| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
GSK356278 是一种有效的特异性磷酸二酯酶 4 (PDE4) 抑制剂,对人 PDE4A、PDE4B 和 PDE4D 的 pIC50 分别为 8.6、8.8 和 8.7。 GSK356278 具有抗炎、抗焦虑和增强认知的作用。
产品描述 | GSK356278 is an effective and selective inhibitor of phosphodiesterase 4 (PDE4), with pIC50s of 8.6, 8.8, and 8.7 for human PDE4A, PDE4B, and PDE4D, respectively. GSK356278 has anti-inflammatory, anxiolytic, and cognition-enhancing effects. |
靶点活性 | PDE4D:8.7 (pIC50), PDE4A:8.6 (pIC50), PDE4B:8.8 (pIC50) |
体外活性 | GSK356278 bounds to the HARBS in rats, mice, marmosets, and ferrets with pKis of 7.9, 7.8, 8.4, and 8.5, respectively. GSK356278 inhibits LPS-induced release of TNF-α in human whole blood, with a pIC50 of 7.6. GSK356278 competes with [3H]rolipram for the high affinity rolipram binding site (HARBS) with a pKi of 8.6 in a competitive filtration-binding assay to the recombinant human PDE4B2B enzyme expressed in yeast membranes[1]. |
体内活性 | GSK356278 (4 doses at 0.03, 0.1, 0.3, and 1.0 mg/kg for 6 weeks; p.o.) enhances performance in a nonhuman primate object retrieval test[1]. GSK356278 exhibits oral bioavailability (rat 91%, monkey 23%) and Cmax (rat 205, monkey 41 nM) following oral administration (rat 1, monkey 0.2 mg/kg). GSK356278 (0.1-0.1 mg/kg; p.o.) demonstrates efficacy in a nonhuman primate model of anxiety at exposures that do not induce emesis. GSK356278 (0.003-30 mg/kg; p.o.) shows anti-inflammatory activity in rodents at exposures that does not induce pica feeding[1]. |
别名 | GSK-356278, GSK 356278 |
分子量 | 439.53 |
分子式 | C21H25N7O2S |
CAS No. | 720704-34-7 |
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
DMSO: 2 mg/mL (4.55 mM), Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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。
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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。
GSK356278 720704-34-7 Metabolism PDE GSK-356278 anti-inflammatory Phosphodiesterase (PDE) anxiolytic cognition Inhibitor phosphodiesterase PDE4 inhibit GSK 356278 inhibitor