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Conduritol B epoxide

Conduritol B epoxide

产品编号 TQ0300   CAS 6090-95-5

Conduritol B epoxide 是不可逆的,β-glucosidase 共价抑制剂。

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Conduritol B epoxide Chemical Structure
Conduritol B epoxide, CAS 6090-95-5
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
产品目录号及名称: Conduritol B epoxide (TQ0300)
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纯度: 100%
纯度: 99.85%
纯度: 99.85%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Conduritol B epoxide is an irreversible inhibitor of β-glucosidase (GCase).
体外活性 Treating N2a and Conduritol B epoxide-N2a cells with G6 gave GC reductions to 7% and 26% of untreated levels, respectively. G6 treated Conduritol B epoxide-N2a also has significantly decreased GS. Conduritol B epoxide-N2a cells have higher calcium levels than in N2a cells without caffeine at baseline. Conduritol B epoxide-N2a cells show a significant increase in cytosolic calcium levels compared to N2a cells. Conduritol B epoxide-N2a cells show a significant reduction in OCR as evidenced by approximately 50% in all the parameters, including the rate of ATP production, basal respiration, and maximal respiration, compared to N2a cells. In dantrolene-treated Conduritol B epoxide-N2a cells, levels of Ryr3 are increased to 76% of the WT level [1].
体内活性 Conduritol B epoxide treatment of 4L, 9H, 9V and WT mice (100 mg/kg/day, i.p.) from postnatal days 5 to 11 does not induce α-synuclein aggregates. Long-term daily Conduritol B epoxide treatment of 4L mice (100 mg/kg/day of Conduritol B epoxide from postnatal day 15 for 24 or 36 doses) leads to hind limb paralysis and small amounts of α-synuclein accumulation in the olfactory bulb, brainstem, and PVP near D3V (dorsal 3rd ventricle) [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

TQ0300_1

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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 50 mg/mL (308.38 mM), sonification is recommended.

H2O: ≥20 mg/mL (123.35 mM)

溶液配制表

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

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Liou B, et al. Modulating ryanodine receptors with dantrolene attenuates neuronopathic phenotype in Gaucher disease mice. Hum Mol Genet. 2016 Sep 20. pii: ddw322. [Epub ahead of print] 2. YH Xu, et al. Accumulation and distribution of α-synuclein and ubiquitin in the CNS of Gaucher disease mouse models. Mol Genet Metab. Author manuscript; available in PMC 2012 Apr 1
Butyl isobutyl phthalate Pinoresinol diglucoside Kaempferol-3,7-di-O-β-glucoside IHVR-17028 α-Glucosidase-IN-4 α-Glucosidase-IN-39 GCase modulator-1 α-Glucosidase-IN-38

相关化合物库

该产品包含在如下化合物库中:
代谢化合物库 抑制剂库 已知活性化合物库 经典已知活性库 NO PAINS 化合物库 激酶抑制剂库 糖代谢化合物库 共价抑制剂库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

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。

Keywords

Conduritol B epoxide 6090-95-5 Metabolism Glucosidase inhibit Inhibitor inhibitor

 

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