Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PF-3644022 是可口服的,具有 ATP 竞争性的MAPKAPK2 (MK2)选择性抑制剂,IC50为 5.2 nM,Ki 为 3 nM。它有效抑制 TNFα 的产生并具有抗炎作用,还抑制 MK3 和 p38 调节/激活激酶,IC50分别为 53 和 5.0 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,080 | 现货 | ||
5 mg | ¥ 2,720 | 现货 | ||
10 mg | ¥ 4,280 | 现货 | ||
25 mg | ¥ 6,830 | 现货 | ||
50 mg | ¥ 9,270 | 现货 | ||
100 mg | ¥ 12,500 | 现货 | ||
500 mg | ¥ 24,800 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,990 | 现货 |
产品描述 | PF-3644022 is an effective, selective, and ATP-competitive MAPKAPK2 (MK2) inhibitor (IC50: 5.2 nM and a Ki of 3 nM). PF-3644022 potently inhibits TNFα production and has an anti-inflammatory effect. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) (IC50s: 53 nM and 5.0 nM, respectively). |
靶点活性 | MK3:53 nM, PRAK:5.0 nM, MK2:(ki)3 nM, MK2:5.2 nM |
体外活性 | PF-3644022 potently inhibits TNFα production with similar activity (IC50 of 160 nM), in the human U937 monocytic cell line or peripheral blood mononuclear cells. PF-3644022 blocks TNFα and IL-6 production in LPS-stimulated human whole blood (IC50: 1.6 and 10.3 μM, respectively). The inhibitory activity of PF-3644022 against other MAPKAP kinase family members is evaluated. Other than MNK2 with an IC50 of 148 nM, other family members are largely not inhibited, showing at least several hundred-fold selectivity versus MK2[1]. |
体内活性 | PF-3644022 (3-100 mg/kg; oral gavage; twice a day; for 12 days; Lewis rats) treatment displays dose-dependent inhibition of chronic paw swelling. It is measured on day 21 after 12 days of oral dosing (ED50: 20 mg/kg)[1]. |
分子量 | 374.46 |
分子式 | C21H18N4OS |
CAS No. | 1276121-88-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 41.67 mg/mL (111.28 mM), ultrasonic and warming and heat to 80°C
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6705 mL | 13.3526 mL | 26.7051 mL | 66.7628 mL |
5 mM | 0.5341 mL | 2.6705 mL | 5.341 mL | 13.3526 mL | |
10 mM | 0.2671 mL | 1.3353 mL | 2.6705 mL | 6.6763 mL | |
20 mM | 0.1335 mL | 0.6676 mL | 1.3353 mL | 3.3381 mL | |
50 mM | 0.0534 mL | 0.2671 mL | 0.5341 mL | 1.3353 mL | |
100 mM | 0.0267 mL | 0.1335 mL | 0.2671 mL | 0.6676 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。
PF-3644022 1276121-88-0 MAPK Proteases/Proteasome Serine Protease p38 MAPK MAPKAP kinase 2 monocytic lipopolysaccharide IL-6 TNFα safety Anti-inflammatory orally PRAK efficacious PF3644022 inhibit Mitogen-activated protein kinase activated protein kinase 2 Inhibitor MK3 PF 3644022 MAP kinase activated protein kinase 2 MAPKAPK2 (MK2) MAPK activated protein kinase 2 inhibitor