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Results for "

GluN1

" in MedChemExpress (MCE) Product Catalog:

23

Inhibitors & Agonists

2

Peptides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P5911
    GluN1(359-378)

    		iGluR Inflammation/Immunology
    GluN1 (359-378) is an anti-N-methyl-D-aspartate receptor (NMDAR) peptide. GluN1 (359-378) can cross the blood-brain barrier. GluN1 (359-378) can be used to study anti-NMDAR encephalitis therapy targeting the immune system [1].
    GluN1(359-378)
  • HY-P5912
    GluN1(356-385)

    		iGluR Neurological Disease
    GluN1 (356-385) is an antigenic peptide against N-methyl-D-aspartate receptor (NMDAR) encephalitis. GluN1 (356-385) has the effect of reducing the density of surface NMDAR clusters in hippocampal neurons. GluN1 (356-385) can be used to study the pathogenesis of anti-NMDAR encephalitis [1].
    GluN1(356-385)
  • HY-13457
    TCN 201
    1 Publications Verification

    		 iGluR Neurological Disease
    TCN 201 is a potent, selective and non-competitive antagonist of GluN1/GluN2A NMDA receptor, with a pIC50 of 6.8. TCN 201 is selective for GluN1/GluN2A NMDA receptor over GluN1/GluN2B NMDA receptor (pIC50<4.3) [1] .
    TCN 201
  • HY-100839
    (RS)-(Tetrazol-5-yl)glycine

    D,L-(tetrazol-5-yl)glycine; LY 285265

    		 iGluR Neurological Disease
    (RS)-(Tetrazol-5-yl)glycine (D,L-(tetrazol-5-yl)glycine) is a highly potent and selective N-methyl-D-aspartate (NMDA) receptor agonist [1]. (RS)-(Tetrazol-5-yl)glycine has EC50s of 99 nM, 1.7 μM for GluN1/GluN2D and GluN1/GluN2A, respectively . (RS)-(Tetrazol-5-yl)glycine induces seizure responses and Fos in mice .
    (RS)-(Tetrazol-5-yl)glycine
  • HY-107701
    CGP 78608 hydrochloride

    		iGluR Neurological Disease
    CGP 78608 hydrochloride is a highly potent and selective antagonist at the glycine-binding site of the NMDA receptor, with an IC50 of 6 nM. CGP 78608 hydrochloride acts as a potentiator of GluN1/GluN3A-mediated glycine currents, with an estimated EC50 in the low nM range (26.3 nM). Anticonvulsant activity [1] .
    CGP 78608 hydrochloride
  • HY-129527
    GNE-9278

    		iGluR Neurological Disease
    GNE-9278 is a highly selective positive allosteric modulator of NMDAR that acts at the GluN1 transmembrane domain (TMD). GNE-9278 acts on activated NMDARs to increase peak current and agonist affinity [1].
    GNE-9278
  • HY-120523
    UBP646

    		iGluR Neurological Disease
    UBP646 is a potent GluN1/GluN2D receptors potentiator, and also potentiates the other three subtypes, GluN1/GluN2A, GluN1/GluN2B, and GluN1/GluN2C receptors [1].
    UBP646
  • HY-172213
    (3S,6R)-NML

    		iGluR Neurological Disease
    (3S,6R)-NML is a NMDA receptor antagonist, with pIC50s of 4.8 (GluN1-GluN2A), 4.6 (GluN1-GluN2B), 5.0 (GluN1-GluN2C), 5.0 (GluN1-GluN2D) respectively. (3S,6R)-NML can be used for depression research [1].
    (3S,6R)-NML
  • HY-107701A
    CGP-78608

    		iGluR Neurological Disease
    CGP 78608 is a highly potent and selective antagonist at the glycine-binding site of the NMDA receptor, with an IC50 of 6 nM. CGP 78608 acts as a potentiator of GluN1/GluN3A-mediated glycine currents, with an estimated EC50 in the low nM range (26.3 nM). CGP 78608 has anticonvulsant activities [1] .
    CGP-78608
  • HY-148611
    NSC339614 potassium

    		iGluR Neurological Disease
    NSC339614 potassium is a selective GluN1/GluN2C and GluN1/GluN2D receptor enhancer with the activity of enhancing neuronal responses to specific NMDA receptors. NSC339614 potassium can selectively enhance the signaling of GluN1/GluN2C and GluN1/GluN2D receptors without affecting other NMDA receptors. The mechanism of action of NSC339614 potassium does not compete with agonists of L-glutamate or glycine, nor does it depend on membrane potential. The activity of NSC339614 potassium depends on the specific structure of the agonist ligand binding domain, showing its potential as a novel pharmacological agent for studying the function of NMDA receptor subtypes and providing new lead compounds for a variety of neurological diseases [1].
    NSC339614 potassium
  • HY-101178
    L-689560

    		iGluR Neurological Disease
    L-689560 is a potent N-methyl-D-aspartate (NMDA) receptor antagonist at the GluN1 glycine binding site. L-689560 is widely used as a radiolabeled ligand in binding studies and used for study the roles of NMDA receptors in normal neurological processes as well as in diseases [1] .
    L-689560
  • HY-117734
    PYD-106

    		iGluR Neurological Disease
    PYD-106 is a stereoselective pyrrolidinone (PYD) positive allosteric modulator for GluN2C-containing NMDA receptors. PYD-106 increases opening frequency and open time of single channel currents activated by maximally effective concentrations of agonist but only has modest effects on glutamate and glycine EC50. PYD-106 selectively enhances the responses of diheteromeric GluN1/GluN2C receptors but not triheteromeric GluN1/GluN2A/GluN2C receptors [1].
    PYD-106
  • HY-169950
    NMDA agonist 1

