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- CAS号:
304448-55-3
- 规格:
1mg/1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg
| 规格: | 1mg | 产品价格: | ¥146.0 |
|---|---|---|---|
| 规格: | 1mLx10mM(inDMSO) | 产品价格: | ¥510.0 |
| 规格: | 5mg | 产品价格: | ¥303.0 |
| 规格: | 10mg | 产品价格: | ¥462.0 |
| 规格: | 25mg | 产品价格: | ¥856.0 |
| 规格: | 50mg | 产品价格: | ¥1488.0 |
| 规格: | 100mg | 产品价格: | ¥2104.0 |
Product Introduction
Bioactivity
| 名称 | Dynasore |
| 描述 | Dynasore (Dynamin Inhibitor I) is a highly selective, reversible small-molecule dynamin inhibitor with an IC₅₀ of 15 μM. Dynasore also inhibits the mitochondrial dynamin Drp1 without affecting other small GTPases. By inhibiting the GTPase activity of dynamin, Dynasore blocks its function in membrane fission, thereby inhibiting clathrin-mediated endocytosis. Dynasore can be used in research on endocytosis, membrane transport, viral entry, and receptor signaling regulation. |
| 细胞实验 | Mouse ventricular myocytes are isolated from male adult C6/Black mouse. Cardiomyocytes subjects to 2 hours of drug treatment followed by oxidative stress (30 μM Water2 for 35 min). For ATP supplement experiments, the cells are treated with 3 mM ATP for 30 min before exposure to Water2. Cardiomyocyte survival and viability are analyzed by trypan blue exclusion (TBE) assay[3]. |
| 激酶实验 | RIP1 kinase assay: Phosphorylation of RIP1 requires its kinase activity. Expression constructs of FLAGtagged wild-type (WT) or a kinase-inactive point mutant of RIP1 (K45M) are are transfected into 293T cells and RIP1 kinase assay is performed as described in the Methods in the presence of [γ-32P]ATP for 30 min at 30℃. Samples are subjected to SDS-PAGE and RIP1 band is visualized by autoradiography. Relative intensities of radioactive bands are quantified and are shown (ratio) in this and all other autoradiographs. In parallel to kinase reactions, a sample of beads is subjected to western blot analysis using anti-RIP1 antibody to ensure equal protein amounts in kinase reactions. |
| 体外活性 | 方法:小鼠骨髓来源巨噬细胞加入 5, 10, 25, 50 μM Dynasore 预处理 1 小时,然后用 100 ng/mL LPS 刺激 24 小时,收集上清和细胞裂解液。实时定量 PCR 检测促炎细胞因子表达水平。 结果:Dynasore 剂量依赖性抑制 LPS 诱导的促炎细胞因子(TNF-α, IL-6, IL-12)的 mRNA 和蛋白水平。[1] 方法:HCLE 细胞(Fluo-4 负载)加入 40 μM Dynasore 或 1 μM YM-58483 预处理 30 分钟,然后加入 1 mM tBHP 诱导氧化应激,实时监测荧光强度监测 2 小时 内的胞质钙变化。 结果: Dynasore 完全阻止了 tBHP 诱导的胞质钙升高。[2] 方法:从成年大鼠制备包含孤束和孤束核的脑干水平切片。采用全细胞膜片钳技术记录 NTS 神经元,钳制电压-60 mV。100 μM Dynasore 溶于人工脑脊液,通过灌流系统持续给药。记录不同时间点(给药前、给药中、洗脱后)的突触后电流。 结果: Dynasore 迅速增加自发性兴奋性突触后电流频率,同时,ST 诱发的 EPSC 逐渐失败直至完全阻断,且恢复期未能逆转。[3] |
| 体内活性 | 方法:C57BL/6J 小鼠通过气管内滴注 LPS(10 mg/kg) 建立 ALI 模型,Dynasore (10, 30, 50 mg/kg)在 LPS 刺激前 3 小时通过腹腔注射单次给药预处理,LPS 刺激 24 小时后处死小鼠。 结果:Dynasore 预处理(尤其 30 和 50 mg/kg)显著降低了肺组织病理学评分,炎症因子降低。[1] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | Ethanol : 1.6 mg/mL (4.96 mM), Sonication is recommended. DMSO : 120 mg/mL (372.31 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (12.41 mM), Sonication is recommended. |
| 关键字 | VirusProtease | Virus Protease | Inhibitor | inhibit | HSV | Herpes simplex virus | Dynasore | Dynamin1/2 | Dynamin | Autophagy |
| 相关产品 | Guanidine hydrochloride | Naringin | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Hemin | Hydroxychloroquine | Sildenafil citrate | Stavudine | Tamoxifen | Thymidine | Paeonol |
| 相关库 | Inhibitor Library | Bioactive Compound Library | Bioactive Compounds Library Max | Autophagy Compound Library | Mitochondria-Targeted Compound Library | Anti-Infection Compound Library | Highly Selective Inhibitor Library | Anti-Aging Compound Library | Cytoskeletal Signaling Pathway Compound Library | Protease Inhibitor Library | Anti-Viral Compound Library | Human Metabolite Library |
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文献和实验网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广,其数量几乎占已知有机化合物的三分之一,用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等,都含有杂环化合物的结构。生物碱多是中草药的有效成分,绝大多数是含氮的杂环化合物。本章内容与医学关系密切,具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式(Ⅰ)和(Ⅱ)两种结构的高能化合物。其作用为贮藏能量(例如 ATP、肌酸磷酸)和作为产生 ATP源的中间代谢产物(例如磷酸烯醇丙酮酸)以及合成反应的中间物质(例如酰基辅酶 A),在蛋白质的结构( conformation)变化周期的第一阶段上(例如钠钾 ATP酶的羧基磷酸中间体)也具有重要作用。多数高等化合物具有磷酸基,但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质,不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开,而必须用化学方法才能分离。
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