Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Crisaborole (AN-2728) 是一种有效的 PDE4和 cytokine 释放抑制剂,能够抑制 PDE4(IC50=0.49 μM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 229 | 现货 | ||
10 mg | ¥ 373 | 现货 | ||
50 mg | ¥ 591 | 现货 | ||
100 mg | ¥ 792 | 现货 | ||
200 mg | ¥ 996 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 415 | 现货 |
产品描述 | Crisaborole (AN-2728) is a Phosphodiesterase 4 Inhibitor. |
靶点活性 | PDE4:0.49 μM |
体外活性 | AN-2728 inhibits PDE isozymes PDE1A3, PDE3Cat , PDE4Cat and PDE7A1 with IC50 values of 6.1, 6.4, 0.11 and 0.73 μM. AN-2728 inhibits PDE4, TNF-α, IL-2, IFN-γ, IL-5 and IL-10 with IC50 values of 0.49, 0.54, 0.61, 0.83, 2.4 and 5.3 μM. AN-2728 shows the most potent activity against PDE4 catalytic domain, but it also shows inhibition against PDE1A3, PDE3Cat, and PDE7A1. Crystallography reveals that interaction of benzoxaboroles with the hydrophobic pocket in the PDE4 catalytic domain increase their affinity for PDE4. These benzoxaboroles strongly suppresses the secretion of cytokines associated with Ps and AD. |
体内活性 | AN-2728 is reported to be well tolerated and to demonstrate significant effects on markers of efficacy, with results that were comparable to positive controls in clinical trials. AN-2728 shows significant inhibition against the ear edema caused by phorbol ester after dosing at 1 mg/ear×2 (78% and 68%, respectively). The efficacy is comparable to that of dexamethasone, suggesting that AN-2728 has good anti-inflammatory activity as well as skin penetration. |
别名 | 克立硼罗, AN-2728, PF-06930164 |
分子量 | 251.05 |
分子式 | C14H10BNO3 |
CAS No. | 906673-24-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 32 mg/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。
Crisaborole 906673-24-3 Metabolism PDE Inhibitor inhibit 克立硼罗 AN 2728 PF06930164 AN2728 AN-2728 PF 06930164 Phosphodiesterase (PDE) PF-06930164 inhibitor