2. Membrane Transporter/Ion Channel NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  3. EAAT Reactive Oxygen Species (ROS)
  4. HCM-01

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.

For research use only. We do not sell to patients.

HCM-01

HCM-01 Chemical Structure

CAS No. : 2117631-52-2

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HCM-01 Related Antibodies

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Description

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[1].

IC50 & Target[1]

EAAT2

 

In Vitro

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.

HCM-01 Related Antibodies

Cell Viability Assay[1]

Cell Line: primary neuronal cultures derived from hippocampus, cortex, and cerebellum
Concentration: 0.1 μM; 1 μM; 10 μM; 100 μM; 1000 μM
Incubation Time: 24 h
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.

Western Blot Analysis[1]

Cell Line: C8-D1A astrocytic cells
Concentration: 1 μM
Incubation Time: 24 h
Result: Increased EAAT2 expression in C8-D1A astrocytic cells under glutamate-induced excitotoxic conditions without affecting cell viability.
In Vivo

HCM-01 (50-100 mg/kg; p.o. or i.p.; once daily for 24 days) improves cognitive function, reduces hippocampal neuronal degeneration, attenuates tau and β-amyloid pathology, and restores cholinergic function in Streptozotocin (HY-13753)-induced Alzheimer's disease-like rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley (female; streptozotocin-induced Alzheimer's disease model)[1]
Dosage: 50 mg/kg; 100 mg/kg
Administration: p.o. or i.p.; once daily for 24 days
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.).
Molecular Weight

660.72

Formula

C37H36N6O6
CAS No.
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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Room temperature in continental US; may vary elsewhere.
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Purity & Documentation
References
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HCM-01 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HCM-012117631-52-2HCM01HCM 01EAATReactive Oxygen Species (ROS)Excitatory amino acid transporter Glutamate transporter| hippocampal regionsSprague-Dawley ratsEAAT2glutamate homeostasisExcitatory amino acid transporter 2C8-D1A astrocytic cellsAlzheimer's diseaseprimary hippocampal neuronsastrocytestau pathologyInhibitorinhibitorinhibit

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