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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
24 Results for "
glutamate uptake
" in MedChemExpress (MCE) Product Catalog:
Products (24)
24 Results for "glutamate uptake" in MCE Product Catalog:
48
Research Areas:
Methyllycaconitine (MLA) citrate is a blood-brain barrier-permeable antagonist of α7 nicotinic acetylcholine receptor (α7nAChR) with an IC50 of 2 nM. Methyllycaconitine citrate inhibits Aβ25-35-induced autophagy by restoring the mTOR pathway, and prevents reactive oxygen species (ROS) production, microglial activation, reduced dopamine uptake, loss of dopaminergic terminals and catecholamine secretion. Methyllycaconitine citrate induces hippocampal glutamate efflux, enhances long-term potentiation, and improves memory acquisition. Methyllycaconitine citrate can be used in research related to Alzheimer's disease, cerebral palsy, Parkinson's disease and schizophrenia .
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32 Cited Publications
Synonyms: Direct Blue 53; T-1824; C.I. 23860
Research Areas:
Evans Blue (Direct Blue 53; T-1824; C.I. 23860) is a potent inhibitor of L-glutamate uptake via the membrane bound excitatory amino acid transporter (EAAT). Evans Blue is a L-glutamate and kainate receptor-mediated currents inhibitor. Evans Blue has a strong affinity towards serum albumin, making it a high molecular weight protein tracer. Evans Blue is also used to study BBB (blood-brain barrier) permeability .
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TFB-TBOA (CF3-Bza-TBOA) is a potent glutamate transporter blocker that potently suppresses the activity of glial transporters. TFB-TBOA shows IC50 values of 22, 17, and 300 nM for glutamate transporters EAAT1, EAAT2, and EAAT3 respectively in an uptake assay using cells transiently expressing EAATs .
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2 Cited Publications
Target:
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Dihydrokainic acid is a glutamate transporters (especially GLT1) inhibitor. Dihydrokainic acid targets GLT1 with high affinity, effectively inhibiting its transport function. Dihydrokainic acid exerts its effect by inhibiting the uptake of glutamate, leading to an increase in extracellular glutamate concentration, thereby affecting neuronal excitability and neurotransmission. Dihydrokainic acid is mainly applied in the field of neuroscience for research on glutamate-related neural functions, epilepsy, learning, and memory .
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1 Cited Publications
Target:
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DL-TBOA is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA inhibits the uptake of [ 14C]glutamate in COS-1 cells expressing the human EAAT1 and EAAT2 with Ki valuesof 42 μM and 5.7 μM, respectively. DL-TBOA blocks EAAT4 and EAAT5 in a competitive manner with Ki values of 4.4 μM and 3.2 μM, respectively .
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1
1 Cited Publications
Cat. No.: HY-16974
CAS No.: 1093861-60-9
Target:
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Afoxolaner is an orally active isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect γ-aminobutyric acid receptor (GABA) and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod .
Cat. No.: HY-162455
CAS No.: 3041127-59-4
Target:
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NA-014 is an excitatory amino acid transporter 2 (EAAT2)-selective positive allosteric modulator. NA-014 increases EAAT2-mediated glutamate uptake. NA-014 can be used for the research of epilepsy, neuropathic pain, stroke, drugs of abuse disorders .
Cat. No.: HY-W585874
CAS No.: 5746-03-2
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Nε-(Carboxyethyl) lysine is an advanced glycation end product (AGE). Nε-(Carboxyethyl) lysine induces cross-linking between proteins, thereby affecting protein structure and function and causing protein denaturation. Nε-(Carboxyethyl) lysine binds to the RAGE receptor, affects cell signal transduction, and regulates processes such as inflammatory responses, cell proliferation, and apoptosis. Nε-(Carboxyethyl) lysine affects glutamate transporters, reduces glutamate uptake and S100β protein secretion, influences neurotransmission in the nervous system, and exhibits diabetes-related neurotoxicity .
Cat. No.: HY-101227
CAS No.: 63088-04-0
Target:
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(±)-threo-3-Methylglutamic acid is a potent EAAT2/4 inhibitor. (±)-threo-3-Methylglutamic acid also is an ionotropic glutamate receptor agonist. (±)-threo-3-Methylglutamic acid inhibits glutamate uptake by rod outer segments .
