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Conduritol B epoxide 是不可逆的,β-glucosidase 共价抑制剂。
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Conduritol B epoxide 是不可逆的,β-glucosidase 共价抑制剂。
规格 | 价格 | 库存 | 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 x 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]. |
别名 | 1,2-脱水肌醇 |
分子量 | 162.14 |
分子式 | C6H10O5 |
CAS No. | 6090-95-5 |
Smiles | O[C@H]1[C@H]2O[C@H]2[C@H](O)[C@@H](O)[C@@H]1O |
密度 | 1.926g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 70 mg/mL (431.73 mM), Sonication is recommended. H2O: ≥20 mg/mL (123.35 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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