Gcase activator 3
Based on 1 Customer Validation
Gcase activator 3 is a β-glucocerebrosidase (GCase) activator with an EC50 of 1.49 μM. By binding to the allosteric site of GCase, Gcase activator 3 partially stabilizes GCase and enhances its activity. Gcase activator 3 can be conjugated with fluorophores to form fluorescent probes, which are used for high-throughput screening of GCase. Gcase activator 3 is applicable to research related to Gaucher's disease, Parkinson's disease, dementia with Lewy bodies, and multiple system atrophy.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.67%
- CAS No.: 2270984-21-7
- Formule: C23H20N4O2
- Masse moléculaire:384.43
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
β-glucocerebrosidase 1.49 μM (EC50) |
In Vitro
Gcase activator 3 (compound 9q) (48 nM-100 μM; 5 min pre-incubation, 30 min reaction incubation) activates recombinant wild-type β-glucocerebrosidase, with an AC50 value of 1.49 μM and a maximum activity increase of up to 780%[1].
Gcase activator 3 (5-15 μM; 3 days) increases the protein level of post-endoplasmic reticulum mature β-glucocerebrosidase in healthy control fibroblasts[1].
Gcase activator 3 (5-15 μM; 3 days) increases the protein level of post-endoplasmic reticulum mature β-glucocerebrosidase in compound heterozygous GBA1N370S/84GG mutant fibroblasts[1].
Gcase activator 3 (5-15 μM; 3 days) dose-dependently increases lysosomal β-glucocerebrosidase activity in homozygous N370S and L444P GBA1 mutant fibroblasts[1].
Gcase activator 3 (5-15 μM; 10 days) increases the protein level of post-endoplasmic reticulum mature β-glucocerebrosidase in dopamine neurons derived from wild-type control induced pluripotent stem cells (iPSCs)[1].
Gcase activator 3 (5-15 μM; 10 days) increases the protein level of post-endoplasmic reticulum mature β-glucocerebrosidase in dopaminergic neurons differentiated from induced pluripotent stem cells (iPSC) derived from patients with heterozygous N370S GBA1 mutations[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Healthy control fibroblasts
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Concentration:5 μM; 15 μM
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Incubation Time:3 days
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Result:Increased post-ER (mature, lysosomal) GCase protein levels and enhanced GCase activity by 1.4-fold relative to vehicle control at 15 μM.
Showed no significant change in activity relative to control at 5 μM.
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Cell Line:Compound heterozygous N370S/84GG GBA1 mutant fibroblasts
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Concentration:5 μM; 15 μM
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Incubation Time:3 days
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Result:Increased post-ER (mature, lysosomal) GCase protein levels and enhanced GCase activity by 2.1-fold relative to vehicle control at 15 μM.
Showed no significant change in activity relative to control at 5 μM.
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Cell Line:Wild-type control induced pluripotent stem cell (iPSC)-derived dopaminergic neurons
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Concentration:5 μM; 15 μM
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Incubation Time:10 days
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Result:Increased post-ER (mature, lysosomal) GCase protein levels and enhanced GCase activity by 1.3-fold relative to vehicle control at 15 μM.
Showed no significant change in activity relative to control at 5 μM.
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Cell Line:Heterozygous N370S GBA1 mutant iPSC-derived dopaminergic neurons
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Concentration:5 μM; 15 μM
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Incubation Time:10 days
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Result:Increased post-ER (mature, lysosomal) GCase protein levels and enhanced GCase activity by 1.6-fold relative to vehicle control at 5 μM.
Increased post-ER (mature, lysosomal) GCase protein levels and enhanced GCase activity by 2.0-fold relative to vehicle control at 15 μM.
Chemical Information
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CAS No. 2270984-21-7
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Appearance Solid
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Masse moléculaire 384.43
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Formule C23H20N4O2
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Color White to off-white
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SMILES
CN(C[C@@H]1OC2=CC=CC=C2OC1)C3=C4C=CC=CC4=NC(C5=CC=CN=C5)=N3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (260.13 mM; Need ultrasonic; 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)
In Vivo:
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.
In Vivo Dissolution Calculator
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.
Pureté et documentation
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Fiche technique (286 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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Instruction de manipulation (2659 KB)
Références
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 |
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| DMSO | 1 mM | 2.6013 mL | 13.0063 mL | 26.0125 mL | 65.0313 mL |
| 5 mM | 0.5203 mL | 2.6013 mL | 5.2025 mL | 13.0063 mL | |
| 10 mM | 0.2601 mL | 1.3006 mL | 2.6013 mL | 6.5031 mL | |
| 15 mM | 0.1734 mL | 0.8671 mL | 1.7342 mL | 4.3354 mL | |
| 20 mM | 0.1301 mL | 0.6503 mL | 1.3006 mL | 3.2516 mL | |
| 25 mM | 0.1041 mL | 0.5203 mL | 1.0405 mL | 2.6013 mL | |
| 30 mM | 0.0867 mL | 0.4335 mL | 0.8671 mL | 2.1677 mL | |
| 40 mM | 0.0650 mL | 0.3252 mL | 0.6503 mL | 1.6258 mL | |
| 50 mM | 0.0520 mL | 0.2601 mL | 0.5203 mL | 1.3006 mL | |
| 60 mM | 0.0434 mL | 0.2168 mL | 0.4335 mL | 1.0839 mL | |
| 80 mM | 0.0325 mL | 0.1626 mL | 0.3252 mL | 0.8129 mL | |
| 100 mM | 0.0260 mL | 0.1301 mL | 0.2601 mL | 0.6503 mL |
Gcase activator 3 Related Classifications
HY-160426 Related Classifications
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Keywords
- Gcase activator 3
- 2270984-21-7
- Gcase activator3
- Gcase activator-3
- Glycosidase
- iPSC-derived dopaminergic neurons
- N370S/84GG GBA1 mutant fibroblasts
- L444P GBA1 mutant fibroblasts
- dementia with Lewy bodies
- healthy control fibroblasts
- multiple system atrophy
- N370S GBA1 mutant fibroblasts
- Gaucher's disease
- β-glucocerebrosidase
- Parkinson's disease
- Inhibitor
- inhibitor
- inhibit