HCM-01
Based on 1 Customer Validation
HCM-01 is an Excitatory amino acid transporter 2 (EAAT2) activator with oral effectiveness and blood-brain barrier penetration.HCM-01 binds to the allosteric site of EAAT2, increases EAAT2 expression in astrocytes, enhances glutamate-handling capacity, and modulates glutamate homeostasis.HCM-01 acts as an antioxidant, improves oxidative/antioxidative balance and increases total antioxidant capacity. HCM-01 can be used for the research of Alzheimer's disease.
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- Pureté: 99.38%
- CAS No.: 2117631-52-2
- Formule: C37H36N6O6
- Masse moléculaire:660.72
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Stockage:
Store at room temperature 3 years.
In solvent -80°C, 2 years , -20°C, 1 year
Activité biologique
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EAAT2 |
HCM-01 (0.1-1000 μM; 24 h) confers significant neuroprotection against glutamate-induced excitotoxicity in primary hippocampal neurons, region-dependent protection in cortical and cerebellar cultures at concentrations of 0.1, 1, and 10 μM, while exhibiting cytotoxicity at 100 and 1000 μM[1].
HCM-01 (1 μM; 24 h) increases EAAT2 expression in C8-D1A astrocytic cells under glutamate-induced excitotoxic conditions without affecting cell viability[1].
HCM-01 (0.1-1000 μM; 24 h) improves oxidative/antioxidative balance in primary hippocampal neuronal cultures under glutamate-induced stress[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:primary neuronal cultures derived from hippocampus, cortex, and cerebellum
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Concentration:0.1 μM; 1 μM; 10 μM; 100 μM; 1000 μM
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Incubation Time:24 h
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Result:Exhibited region-dependent protection in cortical and cerebellar cultures at concentrations of 0.1, 1, and 10 μM.
Exhibited cytotoxicity at 100 and 1000 μM.
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Cell Line:C8-D1A astrocytic cells
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Concentration:1 μM
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Incubation Time:24 h
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Result:Increased EAAT2 expression in C8-D1A astrocytic cells under glutamate-induced excitotoxic conditions without affecting cell viability.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (female; streptozotocin-induced Alzheimer's disease model)[1]
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Dosage:50 mg/kg; 100 mg/kg
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Administration:p.o. or i.p.; once daily for 24 days
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Result:Reduced daily mean escape latencies in the Morris water maze to levels comparable to memantine-treated animals.
Increased step-through latency in the passive avoidance test up to 300 s on day 41, matching untreated control animals.
Left locomotor activity (total distance, mean speed, resting percentage) unchanged relative to control groups.
Resulted in hippocampal CA1/CA2 region histopathological score of 0.16, matching untreated control and sham groups.
Reduced hippocampal CA3 region neuronal degeneration to scores of 1.83 (50 mg/kg p.o.), 1.66 (100 mg/kg p.o.), and 1.66 (50 mg/kg i.p.).
Attenuated tau immunopositivity in hippocampal CA1/CA2 region to scores of 1.16 (50 mg/kg p.o., 50 mg/kg i.p.) and 1.66 (100 mg/kg p.o.).
Attenuated tau immunopositivity in hippocampal CA3 region to scores of 2.00 (50 mg/kg p.o.), 2.83 (100 mg/kg p.o.), and 1.33 (50 mg/kg i.p.).
Eliminated β-amyloid immunopositivity in hippocampal CA1/CA2 and CA3 regions, matching control groups.
Reduced AChE immunopositivity in hippocampal CA3 region to scores of 2.16 (50 mg/kg p.o.), 1.33 (100 mg/kg p.o.), and 1.16 (50 mg/kg i.p.).
Chemical Information
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CAS No. 2117631-52-2
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Appearance Solid
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Masse moléculaire 660.72
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Formule C37H36N6O6
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Color Light yellow to yellow
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SMILES
O=C(C1=C(C)N=C(C)C(C(NCCC2=CNC3=C2C=C(OC)C=C3)=O)=C1C4=C([N+]([O-])=O)C=CC=C4)NCCC5=CNC6=C5C=C(OC)C=C6
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Store at room temperature 3 years
In solvent -80°C 2 years -20°C 1 year
Solvant et solubilité
DMSO : 100 mg/mL (151.35 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (3.78 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
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 (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5135 mL | 7.5675 mL | 15.1350 mL | 37.8375 mL |
| 5 mM | 0.3027 mL | 1.5135 mL | 3.0270 mL | 7.5675 mL | |
| 10 mM | 0.1514 mL | 0.7568 mL | 1.5135 mL | 3.7838 mL | |
| 15 mM | 0.1009 mL | 0.5045 mL | 1.0090 mL | 2.5225 mL | |
| 20 mM | 0.0757 mL | 0.3784 mL | 0.7568 mL | 1.8919 mL | |
| 25 mM | 0.0605 mL | 0.3027 mL | 0.6054 mL | 1.5135 mL | |
| 30 mM | 0.0505 mL | 0.2523 mL | 0.5045 mL | 1.2613 mL | |
| 40 mM | 0.0378 mL | 0.1892 mL | 0.3784 mL | 0.9459 mL | |
| 50 mM | 0.0303 mL | 0.1514 mL | 0.3027 mL | 0.7568 mL | |
| 60 mM | 0.0252 mL | 0.1261 mL | 0.2523 mL | 0.6306 mL | |
| 80 mM | 0.0189 mL | 0.0946 mL | 0.1892 mL | 0.4730 mL | |
| 100 mM | 0.0151 mL | 0.0757 mL | 0.1514 mL | 0.3784 mL |