Q-VD-OPh (Synonyms: QVD-OPH; Quinoline-Val-Asp-Difluorophenoxymethylketone)
目录号: PL12281 纯度: ≥99%
CAS No. :1135695-98-5
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中文名称
Q-VD-OPh
中文别名
(3S)-5-(2,6-二氟苯氧基)-3-[[(2S)-3-甲基-1-氧代-2-[(2-喹啉甲酰基)氨基]丁基]氨基]-4-氧代-戊酸;(3S)-5-(2,6-二氟苯氧基)-3-[[(2S)-3-甲基-1-氧代-2-[(2-喹啉羰基)氨基]丁基]氨基]-4-氧代-戊酸;2,6-二氯苯氧基乙酸;2-[4-(2-氨基乙酰基)哌嗪-1-基]-N-甲基乙酰胺;N-(2-喹啉基)缬氨酰-天门冬氨酰-(2,6-二氟苯氧基)甲基 酮 水合物
英文名称
Q-VD-OPh
英文别名
(3S)-5-(2,6-Difluorophenoxy)-3-[[(2S)-3-methyl-1-oxo-2-[(2-quinolinylcarbonyl)amino]butyl]amino]-4-oxo-pentanoic Acid;(3S)-5-(2,6-Difluorophenoxy)-3-[[(2S)-3-methyl-1-oxo-2-[(2-quinolinylcarbonyl)amino]butyl]amino]-4-o;(3S)-5-(2,6-difluorophenoxy)-3-[[(2S)-3-methyl-2-(quinoline-2-carbonylamino)butanoyl]amino]-4-oxopentanoic acid;Q-VD-OPH;Q-VD-Oph (Q-Val-Asp-OPh);Quinoline-Val-Asp-Difluorophenoxymethylketone;QVD-OPH;Q-VD-OPh
Cas No.
1135695-98-5
分子式
C26H25N3O6F2
分子量
513.49
包装储存
Powder -20°C 3 years;In solvent -80°C 6 months
产品详情
Q-VD-OPh 是一种不可逆的泛胱天蛋白酶 (caspase) 抑制剂,具有高效的抗凋亡能力。抑制胱天蛋白酶 7 的 IC50 值别为 48 nM,抑制胱天蛋白酶 1,3,8,9,10,12 的 IC50 值在 25-400 nM 之间。Q-VD-OPh 可抑制 HIV 感染。Q-VD-OPh 能透过血脑屏障。
生物活性
Q-VD-OPh is an irreversible pan-caspase inhibitor with potent antiapoptotic properties; inhibits caspase 7 with an IC 50 of 48 nM and 25-400 nM for other caspases including caspase 1, 3, 8, 9, 10, and 12. Q-VD-OPh can inhibits HIV infection. Q-VD-OPh is able to cross the blood-brain barrier.
性状
Solid
IC50 & Target[1][2]
Caspase-3 25-400 nM (IC50) Caspase-7 48 nM
体外研究(In Vitro)
Q-VD-OPh is a potent inhibitor of caspase-7 with an IC50 of 48 nM utilizing a cell-free assay consisting of human recombinant caspase-7, Q-VD-OPh, and the substrate AMC-DEVD-pNa. Q-VD-OPh fully inhibits caspase-3 and -7 activity at 0.05 μM. Caspase-8 is also inhibited at low Q-VD-OPh concentrations. The cleavage of PARP-1 is fully prevented at 10 μM Q-VD-OPh. DNA fragmentation and disruption of the cell membrane functionality are both prevented at 2 μM Q-VD-OPh. Q-VD-OPh is significantly more effective in preventing apoptosis than the widely used inhibitors, ZVAD-fmk and Boc-D-fmk, and is also equally effective in preventing apoptosis mediated by the three major apoptotic pathways, caspase 9/3, caspase 8/10, and caspase12. Q-VD-OPh is not toxic to cells even at extremely high concentrations. QVD is also able to increase the expression of differentiation markers in a
体内研究(In Vivo)
Chronic treatment with Q-VD-OPh prevents caspase-7 activation and limits the pathological changes associated with tau, including caspase cleavage. Q-VD-OPh could be a potential therapeutic compound for the treatment of Alzheimers disease. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
参考文献
[1]. Rohn TT, 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.
[2]. Kuzelová K, et al. Dose-dependent effects of the caspase inhibitor Q-VD-OPh on different apoptosis-related processes. J Cell Biochem. 2011 Nov;112(11):3334-42.
溶解度数据
In Vitro: DMSO : 100 mg/mL (194.75 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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