Conduritol B epoxide

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

CAS号

6090-95-5

分子式

C6H10O5

主要靶点

仅限科研使用

Cat No : CM00183

Print datasheet

Synonyms



产品信息

Conduritol B epoxide is an irreversible inhibitor of β-glucosidase (GCase).

CAS号 6090-95-5
分子式 C6H10O5
主要靶点
主要通路
分子量 162.14
纯度 99.85%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

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].

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].

溶解度

H2O:≥20 mg/mL (123.35 mM),DMSO:50 mg/mL (308.38 mM),Sonification is recommended.

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].

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

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
=
×
×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
×
=
×
C1   V1   C2   V2