Conduritol B epoxide
(Synonyms: 1,2-脱水肌醇,CBE) 目录号 : GC18058
An irreversible inhibitor of glucocerebrosidase
Cas No.:6090-95-5
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >97.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
|
Kinase experiment: |
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. |
|
Animal experiment: |
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 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 last injection. Mice are perfused with PBS and organs are harvested for enzyme activity, lipid and histological analyses. |
|
References: [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] |
|
IC50: 9 μM
Conduritol B epoxide is a β-glucosidase inhibitor.
β-glucosidase catalyzes the hydrolysis of the glycosidic bond to terminal non-reducing residues in β-D-glucosides and oligosaccharides, with release of glucose.
In vitro: Conduritol B epoxide was identifies as an active-site-directed inhibitor of some glucosidases. The inactivation of α-glucosidase from Monascus ruber by conduritol B epoxide was found to be irreversible and first-order with respect to time and inhibitor concentration. The inactivation could be prevented in the presence of maltose [1].
In vivo: The time course of the distribution of [3H]conduritol B epoxide was determined in various organs of mice, which had received a single i.p. dose. Results showd that the epoxide was rapidly distributed over all tissues except brain, indicating that the epoxide could pass the blood/brain barrier only with difficulty. A 4-fold enrichment was observed in the kidney. [3H]conduritol B epoxide was excreted with a half-life of about 7 h. A parallel determination of beta-glucosidase activity in the tissues showed greater than 90% inhibition within 1 and 2 h and a beginning recovery between 4 and 12 h. The only exception was brain, where no effects could be found after 1 h and a subsequent decrease to 37% of normal was seen after 12 h [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Yang SJ, Ge SG, Zeng YC, Zhang SZ. Inactivation of alpha-glucosidase by the active-site-directed inhibitor, conduritol B epoxide. Biochim Biophys Acta. 1985 Apr 29;828(3):236-40.
[2] Stephens MC, Bernatsky A, Singh H, Kanfer JN, Legler G. Distribution of conduritol B epoxide in the animal model for Gaucher's disease (Gaucher mouse). Biochim Biophys Acta. 1981 Jan 7;672(1):29-32.
| Cas No. | 6090-95-5 | SDF | |
| 别名 | 1,2-脱水肌醇,CBE | ||
| 化学名 | 1,2-anhydro-myo-inositol | ||
| Canonical SMILES | O[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)[C@H]2[C@@H]1O2 | ||
| 分子式 | C6H10O5 | 分子量 | 162.1 |
| 溶解度 | ≤25mg/ml in DMSO;10mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 6.169 mL | 30.8452 mL | 61.6903 mL |
| 5 mM | 1.2338 mL | 6.169 mL | 12.3381 mL |
| 10 mM | 0.6169 mL | 3.0845 mL | 6.169 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。