Q-VD-OPh
Catalog No.
A1901
Pan-caspase抑制剂。
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QVD-OPh是一种pan-caspase抑制剂，提供了一种低成本，无毒和高特异性的细胞凋亡抑制方式，并为抑制剂的设计提供了新视角。
Q-VD-OPh可以抑制重组的caspases 1、3、8和9，IC50值范围介于25-400 nM之间。Q-VD-OPh可以显著抑制放线菌素D诱导的细胞凋亡。与广泛使用的抑制剂ZVAD-fmk和Boc-D-fmk相比，Q-VD-OPh可以更加有效地抑制凋亡。Q-VD-OPh可以在不到4个小时的时间内完全抑制凋亡诱导子诱导的大量细胞的死亡。Q-VD-OPh也可以有效的阻止三大凋亡途径介导的细胞凋亡，分别是caspase 9/3、caspase 8/10和caspase 12。Q-VD-OPh具有更高的效力，但即使在高浓度下，它对细胞也是无毒的。Q-VD-OPh可以在不同的细胞类型和物种（人，小鼠和大鼠）中起作用，阻止终端caspase激活、底物切除以及与细胞凋亡相关的DNA片段的形成。
Q-VD-OPH作为一个独特的试剂，可以将难以复活的传代细胞从液氮中恢复过来。将Q-VD-OPH加入到要解冻的细胞中，细胞可以获得足够的时间从解冻的压力中恢复并开始增值，即使在标准的DMSO浓度（10％）下。Q-VD-OPh在溶液中可以稳定存在几个月，在培养基中有至少2.5天的效力。
参考文献：
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| Storage | Store at -20°C |
| M.Wt | 513.49 |
| Cas No. | 1135695-98-5 |
| Formula | C26H25F2N3O6 |
| Solubility | ≥25.67 mg/mL in DMSO; insoluble in H2O; ≥28.75 mg/mL in EtOH |
| Chemical Name | (S)-5-(2,6-difluorophenoxy)-3-((S)-3-methyl-2-(quinoline-2-carboxamido)butanamido)-4-oxopentanoic acid |
| SDF | Download SDF |
| Canonical SMILES | O=C(N[C@@H](C(C)C)C(N[C@@H](CC(O)=O)C(COC1=C(F)C=CC=C1F)=O)=O)C2=NC3=CC=CC=C3C=C2 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验[1]： | |
|
细胞系 |
JURL-MK1和HL60细胞 |
|
溶解方法 |
溶解于DMSO。为了获得更高的浓度，可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
|
反应时间 |
N/A |
|
应用 |
Q-VD-OPH在0.05 mM时可大幅度抑制caspase-3和caspase-7的活性，在低浓度时也可以抑制caspase-8。Q-VD-OPH在10 mM时抑制PARP-1的裂解，在2 mM时抑制DNA片段化，干扰细胞膜的功能。而药物诱导的细胞与纤连蛋白粘着性的丧失则需要10 mM Q-VD-OPh。 |
| 动物实验[2]： | |
|
动物模型 |
3个月大的TgCRND8小鼠 |
|
剂量 |
10 mg/kg，3次/周，3个月；腹腔注射 |
|
应用 |
在阿尔兹海默病的慢性治疗中，Q-VD-OPh抑制caspase-7的激活，限制tau和caspase裂解的病理变化。 |
|
注意事项 |
请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的，属于正常现象。 |
|
References: 1. Ku?elová K1, Grebeňová D, Brodská B.Dose-dependent effects of the caspase inhibitor Q-VD-OPh on different apoptosis-related processes. J Cell Biochem. 2011 Nov;112(11):3334-42. 2. Rohn TT, Kokoulina P, Eaton CR et al. Caspase activation in transgenic mice with Alzheimer-like pathology: results from a pilot study utilizing the caspase inhibitor, Q-VD-OPh. Int J Clin Exp Med. 2009 Nov 5;2(4):300-8. |
|
| Q-VD-OPH是一种脑和细胞通透性的、高效的和不可逆的pan-caspase抑制剂。作用于caspase-3、caspase-1、caspase-8和caspase-9，IC50值分别为25 nM、50 nM、100 nM和430 nM。 | ||||||
| 靶点 | caspase-1 | caspase-3 | caspase-8 | caspase-9 | ||
| IC50 | 50nM | 25nm | 100nM | 430nM | ||
质量控制和MSDS
- 批次:
化学结构
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