    		iGluR Neurological Disease
    NMDA agonist 1 (compound 42d) is a potent NMDA agonist with a Ki value of 96 nM. NMDA agonist 1 acts as a partial agonist of the GluN1/GluN2B complex with an EC50 value of 78 nM [1].
    NMDA agonist 1
  • HY-15703
    QNZ46
    1 Publications Verification

    		 iGluR Neurological Disease
    QNZ46 is a highly selective noncompetitive NMDA receptor antagonist targeting GluN2C/D (IC50=3.9 μM), GluN1/GluN2C (IC50=7.1 μM), and GluN1/GluN2D (IC50=182 μM) subunits. QNZ46 inhibits glutamate-mediated calcium influx, thereby blocking excitotoxicity. QNZ46 is membrane permeable and can cross the blood-brain barrier, where it inhibits myelin damage and axonal degeneration [1] .
    QNZ46
  • HY-129517
    UBP714

    		iGluR Neurological Disease
    UBP714 exhibts agonistic activity for recombinant GluN1/GluN2 receptor by binding to the positive allosteric site (PAM) of NMDARs. UBP714 enhances NMDAR-mediated field excitatory postsynaptic potentials (f-EPSPs) in Xenopus oocytes [1].
    UBP714
  • HY-172121
    NMDA agonist 2

    		iGluR Neurological Disease
    NMDA agonist 2 (compound 8d) is a potent inhibitor of NMDA receptor, with the EC50 of 0.034 μM for GluN1/2C. NMDA agonist 2 plays an important role in neurological and psychiatric disorders [1].
    NMDA agonist 2
  • HY-107712
    TCN 213

    		iGluR Neurological Disease
    TCN 213 is a selective, surmountable, glycine-dependentlly GluN1/GluN2A NMDAR antagonist with IC50s of 0.55, 3.5, 40 μM in the presence of 75, 750, 7500 nM glycine, respectively. TCN 213 can be used to monitor, pharmacologically, the switch in NMDAR expression in developing cortical neurones [1] .
    TCN 213
  • HY-169951
    Lu AF90103

    		iGluR Neurological Disease
    Lu AF90103 (Compound 42e) is a methyl ester prodrug of compound 42d capable of penetrating the blood-brain barrier. Compound 42d acts as a partial agonist of the GluN1/GluN2B complex, exhibiting 24% efficacy, and has an EC50 value of 78 nM. Lu AF90103 plays an important role in neuropsychiatric diseases research [1].
    Lu AF90103
  • HY-172884
    MDAR-IN-1

    		Cholinesterase (ChE) iGluR Neurological Disease
    MDAR IN-1 (Compound 5m) is a brain-penetrant inhibitor of acetylcholinesterase (AChE) and antagonist of the GluN1/GluN2B subtype of NMDAR receptor. MDAR IN-1 effectively inhibits AChE activity, enhances cholinergic neurotransmission, and blocks NMDAR, reducing excitatory neurotoxicity. MDAR IN-1 is promising for research of Alzheimer's disease [1].
    MDAR-IN-1
  • HY-170898
    Antidepressant agent 8

    		iGluR Neurological Disease
    Antidepressant agent 8 (Compound 1f) is a selective antagonist for the NMDA receptor GluN1/2A with an IC50 of 2.94 μmol/L. Antidepressant agent 8 exhibits antidepressant-like effects in Hydrocortisone (HY-N0583)-induced zebrafish depression model. Antidepressant agent 8 can cross blood-brain barrier [1].
    Antidepressant agent 8
  • HY-124569
    NAB-14

    		iGluR Neurological Disease
    NAB-14 is a potent, selective, orally active and non-competitive GluN2C/2D antagonists with an IC50 of 580 nM for GluN1/GluN2D. NAB-14 shows >800-fold selective for recombinant GluN2C and GluN2D over GluN2A and GluN2B. NAB-14 can cross the blood-brain-barrier [1].
    NAB-14
  • HY-155735
    AChE/Aβ-IN-2

    		iGluR Cholinesterase (ChE) Amyloid-β Neurological Disease
    AChE/Aβ-IN-2 (compound 33) is a potent and orally active inhibitor of acetylcholinesterase (AChE) with IC50 of 135 nM, as well as an antagonist of NMDA receptor (GluN1-1b/GluN2B subunit combination) with IC50 of 5.054 μM. AChE/Aβ-IN-2 also inhibits Aβ aggregation and shows good blood-brain barrier permeability. AChE/Aβ-IN-2 improves cognitive and spatial memory impairment in rats model [1].
    AChE/Aβ-IN-2
  • HY-155733
    AChE/Aβ-IN-1

    		iGluR Cholinesterase (ChE) Amyloid-β Neurological Disease
    AChE/Aβ-IN-1 (compound 32) is a potent and orally active inhibitor of acetylcholinesterase (AChE) with an IC50 of 86 nM, as well as an antagonist of NMDA receptor (GluN1-1b/GluN2B subunit combination) with IC50 of 3.876 μM. AChE/Aβ-IN-1 also inhibits Aβ aggregation and shows good blood-brain barrier permeability and neuroprotection. AChE/Aβ-IN-1 improves cognitive and spatial memory impairment in rats model [1].
    AChE/Aβ-IN-1

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