Search Result
Results for "
NR2B
" in MedChemExpress (MCE) Product Catalog:
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-107706
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PD 174494 hydrochloride
|
iGluR
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Neurological Disease
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Co 101244 (PD 174494) hydrochloride is a NR2B-containing NMDA receptor antagonist .
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- HY-121100
-
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iGluR
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Neurological Disease
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BZAD-01 is a potent, selective and orally active inhibitor of NMDA NR2B subunit, with a Ki of 72 nM. BZAD-01 can improve postural asymmetry as well as Apomorphine-induced rotation .
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- HY-136299
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FUT-187 free base
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iGluR
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Neurological Disease
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Sepimostat (FUT-187 free base) exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit. Sepimostat inhibits the Ifenprodil binding with a Ki value of 27.7?μM .
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- HY-126123
-
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iGluR
Potassium Channel
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Neurological Disease
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NR2B-selective NMDA receptor antagonist 1 (compound 29) is a potent antagonist of NR1/NR2B receptors, with IC50s of 0.05 μM, 0.73 μM, 2.4 μM to NR1/NR2B NMDA receptor, hERG, α1-AdR, respectivity. NR2B-selective NMDA receptor antagonist 1 exhibites efficient permeability across the blood–brain barrier .
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- HY-P5947
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HIV
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Neurological Disease
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Tat-HA-NR2B9 contains a fragment of the cellmembrane transduction domain of HIV-1 Tat, a influenza virus hemagglutinin (HA) epitope-tag, and the C-terminal 9 amino acids of NR2B (NR2B9c). Tat-HA-NR2B9 reduces infarct size and improves neurological functions in ischemia-induced cerebral injury in the rats
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- HY-177127
-
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iGluR
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Neurological Disease
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Satoprodil (example 2) is a potent N-methyl-D-aspartate (NMDA) receptor negative allosteric modulator with an IC50 value of 123 nM for NR2B [2].
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- HY-107698
-
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iGluR
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Neurological Disease
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PMPA (NMDA antagonist) is an NMDA receptor antagonist with Ki values of 0.84, 2.74, 3.53 and 4.16 μM for NR2A, NR2B, NR2C and NR2D, respectively .
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- HY-145585
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MIJ-821
|
iGluR
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Neurological Disease
|
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Onfasprodil is negative allosteric modulator of NR2B. Onfasprodil in combination with GABA receptor regulator has the potential for the research of Alzheimer's disease (extracted from patent CN111481543A) .
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- HY-136299A
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FUT-187
|
iGluR
|
Neurological Disease
|
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Sepimostat dimethanesulfonate (FUT-187) exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit. Sepimostat dimethanesulfonate inhibits the Ifenprodil binding with a Ki value of 27.7 µM .
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- HY-136659
-
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iGluR
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Others
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Ro 04-5595 is a selective antagonist with specific activity against the NR2B subunit of the NMDA receptor. Ro 04-5595 exhibits favorable pharmacokinetic properties in in vitro and in vivo studies, with rapid uptake and clearance. Ro 04-5595 exhibits strong binding in NR2B receptor-enriched regions and low binding in the cerebellum. Ro 04-5595 is able to effectively inhibit specific binding, showing high affinity for the NR2B receptor and a clear ranking of binding affinity with a variety of other compounds .
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- HY-137049
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PD 174494
|
iGluR
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Others
|
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Co-101244 (PD 174494) is an NMDA receptor blocker that specifically targets the NR2B subunit.
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- HY-12962
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iGluR
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Neurological Disease
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NMDA-IN-1 is a potent and NR2B-selective NMDA antagonist with Ki of 0.85 nM; NR2B Ca2+ influx IC50 is 9.7 nM; no activities on NR2A, NR2C, NR2D, hERG-channel and α1-adrenergic receptor.
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- HY-111500A
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- HY-136299R
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iGluR
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Neurological Disease
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Sepimostat (Standard) is the analytical standard of Sepimostat. This product is intended for research and analytical applications. Sepimostat (FUT-187 free base) exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit. Sepimostat inhibits the Ifenprodil binding with a Ki value of 27.7 μM .
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- HY-P0117
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|
Tat-NR2Bct; NA-1
|
iGluR
NO Synthase
|
Neurological Disease
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Tat-NR2B9c (Tat-NR2Bct; NA-1) is a postsynaptic density-95 (PSD-95) inhibitor, with EC50 values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC50 values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy [2] .
