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glutamate modulators

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115

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4

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1

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-12688A

    Mitochondrial Metabolism Reactive Oxygen Species (ROS) Amyloid-β Neurological Disease Inflammation/Immunology
    Succinyl phosphonate trisodium salt is a α-Ketoglutarate Dehydrogenase Complex (KGDHC) modulator with neuroprotective activity. Succinyl phosphonate trisodium salt protects this complex, reduces cellular succinyl-CoA concentration, downregulates protein succinylation levels, and inhibits the activity of the α-ketoglutarate dehydrogenase complex. Succinyl phosphonate trisodium salt corrects hypoxic or ethanol-induced behavioral impairments, modulates exploratory behavior and emotional stress responses, and improves hypoxia tolerance. Succinyl phosphonate trisodium salt reduces glutamate excitotoxicity, restores the activity of the α-ketoglutarate dehydrogenase complex, reverses the changes in glutamate dehydrogenase and glutamine synthetase activities induced by β-amyloid (Amyloid-β), modulates cognitive function, and prevents β-amyloid-induced neuronal damage. Succinyl phosphonate trisodium salt improves microglial senescence, alleviates neuroinflammation, reactive oxygen species (ROS) production, lipid peroxidation, and the expression of proinflammatory cytokines. Succinyl phosphonate trisodium salt can be used in the research of Alzheimer's disease, aging-related neuroinflammation, and Parkinson's disease .
    Succinyl phosphonate trisodium salt
  • HY-112171
    γ-L-Glutamyl-L-alanine
    1 Publications Verification

    γ-Glu-Ala

    Endogenous Metabolite CaSR Others
    γ-L-Glutamyl-L-alanine (γ-Glu-Ala), composed of gamma-glutamate and alanine, is a proteolytic breakdown product of larger proteins. γ-L-Glutamyl-L-alanine is a natural substrate of the γ-Glutamylcyclotransferase. γ-L-Glutamyl-L-alanine is a positive modulator of calcium-sensing receptor (CaR) function .
    γ-L-Glutamyl-L-alanine
  • HY-115864

    TAK-653; NBI-1065845

    iGluR Lipoxygenase Neurological Disease
    Osavampator (TAK-653) is a AMPA receptor positive allosteric modulator. Osavampator selectively binds to AMPA-R in a glutamate-dependent manner and induces Ca2+ influx in hGluA1i CHO cells (EC50 = 3.3 μM). Osavampator improves learning and memory in many models. Osavampator is can be used for the research of depressive disorders .
    Osavampator
  • HY-70057
    Safinamide
    2 Publications Verification

    FCE 26743; EMD 1195686

    Monoamine Oxidase Neurological Disease
    Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 μM) over MAO-A (IC50=580 μM) . Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 μM) than at resting (IC50=262 μM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al .
    Safinamide
  • HY-100403
    Ro 67-7476
    Maximum Cited Publications
    23 Publications Verification

    mGluR Cancer
    Ro 67-7476 is a potent positive allosteric modulator of mGluR1 and potentiates glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a with an EC50 of 60.1 nM . Ro 67-7476 is a potent P-ERK1/2 agonist and activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50=163.3 nM) .
    Ro 67-7476
  • HY-126752

    Reactive Oxygen Species (ROS) Neurological Disease Metabolic Disease Inflammation/Immunology
    Ophthalmic acid is a ubiquitous metabolite and glutathione modulator, with a Ki of 0.95 mM for glyoxalase I. Ophthalmic acid competitively inhibits glyoxalase I, glutathione S-transferase, glutaredoxin, glutamate-cysteine ligase, protein disulfide reductase (glutathione), as well as non-selective cation channels. Ophthalmic acid is applicable in diabetes-related research .
    Ophthalmic acid
  • HY-110175
    CX614
    1 Publications Verification

