生物活性
Tubastatin A HCl是一种有效的,选择性HDAC6抑制剂,IC50为15 nM,选择性作用于所有其他同工酶(1000倍以上),除了HDAC8(57倍以上)。Tubastatin A 对所有11 种HDAC亚型都有选择性, 对HDAC6的 IC50 为15 nM ,是除HDAC8以外其它所有亚型的1000多倍,是对HDAC8选择性的57倍左右。Tubastatin A 对 HDAC8 IC50为 854 nM。Tubastatin A 对同型半胱氨酸 (HCA) 诱导的神经细胞死亡具有保护作用 ,从5 μM开始这种保护作用具有剂量依赖特性, 到10 μM时基本可以完全保护细胞不受损伤 。
化学数据
分子量 | 371.86 |
分子式 | C20H21N3O2.HCl |
CAS号 | 1310693-92-5 |
纯度 | >99% |
溶解性(25°C) | DMSO: ≥ 11 mg/mL |
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 |
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细胞系 | Primary cortical neuron |
方法 | Neuroprotection Assays Primary cortical neuron cultures were obtained from the cerebral cortex of fetal Sprague-Dawley rats (embryonic day 17) as described previously. All experiments were initiated 24 h after plating. Under these conditions, the cells are not susceptible to glutamate-mediated excitotoxicity. For cytotoxicity studies, cells were rinsed with warm PBS and then placed in minimum essential medium (Invitrogen) containing 5.5 g/liter glucose, 10% fetal calf serum, 2 mM L-glutamine, and 100 μM cystine. Oxidative stress was induced by the addition of the glutamate analog homocysteate (HCA; 5 mM) to the media. HCA was diluted from 100-fold concentrated solutions that were adjusted to pH 7.5. In combination with HCA, neurons were treated with either TSA or Tubastatin A at the indicated concentrations. Viability was assessed after 24 h by MTT assay (3-(4,5-dimethylthiazol-2-yl)- 2,5-diphenyltetrazolium bromide) method. |
浓度 | 0, 1, 2.5, 5.0, 7.5 and 10 μM |
处理时间 | 24 h |
动物实验 |
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动物模型 | dextran sodium sulfate (DSS) and adoptive transfer models of colitis |
配制 | DMSO |
剂量 | 0.5 mg/kg of body weight/day |
给药处理 | i.p |
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 |
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1 mM | 2.6892 mL | 13.4459 mL | 26.8918 mL |
5 mM | 0.5378 mL | 2.6892 mL | 5.3784 mL |
10 mM | 0.2689 mL | 1.3446 mL | 2.6892 mL |