Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BIX 02565 是核糖体 S6 激酶 2 (RSK2) 抑制剂,IC50为 1.1 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 666 | 待询 | ||
2 mg | ¥ 973 | 待询 | ||
5 mg | ¥ 1,800 | 待询 | ||
10 mg | ¥ 2,810 | 待询 | ||
25 mg | ¥ 4,680 | 待询 | ||
50 mg | ¥ 6,670 | 待询 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,800 | 现货 |
产品描述 | BIX 02565 is a potent inhibitor of ribosomal S6 kinase 2 (RSK2, IC50: 1.1 nM). |
靶点活性 | PRKD1:35 nM (cell free), RSK2:1.1 nM (cell free), LRRK2:16 nM (cell free) |
体外活性 | BIX 02565 inhibited RSK2 with IC50 value of 1.1 nM. It also inhibited LRRK2 and PRKD1 with IC50 values of 16 and 35 nM [1]. BIX 02565 elicited >50% inhibition at adrenergic α1A-, α1B-, α1D-, α2A-, β2-, and imidazoline I2 receptors (IC50s: 0.052-1.820 μM) [2]. |
体内活性 | Infusion of BIX 02565 (1, 3, and 10 mg/kg) in the rat CV screen resulted in a precipitous decrease in both mean arterial pressure (MAP; to -65 ± 6 mm Hg below baseline) and heart rate (-93 ± 13 beats/min). In telemetry-instrumented rats, BIX 02565 (30, 100, and 300 mg/kg p.o. QD for 4 days) elicited concentration-dependent decreases in MAP after each dose (to -39 ± 4 mm Hg on day 4 at T(max)); analysis by Demming regression demonstrated strong correlation independent of route of administration and influence of anesthesia [2]. |
细胞实验 | A monolayer of exponentially growing HLR-CREB cells was prepared and transfected using Effectene with RSK2. Cells were plated into 96-well culture plates, and compounds were added 20 to 24 h after transfection. Luciferase expression (48 h) and activity (5 min) were determined using Steady-Glo per manufacturer's instructions, and results were represented as the percentage luciferase activity relative to the control measured in the absence of inhibitors (percentage of control); the IC50 was fitted to a standard four-parameter logistic equation. Each data point represents an average of triplicate observations [2]. |
动物实验 | Mean arterial pressure was assessed in conscious, freely moving male Sprague-Dawley rats (n = 6/group) instrumented with telemetry transmitters similar to that described previously. BIX 02565 (30, 100, and 300 mg/kg p.o. QD) was administered as a solution (10 ml/kg) in a 20% hydroxy-propyl-β-cyclodextran vehicle as described previously. Mean arterial pressure was reported from 2 h before (baseline) and 90 h after the first dose; compound was administered at 0, 24, 48, and 72 h. A blood sample was collected from satellite rats (n = 3/group) at 1-h after dose (Tmax) on days 1 and 4 for analysis of plasma drug concentrations by mass spectrometry [2]. |
分子量 | 458.56 |
分子式 | C26H30N6O2 |
CAS No. | 1311367-27-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 20 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。
BIX 02565 1311367-27-7 Autophagy MAPK PI3K/Akt/mTOR signaling LRRK2 S6 Kinase Inhibitor Ribosomal S6 Kinase (RSK) S6K inhibit BIX-02565 BIX02565 inhibitor