Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK6853 是一种强选择性RPF1乙酰赖氨酸抑制剂,pKd 为9.5,其选择性是其它的乙酰赖氨酸的 1600 倍。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 289 | 现货 | ||
2 mg | ¥ 413 | 现货 | ||
5 mg | ¥ 579 | 现货 | ||
10 mg | ¥ 953 | 现货 | ||
25 mg | ¥ 1,790 | 现货 | ||
50 mg | ¥ 2,880 | 现货 | ||
100 mg | ¥ 4,630 | 现货 | ||
500 mg | ¥ 9,630 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 588 | 现货 |
产品描述 | GSK6853 is a potent, soluble, cell-active, and highly selective inhibitor of the BRPF1 bromodomain. |
靶点活性 | BRPF1:8.1(pIC50) |
体外活性 | Screening GSK6853 against a panel of 48 unrelated assays reveals only off-target activities that are relatively weak compared to the BRPF1 potency. However, to minimize the chance of off-target effects , the recommended concentration is no higher than 1 μM in cell-based assays[1]. |
体内活性 | In male CD1 mouse, following IV administration (1 mg/kg), GSK6853 demonstrates a high blood clearance of 107 mL/min/kg, a moderate volume of distribution (5.5 L/kg) and a moderate terminal half-life of 1.7 h. Oral administration (PO, 3 mg/kg) achieves a moderate systemic exposure, with a Cmax of 42 ng/mL and Tmax of 1.5 h, resulting in a bioavailability of 22%. The intraperitoneal route of administration (IP, 3 mg/kg) reaches a Cmax of 469 ng/mL and Tmax of 0.25 h, resulting in a bioavailability of 85%. The results indicate that the IP route of administration would be suitable for dosing this molecule in potential PKPD models[1]. |
分子量 | 409.48 |
分子式 | C22H27N5O3 |
CAS No. | 1910124-24-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55 mg/mL (134.41 mM)
Ethanol: 81 mg/mL (197.81 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.4421 mL | 12.2106 mL | 24.4212 mL | 61.053 mL |
5 mM | 0.4884 mL | 2.4421 mL | 4.8842 mL | 12.2106 mL | |
10 mM | 0.2442 mL | 1.2211 mL | 2.4421 mL | 6.1053 mL | |
20 mM | 0.1221 mL | 0.6105 mL | 1.2211 mL | 3.0527 mL | |
50 mM | 0.0488 mL | 0.2442 mL | 0.4884 mL | 1.2211 mL | |
100 mM | 0.0244 mL | 0.1221 mL | 0.2442 mL | 0.6105 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。
GSK6853 1910124-24-1 Chromatin/Epigenetic Epigenetic Reader Domain Inhibitor inhibit GSK 6853 GSK-6853 inhibitor