生物活?/h4>
MG-132是一种蛋白酶体抑制剂,IC50?00 nM,也抑制钙蛋白酶,IC50?.2 μM。MG132通过诱导细胞周期停滞以及引发细胞凋亡来抑制HeLa细胞的生长。MG-132 (10 μM) 通过抑制蛋白酶体介导的IκBα降解,有效抑制A549细胞中TNF-α诱导的NF-κB活化。MG132可以抑制NLRP1的活化、/p>
体内研究中,MG-132(ip?.1 mg/kg/day)通过调节ERK1/2和JNK1信号通路,减轻压力超负荷引起的心脏肥大。MG-132治疗通过下调肌肉特异性泛素连接酶atrogin-1/MAFbx 和MuRF-1 mRNA,显著减少小鼠体内固定化诱导的骨骼肌萎缩、/p>
化学数据
| 分子野/td> |
475.62 |
| 分子弎/td> |
C26H41N3O5 |
| CAS叶/td> |
133407-82-6 |
| 纯度 |
98.80% |
| 溶解性(25C(/td> |
DMSO 80 mg/mL Ethanol 20 mg/mL |
| 储存和运输条仵/td> |
固体粉末 -20C 冷藏长期储存 常温运输及临时存攽/td> |
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 |
| 细胞糺/td> |
Lung cancer cell lines A549 and H1299 |
| 方法 |
Cell viability assay. Cell viability was determined using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Cells were seeded in 96-well plates at a density of 2.5x103/well 1 day prior to treatment. Then, cells were treated with MG132 or/and irradiation. After treatment, 20 μl of 5 mg/ml MTT solution was added into each well and incubated for 4 h. After the supernatant was removed, 100 μl of DMSO was added, and then placed in a microplate reader to measure OD value. Cell viability rate (vR) was calculated according to the following formula: vR = (OD in observed group/OD in 0 Gy group) x 100%. All assays were repeated 3 times in quintuplicate. |
| 浓度 |
200 nM |
| 处理时间 |
6h |
| 动物实验 |
| 动物模型 |
Male mdx (C57BL/10ScSn DMD mdx) mice |
| 配制 |
Dissolved in DMSO, and diluted in PBS |
| 剂量 |
~10 μg/kg/day |
| 给药处理 |
Injection |
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(/h4>
|
小鼠 |
大鼠 |
兓/td> |
豚鼠 |
仓鼠 |
狖/td> |
| 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?),再除以大鼠的Km系数?),得到化合物用于大鼠的等效剂量?0 mg/kg、/p>
储备液配刵/h4>
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、/p>
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
2.1025 mL |
10.5126 mL |
21.0252 mL |
| 5 mM |
0.4205 mL |
2.1025 mL |
4.205 mL |
| 10 mM |
0.2103 mL |
1.0513 mL |
2.1025 mL |