生物活性
LY333531盐酸盐具有竞争性和可逆性抑制PKCβI和PKCβII (IC50值分别为4.7和5.9 nM)。
化学数据
分子量 | 505.01 |
分子式 | C28H28N4O3.HCl |
CAS号 | 169939-93-9 |
纯度 | >98% |
溶解性(25°C) | DMSO |
储存和运输条件 | 固体粉末: -20°C 冷藏长期储存 常温运输及临时存放 |
实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)
细胞实验 |
---|
细胞系 | HUVECs |
方法 | Western blot Aortas and HUVECs were lysed in lysis buffer or membrane and cytosol protein extraction kit and total proteins in the supernatant were extracted to perform Western blot analysis. Equal amounts of proteins were separated through electrophoresis on SDS-PAGE gels and transferred to nitrocellulose membranes (Millipore, MA, USA). After blocked with 5% skim milk, the membranes were incubated with the appropriate primary antibodies respectively against PKC-β (Abcam, CA, USA), and β-actin (Zhong Shan Golden Bridge Biotechnology, Beijing, China) with recommended dilution at 4 °C overnight. The membranes were washed and further incubated with corresponding secondary antibodies [Anti-Rabbit IgG; Anti-mouse IgG (Zhong Shan Golden Bridge Biotechnology, Beijing, China)] with horseradish peroxidase (HRP) conjugation at 37 °C for 60 min. The films were developed using an ECL Plus chemiluminescence reagent kit (Millipore, MA, USA) and visualized using ChemiDocXRS (Bio-Rad Laboratory, CA, USA). Densitometries were analyzed using Quantity One software. |
浓度 | 5μM |
处理时间 | 24h |
动物实验 |
---|
动物模型 | Male Sprague-Dawley rats diabetes models |
配制 | dissolved in citrate buffer (0.1 mol/L, pH 4.5) |
剂量 | 1 mg/kg/day |
给药处理 | oral gavage for 4 weeks |
不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
动物 A的Km系数 |
例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 1.9802 mL | 9.9008 mL | 19.8016 mL |
5 mM | 0.396 mL | 1.9802 mL | 3.9603 mL |
10 mM | 0.198 mL | 0.9901 mL | 1.9802 mL |