    iGluR Neurological Disease
    CX614 is a positive variant modulator of AMPA receptors that enhances excitatory postsynaptic potentials (amplitude and duration) by blocking and slowing the inactivation of responses to glutamate and automatically evokes excitatory postsynaptic currents in neuronal cultures. CX614 can be used in the study of psychiatric disorders such as depression .
    CX614
  • HY-101165
    Cyclothiazide
    2 Publications Verification

    iGluR GABA Receptor Neurological Disease
    Cyclothiazide is a positive allosteric modulator of ionotropic AMPA-type glutamate receptors. Cyclothiazide inhibits GABAA receptors. Cyclothiazide is frequently used to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current. Cyclothiazide can potentiate responses to kainate in hippocampal neurons. Cyclothiazide has effects on glutamatergic neurotransmission. Cyclothiazide also induces epileptiform EEG activity accompanying behavioral seizures .
    Cyclothiazide
  • HY-70057A
    Safinamide mesylate
    2 Publications Verification

    FCE 26743 mesylate; EMD 1195686 mesylate

    Monoamine Oxidase Cardiovascular Disease Neurological Disease
    Safinamide (FCE 26743; EMD 1195686) mesylate is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 μM) over MAO-A (IC50=580 nM) . Safinamide mesylate also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8?μM) than at resting (IC50=262?μM) potentials. Safinamide mesylate has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke et.al .
    Safinamide mesylate
  • HY-108710
    VU0650786
    2 Publications Verification

    mGluR Neurological Disease
    VU0650786 is a potent and selective CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM), with an IC50 of 392 nM. VU0650786 has antidepressant and anxiolytic activity in rodents .
    VU0650786
  • HY-N7144A

    Environmental Pollutants PKC TRP Channel PKA Neurological Disease
    Citronellyl acetate, a monoterpene product of the secondary metabolism of plants, is an orally active antinociceptive agent. Citronellyl acetate modulates TRPV1, TRPM8, ASIC, glutamate receptors, PKC, and PKA-mediated nociception. Citronellyl acetate can be used for the research of acute pain .
    Citronellyl acetate
  • HY-15748

    ADX-71149

    mGluR Neurological Disease
    JNJ-40411813 (ADX-71149) is a novel positive allosteric modulator of the metabotropic Glutamate 2 receptor (mGlu2R) with EC50 of 147 nM. JNJ-40411813 has orally bioactivity and penetrate the blood-brain barriers. JNJ-40411813 has the potential property of anti-depression .
    JNJ-40411813
  • HY-162455

    EAAT Neurological Disease
    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 .
    NA-014
  • HY-101310

    iGluR EAAT Bcl-2 Family Caspase Cardiovascular Disease Neurological Disease Inflammation/Immunology
    SYM 2081 is a kainate receptor agonist. SYM 2081 is a substrate of EAAT1 (Km of 54 μM). SYM 2081 inhibits EAAT2-mediated glutamate transport (Kb is 3.4 μM in Xenopus oocytes), modulates Apoptotic signaling pathways (increases Bcl-2 and decreases Bax/caspase-3 expression). SYM 2081 exhibits neuroprotective activity. SYM 2081 can be used in the study of hypoxic-ischemic brain damage and inflammatory or neuropathic pain .
    SYM 2081
  • HY-122487

    BHV-4157

    mGluR Neurological Disease Cancer
    Troriluzole, a third-generation, tripeptide proagent of Riluzole (HY-B0211), is an orally active glutamate modulator. Troriluzole reduces synaptic glutamate level and increases the synaptic glutamate absorption. Troriluzole has the potential for Alzheimer disease and generalized anxiety disorder (GAD) .
    Troriluzole
  • HY-18654
    ADX88178
    1 Publications Verification

    mGluR Neurological Disease
    ADX88178 is a potent metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 4 nM for human mGluR4.
    ADX88178
  • HY-13058
    ADX-47273
    1 Publications Verification

    mGluR Neurological Disease
    ADX-47273 is a potent, selective and brain-penetrant mGluR5 positive allosteric modulator (PAM), with an EC50 of 0.17 μM for potentiation of glutamate (50 nM) response. ADX-47273 has antipsychotic and procognitive activities .
    ADX-47273
  • HY-122559

    mGluR Neurological Disease
    BMS-984923, a potent mGluR5 silent allosteric modulator (SAM), with exquisite binding affinity (Ki = 0.6 nM), exhibits good oral bioavailability and BBB penetration. BMS-984923 potently inhibits the PrPC-mGluR5 interaction and prevents pathological Aβo signaling without affecting physiological glutamate signaling .
    BMS-984923
  • HY-107520

