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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
34 Results for "
GluN1
" in MedChemExpress (MCE) Product Catalog:
Products (34)
34 Results for "GluN1" in MCE Product Catalog:
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1 Cited Publications
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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] .
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1 Cited Publications
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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] .
Cat. No.: HY-P5912
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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] .
Cat. No.: HY-172997
CAS No.: 1147526-22-4
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GluN1/3A-IN-1 (Compound GM-10) is a GluN1/GluN3A NMDA receptor inhibitor. GluN1/3A-IN-1 exhibits potent inhibitory activity against GluN1/GluN3A (IC50: 0.98 µM). GluN1/3A-IN-1 exerts its inhibitory effect by targeting the pre-M1 region and forming hydrogen bond interactions with key residues. GluN1/3A-IN-1 can be used to study GluN1/GluN3A-related neurological diseases [1].
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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].
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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] .
Cat. No.: HY-P5911
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Cat. No.: HY-175442
CAS No.: 887220-24-8
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GluN1/3A-IN-2 (Compound DD-1) is a selective GluN1/GluN3A NMDA receptor inhibitor with an IC50 of 1.26 μM for GluN1/GluN3A NMDA receptor. GluN1/3A-IN-2 can be used for neurological and psychiatric disorders research [1].
Cat. No.: HY-178121
CAS No.: 3106013-91-3
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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 [1].
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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].
Cat. No.: HY-P991611
CAS No.: 3058434-76-4
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Cat. No.: HY-112095
CAS No.: 627525-33-1
Synonyms: ENS-101 free base
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EVT-101 free base is a GluN2B antagonist. EVT-101 free base binds at the same GluN1/GluN2B dimer interface as Ifenprodil (HY-12882). EVT-101 free base inhibits calcium influx in chicken-derived cells, with an EC50 of 22 nM. EVT-101 can be used in the research of brain disorders [1] .
Cat. No.: HY-W115558
CAS No.: 17436-02-1
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L-Serine-O-sulfate potassium is a serine racemase (Srr) inhibitor. L-Serine-O-sulfate potassium attenuates the chronic constriction injury (CCI)-induced increases in NO levels, nNOS phosphorylation at Ser847, PKC-dependent GluN1 phosphorylation at Ser896, and the development of mechanical allodynia in mice. L-Serine-O-sulfate potassium can be used for the research of peripheral neuropathy [1].
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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].
Cat. No.: HY-179108
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NMDAR modulator 1 (Compound 12) is a positive, allosteric GluN1/GluN2B receptor modulator. NMDAR modulator 1 enhances NMDAR current. NMDAR modulator 1 can be used in the research of psychiatric disorders [1].
Cat. No.: HY-129517
CAS No.: 773109-55-0
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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].
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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] .
Cat. No.: HY-169951
CAS No.: 2577196-14-4
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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].
Cat. No.: HY-120523
CAS No.: 1333213-35-6
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UBP646 is a potent GluN1/GluN2D receptors potentiator, and also potentiates the other three subtypes, GluN1/GluN2A, GluN1/GluN2B, and GluN1/GluN2C receptors [1].
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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
