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Pathways Recommended:	Membrane Transporter/Ion Channel

Results for "

glutamate transporters

" in MedChemExpress (MCE) Product Catalog:

By Targets:	EAAT (9) GlyT (2) iGluR (2) Ferroptosis (1) FKBP (1) HIV (1)
By Research Areas:	Cardiovascular Disease (1) Infection (1) Metabolic Disease (1) Neurological Disease (14)

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Peptides

Targets Recommended: Glutamate Dehydrogenase (GLDH) GlyT mGluR iGluR EAAT

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-107521

TFB-TBOA 2 Publications Verification CF3-Bza-TBOA	EAAT	Neurological Disease
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 .

HY-139692

EAAT2 activator 1	EAAT	Neurological Disease
EAAT2 activator 1 is the potent activator of *excitatory amino acid transporter* 2 (EAAT2*). EAAT2 is the major glutamate* transporter and functions to remove glutamate from synapses. EAAT2 activator 1 increases EAAT2 protein levels dose-dependently .

HY-139087

Erastin2	Ferroptosis	Metabolic Disease
Erastin2, an Erastin (HY-15763) analog, is a ferroptosis inducer and a potent, selective inhibitor of the system xc(-) cystine/glutamate transporter

HY-100784

Dihydrokainic acid	EAAT	Neurological Disease
Dihydrokainic acid (DHK) is a glutamate transporter GLT1 (EAAT2) inhibitor. Dihydrokainic acid impairs novel object recognition (NOR) memory performance in mice. Dihydrokainic acid also shows epileptogenic effects .

HY-12741

LDN-212320 5+ Cited Publications LDN-0212320; OSU-0212320	EAAT	Neurological Disease
LDN-212320 (LDN-0212320) is a glutamate transporter (GLT-1)/*excitatory amino acid transporter* 2 (EAAT2)** activator (at translational level). LDN-212320 (LDN-0212320) prevents nociceptive pain by upregulating astroglial GLT-1 expression in the hippocampus and ACC ^[1]

HY-100836

trans-4-Carboxy-L-proline	iGluR	Neurological Disease
Trans-4-Carboxy-L-prolineis a selective glutamate transporter inhibitor .

HY-101334

MPDC	GlyT	Neurological Disease
MPDC is a potent and competitive inhibitor of the Na ⁺-dependent high-affinity **glutamate transporter** in forebrain synaptosomes .

HY-101334A

MPDC hydrochloride	GlyT	Neurological Disease
MPDC hydrochloride is a potent and competitive inhibitor of the Na ⁺-dependent high-affinity **glutamate transporter** in forebrain synaptosomes .

HY-100616

cis-ACBD cis-1-Aminocyclobutane-1,3-dicarboxylic acid	Others	Neurological Disease
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 .

HY-100838

cis-α-(Carboxycyclopropyl)glycine L-CCG III	EAAT	Neurological Disease
cis-α-(Carboxycyclopropyl)glycine (L-CCG III) is a potent, competitive glutamate uptake inhibitor. cis-α-(Carboxycyclopropyl)glycine is a substrate of glutamate transporters (GluT) (EC₅₀: 13 μM, 2 μM for EAAT 1 and EAAT 2, respectively). cis-α-(Carboxycyclopropyl)glycine inhibits a Na ⁺-dependent high-affinity L-glutamate uptake in glial plasmalemmal vesicles (GPV) and synaptosomes .

HY-B1102

Evans Blue Maximum Cited Publications 16 Publications Verification Direct Blue 53; T-1824; C.I. 23860	EAAT iGluR	Cardiovascular Disease Neurological Disease
Evans Blue (Direct Blue 53) 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 .

HY-107522

DL-TBOA	EAAT	Neurological Disease
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 K_i valuesof 42 μM and 5.7 μM, respectively. DL-TBOA blocks EAAT4 and EAAT5 in a competitive manner with K_i values of 4.4 μM and 3.2 μM, respectively .

HY-107522B

DL-TBOA ammonium	EAAT	Neurological Disease
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 K_i valuesof 42 μM and 5.7 μM, respectively. DL-TBOA ammonium blocks EAAT4 and EAAT5 in a competitive manner with K_i values of 4.4 μM and 3.2 μM, respectively .

HY-161062

TAOA AM Ester trimethyl lock	EAAT	Neurological Disease
TAOA AM Ester trimethyl lock is a high-affinity fluorescent prodrug-like inhibitor of the excitatory amino acid transporter (EAAT). It can penetrate the cell membrane and be activated by hydrolysis by endogenous cell esterases to form active EAAT inhibitors. TAOA AM Ester trimethyl lock can be used to study neurodegeneration and neuronal cell death .

