK phosphorylation with IC50 values of 6 and 2.6 nM, respectively. |
体内活性 | INCB 3284 significantly reduces the pERK1/2 to tERK1/2 ratio, as well as G-protein signaling pathway activity and proinflammatory cytokine production in cortex lysates from mice administed with azoxymethane.INCB 3284 (1 mg/kg/day, ip) reduces liver damage, and decreases microglia activation in AOM-treated mice via inhibition on CCR2. |
分子量 | 520.553 |
分子式 | C26H31F3N4O4 |
CAS No. | 887401-92-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 83.3 mg/mL (160.03 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.921 mL | 9.6052 mL | 19.2103 mL | 48.0258 mL |
5 mM | 0.3842 mL | 1.921 mL | 3.8421 mL | 9.6052 mL | |
10 mM | 0.1921 mL | 0.9605 mL | 1.921 mL | 4.8026 mL | |
20 mM | 0.0961 mL | 0.4803 mL | 0.9605 mL | 2.4013 mL | |
50 mM | 0.0384 mL | 0.1921 mL | 0.3842 mL | 0.9605 mL | |
100 mM | 0.0192 mL | 0.0961 mL | 0.1921 mL | 0.4803 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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