| 名称 | Q-VD-OPH |
| 描述 | Q-VD-OPh is an irreversible caspase inhibitor with an IC50 value of 48 nM against caspase-7 and between 25 and 400 nM against caspase-1, 3, 8, 9, 10, 12. Q-VD-OPh inhibits HIV infection and can cross the blood-brain barrier. |
| 细胞实验 | Caspase inhibitors are added at the indicated concentrations 30 minutes prior to the addition of apoptotic stimuli. Viability and cell number are determined by trypan blue exclusion from three random fields of greater than 200 cells/field. All experiments are performed a minimum of three times.(Only for Reference) |
| 激酶实验 | Enzyme assay is conducted in buffer containing 25 mM Tris, pH 8.0, 1 mM DTT, 1 mM spermine, 50 mM KCl, 0.01% Nonidet P-40, and 1 mM MgCl2. PARP reaction contains 0.1 μCi [3H]NAD+ (200?000 DPM), 1.5 μM NAD+, 150 nM biotinylated NAD+, 1 μg/mL activated calf thymus, and 1?5 nM PARP-1. Autoreactions utilizing SPA bead-based detection are carried out in 50 μL volumes in white 96-well plates. Compounds (e.g., MK-4827) are prepared in 11-point serial dilution in 96-well plate, 5 μL/well in 5% DMSO/Water (10× concentrated). Reactions are initiated by adding first 35 μL of PARP-1 enzyme in buffer and incubating for 5 min at room temperature and then 10 μL of NAD+ and DNA substrate mixture. After 3 h at room temperature, these reactions are terminated by the addition of 50 μL of streptavidin-SPA beads (2.5 mg/mL in 200 mM EDTA, pH 8). After 5 min, they are counted using a TopCount microplate scintillation counter. IC50 data is determined from inhibition curves at various substrate concentrations[1]. |
| 体外活性 | 方法：心肌细胞用Q-VD-OPH处理后，使用 Flow Cytometry 方法检测细胞凋亡
结果：Q-VD-OPH能够保护心肌细胞免受病毒诱导的凋亡。[1] |
| 体内活性 | 方法：为研究Q-VD-OPH对细胞凋亡、免疫反应和病毒复制的影响，将SIVmac251 病毒静脉注射给中国猕猴来模拟 HIV 感染，将Q-VD-OPH（20 mg/kg）在第 5、7、9、11 和 14 天静脉注射给中国猕猴。
结果：Q-VD-OPH显著降低了外周淋巴结中 T 细胞的凋亡水平。Q-VD-OPh 治疗组的 TUNEL+ 细胞数量显著低于未治疗组。Q-VD-OPH治疗显著提高了 CD4+ T 细胞计数和 CD4/CD8 比值，减少了病毒复制。[2]
方法：为研究Q-VD-OPH对缺血性急性肾功能衰竭（ARF）的保护作用，将Q-VD-OPH（120 mg/kg）腹腔注射给小鼠。
结果：Q-VD-OPH在小鼠缺血性ARF中抑制caspase-1、IL-18蛋白表达和中性粒细胞浸润。[3]
方法：为研究Q-VD-OPH对心肌损伤的保护作用，在第3天至第6天将Q-VD-OPH（50 mg/kg）腹腔注射给感染病毒的小鼠。
结果：Q-VD-OPH通过抑制caspase来防护病毒引起的心肌损伤，降低 caspase-3 活性。[1]
方法：为研究Q-VD-OPH治疗AD的作用，将Q-VD-OPH（10 mg/kg）腹腔注射给TgCRND8小鼠，每周三次，持续三个月。
结果：Q-VD-OPH抑制 caspase-7活化，抑制包括caspase裂解在内的与tau蛋白相关的病理变化。[4] |
| 存储条件 | keep away from moisture,store at low temperature | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | Ethanol : 100 mg/mL (194.74 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (9.74 mM), Sonication is recommended.
DMSO : 260 mg/mL (506.33 mM), Sonication is recommended.
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| 关键字 | QVD-OPH | Q-VD-OPH | QVDOPH | Q VD OPH | Inhibitor | inhibit | Human immunodeficiency virus | HIVProtease | HIV Protease | HIV | Caspase-9 | Caspase-8 | Caspase-3 | Caspase-1 | Caspase |
| 相关产品 | Valproic Acid | (-)-Epigallocatechin Gallate | Dimethyl fumarate (Standard) | Emtricitabine | Dextran sulfate sodium salt (MW 5000) | Lamivudine | 5-Fluorouracil | Decanedioic acid | Stavudine | Lysozyme from chicken egg white | Cystamine dihydrochloride | Copper Sulfate Pentahydrate |
| 相关库 | 抑制剂库 | 经典已知活性库 | 已知活性化合物库 | 抗感染化合物库 | 含氟化合物库 | 抗衰老化合物库 | 蛋白酶抑制剂库 | NO PAINS 化合物库 | 抗病毒库 | 膜蛋白靶向化合物库 | 神经退行性疾病化合物库 | 共价抑制剂库 |