    Drug Derivative Neurological Disease
    MNI-caged-L-glutamate is an inert photolabile glutamate precursor. MNI-caged-L-glutamate does not modulate NMDA and AMPA receptor function in cultured neurones. MNI-caged-L-glutamate can be used for research on neurotransmitters .
    MNI-caged-L-glutamate
  • HY-177873

    iGluR Neurological Disease
    AMPA receptor modulator-10 (Compound 9a) is an orally active AMPA receptor (AMPAR) positive allosteric modulator. AMPA receptor modulator-10 exhibits potent activity (pEC50 = 5.0) on the GluA2 subtype of AMPAR, significantly enhancing glutamate-induced calcium influx and current responses. AMPA receptor modulator-10 can reverse the memory impairment induced by Scopolamine (HY-N0296) and enhance cognitive function. AMPA receptor modulator-10 can be used for the research of neurological disease, such as schizophrenia .
    AMPA receptor modulator-10
  • HY-108703A

    PXT002331 monohydrochloride

    mGluR Neurological Disease
    Foliglurax monohydrochloride (PXT002331 monohydrochloride) is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) , with an EC50 of 79 nM . Antiparkinsonian effect .
    Foliglurax monohydrochloride
  • HY-120530

    mGluR Neurological Disease
    JNJ-46281222 is an metabotropic glutamate (mGlu) 2-selective, highly potent PAM (positive allosteric modulator) with nanomolar affinity (Kd = 1.7 nM) and a high modulatory potency (pEC50 = 7.71) .
    JNJ-46281222
  • HY-110278

    mGluR Neurological Disease
    ADX71743 is a highly selective, noncompetitive and brain-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM). ADX71743 can cross the blood-brain barrier (BBB) and possesses anxiolytic activity. .
    ADX71743
  • HY-14612

    mGluR Neurological Disease
    CPPHA is potent and selective positive allosteric modulator (PAM) of the mGluR5 and mGluR1 (metabotropic glutamate receptor). CPPHA can potentiate responses of mGluR5 and mGluR1 to activation of these receptors. CPPHA is developed for the research of central nervous system disorders .
    CPPHA
  • HY-14418

    ML-128

    mGluR Neurological Disease
    VU0361737 (ML-128) is a potent, selective and CNS penetrant positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4 PAM), with EC50s of 240 nM and 110 nM for human and rat mGluR4 receptors, respectively. VU0361737 has neuroprotective effect. VU0361737 is potential for Parkinson's disease research .
    VU0361737
  • HY-122255

    mGluR Neurological Disease
    LY487379 is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 potentiates glutamate-stimulated [ 35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 can be used for schizophrenia research .
    LY487379
  • HY-178121

    iGluR Neurological Disease Inflammation/Immunology
    JNJ-78911118 is a potent, brain-penetrant, selective GluN2A antagonist (IC50 = 44 nM). JNJ-78911118 shows >200-fold selectivity against GluN1/2B, 2C and 2D receptors. JNJ-78911118 functions as a negative allosteric modulator (NAM) by insurmountably suppressing glutamate efficacy and reducing glycine potency at GluN1/2A receptors. JNJ-78911118 produces profound pharmacodynamic effects in vivo. JNJ-78911118 can be used for depression research .
    JNJ-78911118
  • HY-114403

    mGluR Neurological Disease
    VU6012962 is an orally bioavailable and CNS-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM) with an IC50 of 347 nM .
    VU6012962
  • HY-12688

