Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GNE-049 is a highly potent and selective inhibitor of CBP (IC50: 1.1 nM in TR-FRET assay). GNE-049 also inhibits BRET and BRD4(1) (IC50s: 12 nM and 4200 nM, respectively).
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 3,630 | 5日内发货 | ||
5 mg | ¥ 4,570 | 5日内发货 | ||
25 mg | ¥ 13,900 | 8-10周 | ||
50 mg | ¥ 18,300 | 8-10周 | ||
100 mg | ¥ 23,500 | 8-10周 | ||
1 mL * 10 mM (in DMSO) | ¥ 5,130 | 5日内发货 |
产品描述 | GNE-049 is a highly potent and selective inhibitor of CBP (IC50: 1.1 nM in TR-FRET assay). GNE-049 also inhibits BRET and BRD4(1) (IC50s: 12 nM and 4200 nM, respectively). |
靶点活性 | BRD41:4200 nM, CBP:1.1 nM, BRET:12 nM |
体外活性 | GNE-049 inhibits the expression of MYC (EC50: 14 nM). GNE-049 has excellent potency in the BRET cellular assay and, in an orthogonal measure of the target engagement. GNE-049 is selected for further profiling as it has the best balance of liver microsomes (LM) stability, selectivity, and cellular potency. |
体内活性 | GNE-049 shows acceptable PK in mouse, rat, dog, and monkey. GNE-049 is further evaluated in a rat single dose (30-250 mg/kg QD) toxicokinetic study. GNE-049 is selective for CBP/P300 and, importantly, quite selective (3820-fold) over BRD4(1), which revealed from the Determination of potency versus a selection of bromodomains. Furthermore, at the 250 mg/kg dose level, the ratio of the unbound drug concentration in the brain to unbound drug concentration in plasma (Kp,uu) 3 h post-dose is determined to be 0.43, indicating that GNE-049 is penetrating into the CNS and potentially resulting in the observed toxicity. |
分子量 | 510.58 |
分子式 | C27H32F2N6O2 |
CAS No. | 1936421-41-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (195.86 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.9586 mL | 9.7928 mL | 19.5856 mL | 48.9639 mL |
5 mM | 0.3917 mL | 1.9586 mL | 3.9171 mL | 9.7928 mL | |
10 mM | 0.1959 mL | 0.9793 mL | 1.9586 mL | 4.8964 mL | |
20 mM | 0.0979 mL | 0.4896 mL | 0.9793 mL | 2.4482 mL | |
50 mM | 0.0392 mL | 0.1959 mL | 0.3917 mL | 0.9793 mL | |
100 mM | 0.0196 mL | 0.0979 mL | 0.1959 mL | 0.4896 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。
GNE-049 1936421-41-8 Chromatin/Epigenetic Epigenetic Reader Domain GNE 049 GNE049 Inhibitor inhibitor inhibit