Egalognastat
Based on 1 Customer Validation
Egalognastat (ASN90) is a selective, brain-penetrant and orally active O-GlcNAcase (OGA) enzyme inhibitor with an IC50 value of 10.2 nM. Egalognastat increases O-GlcNAcylation of intracellular proteins like tau and α-synuclein, preventing their aggregation and toxicity. Egalognastat does not inhibit hexosaminidase (Hex). Egalognastat can be used for the research of neurodegenerative diseases, such as tauopathies and α-synucleinopathies (e.g., Alzheimer’s disease and Parkinson’s disease).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.03%
- CAS No.: 1884154-02-2
- 화학식: C17H21N5O3S
- 분자량:375.45
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Neuronal Signaling Compound Library
HY-L013
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CNS-Penetrant Compound Library
HY-L028
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Orally Active Compound Library
HY-L061
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Anti-Alzheimer's Disease Compound Library
HY-L069
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Anti-Parkinson's Disease Compound Library
HY-L085
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Neurodegenerative Disease-related Compound Library
HY-L086
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Highly Selective Inhibitors Library
HY-L158
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Extracellular Vesicles (EVs) Compound Library
HY-L168
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
Egalognastat (ASN90) inhbibits O-GlcNAcase (OGA) by substrate competition and reversible binding[1].
Egalognastat induces protein O-GlcNAcylation in plated human and rodent PBMC with EC50 values of 209 nM and 489 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Egalognastat (30-100 mg/kg; oral administration; once a day; administered for 3.5 months) reduces pathological tau protein in the cerebral cortex and hippocampus and alleviates neurofibrillary tangle-like pathology in P301S tau transgenic mice[1].
Egalognastat (30-100 mg/kg; oral administration; once a day; administered for 4 days) improves upper airway dysfunction in 7-month-old P301L tau transgenic mice[1].
Egalognastat (30-100 mg/kg; oral administration; once a day; administered for 6 months) improves motor behavior and increases survival rate in 3.5-month-old P301L tau transgenic mice[1].
Egalognastat (30-100 mg/kg; oral administration; once a day; administered for 24 weeks) improves motor function, reduces astrogliosis, and promotes O-GlcNAcylation of α-synuclein in Line 61 α-synuclein transgenic mice.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Homozygous female hTauP301L mice (7 months of age), the model is generated by crossing two homozygous hTauP301L-Tg parental mice in the FVB/N background[1].
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Dosage:30 mg/kg and 100 mg/kg
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Administration:Oral gavage, once a day, 4 days
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Result:Significantly improved upper airway dysfunction.
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Animal Model:Homozygous female hTauP301L mice (3.5 months of age), the model is generated by crossing two homozygous hTauP301L-Tg parental mice in the FVB/N background[1].
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Dosage:30 mg/kg and 100 mg/kg
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Administration:Oral gavage, once a day, 6 months
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Result:Showed a tendency to decrease the clasping score.
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Animal Model:Male Line 61 α-synuclein transgenic mice (1 month of age), overexpress human α-synuclein throughout the brain under the Thy1 promoter[1].
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Dosage:30 mg/kg and 100 mg/kg
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Administration:Oral gavage, once a day, 24 weeks
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Result:A highly significant treatment benefit in three different types of beam walk was observed.
Indicated a statistically significant reduction of glial fibrillary astrocytic protein (GFAP) expression, indicative of a reduction of astrogliosis.
Chemical Information
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CAS No. 1884154-02-2
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Appearance Solid
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분자량 375.45
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화학식 C17H21N5O3S
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Color Light yellow to light brown
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SMILES
CC(NC1=NN=C(N2CCN(CC2)[C@H](C3=CC=C(OCO4)C4=C3)C)S1)=O
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Synonyms
ASN90
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (266.35 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (6.66 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.66 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6635 mL | 13.3174 mL | 26.6347 mL | 66.5868 mL |
| 5 mM | 0.5327 mL | 2.6635 mL | 5.3269 mL | 13.3174 mL | |
| 10 mM | 0.2663 mL | 1.3317 mL | 2.6635 mL | 6.6587 mL | |
| 15 mM | 0.1776 mL | 0.8878 mL | 1.7756 mL | 4.4391 mL | |
| 20 mM | 0.1332 mL | 0.6659 mL | 1.3317 mL | 3.3293 mL | |
| 25 mM | 0.1065 mL | 0.5327 mL | 1.0654 mL | 2.6635 mL | |
| 30 mM | 0.0888 mL | 0.4439 mL | 0.8878 mL | 2.2196 mL | |
| 40 mM | 0.0666 mL | 0.3329 mL | 0.6659 mL | 1.6647 mL | |
| 50 mM | 0.0533 mL | 0.2663 mL | 0.5327 mL | 1.3317 mL | |
| 60 mM | 0.0444 mL | 0.2220 mL | 0.4439 mL | 1.1098 mL | |
| 80 mM | 0.0333 mL | 0.1665 mL | 0.3329 mL | 0.8323 mL | |
| 100 mM | 0.0266 mL | 0.1332 mL | 0.2663 mL | 0.6659 mL |
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