    Mitochondrial Metabolism Reactive Oxygen Species (ROS) Amyloid-β Neurological Disease Inflammation/Immunology
    Succinyl phosphonate is a α-Ketoglutarate Dehydrogenase Complex (KGDHC) modulator with neuroprotective activity. Succinyl phosphonate protects this complex, reduces cellular succinyl-CoA concentration, downregulates protein succinylation levels, and inhibits the activity of the α-ketoglutarate dehydrogenase complex. Succinyl phosphonate corrects hypoxic or ethanol-induced behavioral impairments, modulates exploratory behavior and emotional stress responses, and improves hypoxia tolerance. Succinyl phosphonate reduces glutamate excitotoxicity, restores the activity of the α-ketoglutarate dehydrogenase complex, reverses the changes in glutamate dehydrogenase and glutamine synthetase activities induced by β-amyloid (Amyloid-β), modulates cognitive function, and prevents β-amyloid-induced neuronal damage. Succinyl phosphonate improves microglial senescence, alleviates neuroinflammation, reactive oxygen species (ROS) production, lipid peroxidation, and the expression of proinflammatory cytokines. Succinyl phosphonate can be used in the research of Alzheimer's disease, aging-related neuroinflammation, and Parkinson's disease .
    Succinyl phosphonate
  • HY-18162

    mGluR Neurological Disease
    JNJ-42153605 is a positive allosteric modulator of the metabotropic glutamate 2 (mGlu2) receptor with an EC50 of 17 nM.
    JNJ-42153605
  • HY-130630

    mGluR Neurological Disease
    mGluR2 modulator 1 (compound 95) is a potent and BBB-penetrated mGluR2 (metabotropic glutamate receptor-2) positive allosteric modulator, with an EC50 of 0.03 μM. mGluR2 modulator 1 can be used for psychosis research .
    mGluR2 modulator 1
  • HY-100605

    mGluR Others
    VU0483605 is a potent and brain-penetrated mGlu1 receptor positive allosteric modulator (PAM). VU0483605 shows excellent mGlu1 PAM activity at both human and rat, with EC50 values of 390 and 356 nM, respectively .
    VU0483605
  • HY-107508

    mGluR Neurological Disease
    VU-29 is a positive allosteric modulator of metabotropic glutamate 5 (mGlu5) receptor (EC50=9 nM and Ki=244 nM for rmGluR5). VU-29 is selective for mGluR5 relative to other mGluR subtypes (EC50: rmGluR1/rmGluR2=557 nM/1.5 μM; hmGluR4=154 nM) .
    VU-29
  • HY-110152

    mGluR Neurological Disease
    LSN2463359 is positive allosteric modulator of metabotropic glutamate 5 (mGlu5). LSN2463359 attenuates aspects of the behavioral response to administration of the competitive NMDA receptor antagonist. LSN2463359 selectively attenuates reversal learning deficits observed in the neurodevelopmental MAM E17 model . LSN2463359 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    LSN2463359
  • HY-119078

    mGluR Neurological Disease
    VU0080241 is a positive allosteric modulator (PAM) of the metabotropic glutamate receptor subtype 4 (mGluR4), with an EC50 of 4.6 μM .
    VU0080241
  • HY-108703

    PXT002331

    mGluR Neurological Disease
    Foliglurax (PXT002331) is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 79 nM . Antiparkinsonian effect .
    Foliglurax
  • HY-103572

    mGluR Neurological Disease
    MNI137 is a potent and selective negative allosteric modulator for group II mGluRs. MNI137 has IC50s values of 8.3 and 12.6 nM for human and rat mGlu2 inhibition of glutamate-induced calcium mobilization .
    MNI137
  • HY-103574