HY-124619

GPI-1046	FKBP HIV	Infection Neurological Disease
GPI-1046 is a immunophilin ligand without antibiotic action and attenuates ethanol intake in part through the upregulation of glutamate transporter 1 (GLT1) in PFC and NAc-core. GPI-1046 is an analog of FK506, which is an immunophilin ligand that has been shown neuroprotective effects in neurodegenerative disease models . GPI-1046 readily crosses the blood-brain barrier and promotes the regeneration of dopamine (DA) cells in the CNS in association with functional recovery in rodent models . GPI-1046 improves HIV-associated injury of peripheral nerves .

Cat. No.	Product Name

HY-L064

Glutamine Metabolism Compound Library	973 compounds
Glutamine is an important metabolic fuel that helps rapidly proliferating cells meet the increased demand for ATP, biosynthetic precursors, and reducing agents. Glutamine Metabolism pathway involves the initial deamination of glutamine by glutaminase(GLS), yielding glutamate and ammonia. Glutamate is converted to the TCA cycle intermediate α-ketoglutarate (α-KG) by either glutamate dehydrogenase (GDH) or by the alanine or aspartate transaminases (TAs), to produce both ATP and anabolic carbons for the synthesis of amino acids, nucleotides and lipids. During periods of hypoxia or mitochondrial dysfunction, α-KG can be converted to citrate in a reductive carboxylation reaction catalyzed by IDH2. The newly formed citrate exits the mitochondria where it is used to synthesize fatty acids and amino acids and produce the reducing agent, NADPH. Cancer cells display an altered metabolic circuitry that is directly regulated by oncogenic mutations and loss of tumor suppressors. Mounting evidence indicates that altered glutamine metabolism in cancer cells has critical roles in supporting macromolecule biosynthesis, regulating signaling pathways, and maintaining redox homeostasis, all of which contribute to cancer cell proliferation and survival. Thus, intervention in glutamine metabolic processes could provide novel approaches to improve cancer treatment. MCE owns a unique collection of 973 compounds targeting the mainly proteins and enzymes involved in glutamine metabolism pathway. Glutamine Metabolism compound library is a useful tool for intervention in glutamine metabolic processes.

Glutamine Metabolism Compound Library

973 compounds

Glutamine is an important metabolic fuel that helps rapidly proliferating cells meet the increased demand for ATP, biosynthetic precursors, and reducing agents. Glutamine Metabolism pathway involves the initial deamination of glutamine by glutaminase(GLS), yielding glutamate and ammonia. Glutamate is converted to the TCA cycle intermediate α-ketoglutarate (α-KG) by either glutamate dehydrogenase (GDH) or by the alanine or aspartate transaminases (TAs), to produce both ATP and anabolic carbons for the synthesis of amino acids, nucleotides and lipids. During periods of hypoxia or mitochondrial dysfunction, α-KG can be converted to citrate in a reductive carboxylation reaction catalyzed by IDH2. The newly formed citrate exits the mitochondria where it is used to synthesize fatty acids and amino acids and produce the reducing agent, NADPH.

Cancer cells display an altered metabolic circuitry that is directly regulated by oncogenic mutations and loss of tumor suppressors. Mounting evidence indicates that altered glutamine metabolism in cancer cells has critical roles in supporting macromolecule biosynthesis, regulating signaling pathways, and maintaining redox homeostasis, all of which contribute to cancer cell proliferation and survival. Thus, intervention in glutamine metabolic processes could provide novel approaches to improve cancer treatment.

MCE owns a unique collection of 973 compounds targeting the mainly proteins and enzymes involved in glutamine metabolism pathway. Glutamine Metabolism compound library is a useful tool for intervention in glutamine metabolic processes.

Cat. No.	Product Name	Type

HY-B1102

Evans Blue 15+ Cited Publications Direct Blue 53; T-1824; C.I. 23860	Cell Assay Reagents
Evans Blue (Direct Blue 53) 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 .

Evans Blue

15+ Cited Publications

Direct Blue 53; T-1824; C.I. 23860

Cell Assay Reagents

Evans Blue (Direct Blue 53) 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 .

Cat. No.	Product Name	Target	Research Area

HY-100838

cis-α-(Carboxycyclopropyl)glycine L-CCG III	EAAT	Neurological Disease
cis-α-(Carboxycyclopropyl)glycine (L-CCG III) is a potent, competitive glutamate uptake inhibitor. cis-α-(Carboxycyclopropyl)glycine is a substrate of glutamate transporters (GluT) (EC₅₀: 13 μM, 2 μM for EAAT 1 and EAAT 2, respectively). cis-α-(Carboxycyclopropyl)glycine inhibits a Na ⁺-dependent high-affinity L-glutamate uptake in glial plasmalemmal vesicles (GPV) and synaptosomes .

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