Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Conduritol B epoxide 是不可逆的,β-glucosidase 共价抑制剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 197 | 现货 | ||
5 mg | ¥ 452 | 现货 | ||
10 mg | ¥ 725 | 现货 | ||
25 mg | ¥ 1,150 | 现货 | ||
50 mg | ¥ 1,940 | 现货 | ||
100 mg | ¥ 2,610 | 现货 | ||
500 mg | ¥ 5,990 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 497 | 现货 |
产品描述 | Conduritol B epoxide is an irreversible inhibitor of β-glucosidase (GCase). |
体外活性 | 对 N2a and Conduritol B epoxide-N2a细胞处理G6后,GC含量分别降至未处理水平的7%和26%。G6处理的Conduritol B epoxide-N2a细胞GS明显下降。与未加咖啡因的N2a细胞相比,Conduritol B epoxide-N2a细胞的钙水平更高。与N2a细胞相比,Conduritol B epoxide-N2a细胞细胞质钙水平显著增加。Conduritol B epoxide-N2a细胞在氧化消耗率(OCR)上表现出显著降低,包括ATP产生率、基础呼吸和最大呼吸速率的各项参数近50%下降。在dantrolene处理的Conduritol B epoxide-N2a细胞中,Ryr3水平增至WT水平的76%[1]。 |
体内活性 | Conduritol B epoxide对4L、9H、9V和WT小鼠(100 mg/kg/天,腹腔注射)从出生后第5天至第11天的治疗不会引发α-synuclein聚集。长期每日给予4L小鼠Conduritol B epoxide(自出生后第15天起,每日100 mg/kg,连续24或36次)会导致后肢瘫痪以及在嗅球、脑干和靠近D3V(第三脑室背侧)的PVP区域出现少量α-synuclein积累[2]。 |
激酶实验 | Cells are homogenized in 1% sodium taurocholate/1% Triton X-100. GCase activity is determined fluorometrically using 4MU-Glucose as the substrate in 0.25% sodium taurocholate, 0.25% Triton X-100 and 0.1M citric-phosphate buffer (pH 5.6). Brain tissues are homogenized in 1X PBS and incubated in 5 μM brain phosphatidylserine and 0.1M citric-phosphate buffer (pH 5.6) for GCase activity assay using 4MU-Glucose as substrate. Protein concentrations are determined by BCA assay using BSA as standard [1]. |
动物实验 | Gba1 point mutated 4L, 9H and 9V mice or WT mice are intraperitoneally injected with 100 mg/kg/day of Conduritol B epoxide. In short-term experiments, daily injections are initiated at postnatal day 5 and continued for 6 daily doses. The mice are sacrificed on day 12 or 2 months after the last injection. In long-term experiments, 4L mice are injected daily beginning at postnatal day 15 for 24 or 36 daily doses and sacrificed the day after the last injection. Mice are perfused with PBS and organs are harvested for enzyme activity, lipid, and histological analyses [2]. |
化合物与蛋白结合的复合物 |
X-ray structure of human acid-beta-glucosidase covalently bound to conduritol B epoxide |
分子量 | 162.14 |
分子式 | C6H10O5 |
CAS No. | 6090-95-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (308.38 mM), Sonication is recommended.
H2O: ≥20 mg/mL (123.35 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / H2O | 1 mM | 6.1675 mL | 30.8375 mL | 61.6751 mL | 154.1877 mL |
5 mM | 1.2335 mL | 6.1675 mL | 12.335 mL | 30.8375 mL | |
10 mM | 0.6168 mL | 3.0838 mL | 6.1675 mL | 15.4188 mL | |
20 mM | 0.3084 mL | 1.5419 mL | 3.0838 mL | 7.7094 mL | |
50 mM | 0.1234 mL | 0.6168 mL | 1.2335 mL | 3.0838 mL | |
100 mM | 0.0617 mL | 0.3084 mL | 0.6168 mL | 1.5419 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Conduritol B epoxide 6090-95-5 Metabolism Glucosidase inhibit Inhibitor inhibitor