    ADX-10059 hydrochloride

    mGluR Neurological Disease
    Raseglurant hydrochloride is a negative allosteric modulator of mGluR5. Raseglurant hydrochloride can be used in study migraine .
    Raseglurant hydrochloride
  • HY-107506

    mGluR Neurological Disease
    Ro 67-4853 is a positive allosteric modulator (PAM) of mGluR1 (pEC50=7.16 for rmGlu1a receptor). Ro67-4853 exhibits activity at all group I mGlu receptors including hmGlu1, rmGlu1, and rmGlu5. Ro 67-4853 enhances the potency of L-Glu by interacting with the transmembrane domain (TMD) of the receptor. Ro 67-4853 potentiates sensory synaptic responses to repetitive vibrissa stimulation .
    Ro 67-4853
  • HY-70057S1

    FCE 26743-d4-1; EMD 1195686-d4-1

    Isotope-Labeled Compounds Monoamine Oxidase Neurological Disease
    Safinamide-d4-1 is deuterium labeled Safinamide. Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 μM) over MAO-A (IC50=580 μM) . Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8?μM) than at resting (IC50=262?μM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al .
    Safinamide-d4-1
  • HY-122487A

    BHV-4157 hydrochloride

    mGluR Neurological Disease
    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) .
    Troriluzole hydrochloride
  • HY-W565924

    mGluR ERK Neurological Disease
    STX107 is a metabotropic glutamate 5 (mGlu5) receptor negative allosteric modulator (NAM) with a pKi of 8.32. STX107 inhibits glutamate-induced Ca 2+ mobilization, IP1 accumulation, and ERK1/2 phosphorylation. STX107 also inhibits glutamate-induced mGlu5 internalization .
    STX107
  • HY-16951

    mGluR Neurological Disease
    VU-1545 is a metabotropic glutamate receptor 5 positive allosteric modulator (mGluR5 PAM) with a Ki of 156 nM and an EC50 of 9.6 nM .
    VU-1545
  • HY-103561

    mGluR Neurological Disease
    DCB (3,3′-dichlorobenzaldazine) is an neutral allosteric modulator of themetabotropic glutamate receptor metabotropic glutamate receptor subtype 5 (mGluR5) . DCB blocks the positive allosteric regulation of mGluRs (mGluR5) with the help of 3,3′-difluorobenzaldazine (DFB). DCB shows the negative modulatory effect of 3,3′-dimethoxybenzaldazine (DMeOB) .
    DCB
  • HY-110191

    mGluR Neurological Disease Cancer
    VU0469650 is a potent, selective and brain-penetrant negative allosteric modulator of mGlu1 receptor, with an IC50 of 99 nM .
    VU0469650
  • HY-116855

    mGluR Neurological Disease
    TASP0433864 is a selective positive allosteric modulator (PAM) of metabotropic glutamate 2 (mGlu2) receptor with EC50 values of 199 nM and 206 nM against human and rat mGlu2 receptors, respectively. TASP0433864 has antipsychotic activity .
    TASP0433864
  • HY-115483

    mGluR Neurological Disease
    VU0477573 is a brain-penetrant partial negative allosteric modulator of metabotropic glutamate receptor subtype 5 (mGluR5). VU0477573 exhibits neuroprotective and anxiolytic effects. VU0477573 can be used for the research of neurological disease, such as Parkinson disease .
    VU0477573
  • HY-175296

    EAAT Neurological Disease
    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) .
    EAAT2 activator 2
  • HY-114576

    Nooglutyl; ONK-10

    iGluR Dopamine Receptor Neurological Disease
    Nooglutil (Nooglutyl; ONK-10) is a positive modulator of AMPA-type glutamate receptors (AMPARs). Nooglutil also regulates dopamine D2 receptor function to exert anxiolytic effects. Nooglutil is promising for research of neurodegenerative disorders (e.g., Alzheimer’s disease) .
    Nooglutil
  • HY-120641

    mGluR Neurological Disease
    BMS-955829 is an orally active and selective mGluR5 positive allosteric modulator with an EC50 of 2.6 nM. BMS-955829 has no intrinsic agonist activity and a low glutamate fold shift (2.4). BMS-955829 can effectively improve cognitive and executive function deficits in rodents. BMS-955829 can be used in the research of cognitive impairment diseases such as schizophrenia .
    BMS-955829

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