Cat. No.: HY-16974R
CAS No.: 1093861-60-9
Research Areas:
Afoxolaner (Standard) is the analytical standard of Afoxolaner. This product is intended for research and analytical applications. Afoxolaner is an orally active isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect γ-aminobutyric acid receptor (GABA) and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod .
Cat. No.: HY-108385
CAS No.: 1448049-50-0
Target:
Isotope-Labeled Compounds Endogenous Metabolite DNA/RNA Synthesis PPAR Reactive Oxygen Species (ROS) Apoptosis Fungal
Research Areas:
Ochratoxin A-D4 (Phe-OTA-D4) is the deuterium labeled Ochratoxin A. Ochratoxin A is an orally active food-borne mycotoxin that can cross the blood-brain barrier. Ochratoxin A is a secondary metabolite of fungi belonging to the genera Aspergillus and Penicillium, and is classified as a Group 2B carcinogen. Ochratoxin A exerts its effects through multiple pathways, including inducing oxidative stress, inhibiting mitochondrial respiration, causing oxidative DNA damage, disrupting the PPAR-γ-CD36 axis, inducing immunosuppression, generating ROS, mediating mitochondria-dependent apoptosis, inhibiting glutamate uptake, triggering demyelination and neuroinflammation, inducing DNA hypomethylation, and inhibiting cell proliferation. Ochratoxin A can induce nephrotoxicity, hepatotoxicity, immunotoxicity, and neurotoxicity, and also exhibits mutagenicity, teratogenicity, and carcinogenicity.
Cat. No.: HY-107522B
CAS No.: 2093503-71-8
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DL-TBOA ammonium is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA ammonium inhibits the uptake of [ 14C]glutamate in COS-1 cells expressing the human EAAT1 and EAAT2 with Ki valuesof 42 μM and 5.7 μM, respectively. DL-TBOA ammonium blocks EAAT4 and EAAT5 in a competitive manner with Ki values of 4.4 μM and 3.2 μM, respectively .
Cat. No.: HY-122487A
CAS No.: 1926204-76-3
Synonyms: BHV-4157 hydrochloride
Target:
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Troriluzole hydrochloride is a third-generation peptide precursor of Riluzole (HY-B0211) and is an orally active glutamate modulator. Troriluzole hydrochloride can reduce synaptic glutamate levels and enhance the uptake of synaptic glutamate. Troriluzole hydrochloride shows potential for treating Alzheimer's disease and Generalized Anxiety Disorder (GAD) .
Cat. No.: HY-175296
Target:
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EAAT2 activator 2 (Compound 4(SF-2)) is a brain-penetrant excitatory amino acid transporter 2 (EAAT2) modulator (Ki=28.7 nM). EAAT2 activator 2 enhances EAAT2-mediated glutamate uptake, improving synaptic glutamate clearance. EAAT2 activator 2 is promising for research of neurodegenerative diseases (e.g., ALS, Alzheimer’s disease) .
Synonyms: cis-1-Aminocyclobutane-1,3-dicarboxylic acid
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cis-ACBD is a potent and selective inhibitor of the high-affinity, Na +-dependent plasma membrane glutamate transporter. cis-ACBD is a glutamate reuptake inhibitor. cis-ACBD also acts as linear competitive inhibitor of the uptake of D-[3H]aspartate .
Cat. No.: HY-100838
CAS No.: 117857-95-1
Synonyms: L-CCG III
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Cat. No.: HY-16974S
Cat. No.: HY-182941
Target:
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Parawixin10 (Compound 2) is an N-acylpolyamine. Parawixin10 fails to enhance glutamate uptake in radioligand uptake assays of EAAT1, EAAT2 or EAAT3. Parawixin10 exhibits no positive allosteric modulatory activity in radioligand uptake assays of EAAT1−EAAT3, nor can it improve neuronal survival rates in mice in a dose-dependent and statistically significant manner. Parawixin10 has no neuroprotective activity .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
