| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
Conduritol B epoxide (formerly known as CBE) is an irreversible/covalent inhibitor of non-mammalian and mammalian β-glucosidase (GCase). β-glucosidase catalyzes the hydrolysis of the glycosidic bond to terminal non-reducing residues in β-D-glucosides and oligosaccharides, with release of glucose. When injected in mice it produces the bioactive compound and certain clinical and pathological characteristics of Gaucher disease. Conduritol B epoxide is a mechanism-based inhibitor which binds covalently to the catalytic site of acid β-glucosidase.
| ln Vitro |
G6 treatment decreased GC to 7% and 26% of untreated levels in N2a and Conduritol B Epoxide-N2a cells, respectively. Conduritol B Epoxide-N2a treated with G6 likewise demonstrated a markedly lower GS. In comparison to untreated levels, the GC of Conduritol B Epoxide-N2a cells was decreased to 7% and 26%, respectively. A comparable level of GC and GS decrease was observed upon co-treatment of G6 and dantrolene as compared to G6 alone, suggesting that G6 has a distinct effect on preventing substrate accumulation. Cytoplasmic calcium levels were considerably greater in Conduritol B epoxy-N2a cells compared to N2a cells. Conduritol B epoxy-N2a cells had higher calcium levels than baseline caffeine-calibrated N2a cells. lowered mitochondrial function in this nGD cell type was indicated by the OCR of Conduritol B epoxy-N2a cells, which was much lower than that of N2a cells. All parameters, including ATP generation rate, basal respiration, and maximal respiration, were lowered by roughly 50%. Ryr3 levels rose to 76% of WT levels in Conduritol B epoxy-N2a cells treated with dantrolene [1].
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| ln Vivo |
Following treatment from postnatal days 5 to 11, 4L, 9H, 9V, and WT mice do not develop α-synuclein aggregates in response to conduritol B epoxide (100 mg/kg/d, i.p.). When given 24 or 36 times a day starting on day 15 after birth, Conduritol B epoxide (100 mg/kg/d) caused hindlimb paralysis in 4L mice and reduced levels of α-synuclein in the brainstem and olfactory bulb. and buildup at the PVP close to the dorsal third ventricle, or D3V [2].
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| 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]
[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 |
| Molecular Formula |
C6H10O5
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|---|---|
| Molecular Weight |
162.141
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| Exact Mass |
162.0528
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| CAS # |
6090-95-5
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| Related CAS # |
6090-95-5;
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| SMILES |
O[C@H]1[C@@]2([H])O[C@@]2([H])[C@H](O)[C@@H](O)[C@@H]1O
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| InChi Key |
ZHMWOVGZCINIHW-FTYOSCRSSA-N
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| InChi Code |
InChI=1S/C6H10O5/c7-1-2(8)4(10)6-5(11-6)3(1)9/h1-10H/t1-,2-,3+,4+,5-,6+/m0/s1
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| Chemical Name |
(1R,2R,3S,4S,5R,6S)-7-oxabicyclo[4.1.0]heptane-2,3,4,5-tetrol
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| Synonyms |
Conduritol B epoxide Conduritol-B-epoxide CBE
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~100 mg/mL (~616.75 mM)
DMSO : ~50 mg/mL (~308.38 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (15.42 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (15.42 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (15.42 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (616.75 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 6.1675 mL | 30.8375 mL | 61.6751 mL | |
| 5 mM | 1.2335 mL | 6.1675 mL | 12.3350 mL | |
| 10 mM | 0.6168 mL | 3.0838 mL | 6.1675 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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