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- HY-P0117A
-
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Tat-NR2Bct TFA; NA-1 TFA
|
iGluR
NO Synthase
|
Neurological Disease
|
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Tat-NR2B9c TFA (Tat-NR2Bct TFA) is a postsynaptic density-95 (PSD-95) inhibitor, with EC50 values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c TFA disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC50 values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c TFA also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy .
|
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-
- HY-107716
-
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iGluR
|
Neurological Disease
|
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Ro 8-4304 hydrochloride is a potent NMDA receptor antagonist. Ro 8-4304 hydrochloride is a NR2B selective, non-competitive, voltage-independent antagonist .
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- HY-12962A
-
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iGluR
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Neurological Disease
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NMDA-IN-1 dihydrochloride is a selective NMDA NR2B antagonist with a Ki of 0.85 nM; NR2B Ca2+ influx IC50 is 9.7 nM. NMDA-IN-1 dihydrochloride inhibits Glu/Gly stimulated Ca2+ flux in Ltk- cells expressing the hNR1a/NR2B with a IC50 of 9.7 nM. NMDA-IN-1 dihydrochloride has no activities on NR2A, NR2C, NR2D, hERG-channel and α1-adrenergic receptor. NMDA-IN-1 dihydrochloride shows excellent activity in the mechanical hyperalgesia assay in rats. NMDA-IN-1 dihydrochloride can be used for the studies of stroke, parkinson, and neuropathic pain .
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- HY-111500
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iGluR
|
Neurological Disease
|
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(Rac)-NMDAR antagonist 1 is the racemate of NMDAR antagonist 1. NMDAR antagonist 1 is a potent and orally bioavailable NR2B-selective NMDAR antagonist .
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- HY-14777
-
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RGH-896
|
iGluR
|
Neurological Disease
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Radiprodil (RGH-896) is an orally active and selective NMDA NR2B antagonist. A potential therapeutic agent in treatment of neuropathic pain and possibly other chronic pain conditions .
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- HY-170410
-
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iGluR
|
Neurological Disease
|
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EMD-95885 is a selective NR2B-containing NMDA receptors antagonist with an IC50 of 3.9 nM. EMD-95885 does not interact with other sites on the NMDA receptor .
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- HY-136459
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iGluR
|
Neurological Disease
|
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NMDA receptor antagonist 2 is a potent and orally active NR2B subtype-selective NMDA antagonist with an IC50 and a Ki of 1.0 nM and 0.88 nM, respectively. NMDA receptor antagonist 2 is used for the study of neuropathic pain and Parkinson’s disease .
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- HY-12881
-
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SL-820715
|
iGluR
|
Neurological Disease
|
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Eliprodil(SL-820715) is a non-competitive NR2B-NMDA receptor antagonist(IC50=1 uM), less potent for NR2A- and NR2C-containing receptors(IC50> 100 uM).
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- HY-106408A
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Salfaprodil; Neu2000 potassium
|
iGluR
|
Neurological Disease
|
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Nelonemdaz (Salfaprodil) potassium is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA). Nelonemdaz potassium is also a free radical scavenger. Nelonemdaz potassium has excellent neuroprotection against NMDA- and free radical-induced cell death [2].
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-
- HY-116142
-
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|
iGluR
|
Neurological Disease
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CP-283097 is a conformationally restricted and NR2B subtype-selective NMDA antagonist. CP-283097 efficiently competitively inhibits the binding of [³H]CP-101,606 to the rat meninges, with an IC50 value of 18 nM. CP-283097 exhibits nearly complete inhibition of the current mediated by the NR2B receptor (IC50 = 206 nM), while the inhibitory effect on the NR2A or NR2C receptors is very weak. CP-283097 demonstrates excellent central nervous system permeability and in vivo efficacy in animal models. CP-283097 can be used for neurological diseases related to excessive activation of NMDA receptors .
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- HY-14777R
-
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|
iGluR
|
Neurological Disease
|
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Radiprodil (Standard) is the analytical standard of Radiprodil. This product is intended for research and analytical applications. Radiprodil (RGH-896) is an orally active and selective NMDA NR2B antagonist. A potential therapeutic agent in treatment of neuropathic pain and possibly other chronic pain conditions .
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- HY-106408
-
|
Salfaprodil free base; Neu2000
|
iGluR
|
Neurological Disease
|
|
Nelonemdaz (Salfaprodil free base) is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA). Nelonemdaz is also a free radical scavenger. Nelonemdaz has excellent neuroprotection against NMDA- and free radical-induced cell death [2].
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- HY-13993B
-
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iGluR
|
Neurological Disease
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Ro 25-6981 hydrochloride is a potent, selective and activity-dependent NR2B subunit specific NMDA receptor antagonist. Ro 25-6981 hydrochloride shows anticonvulsant and anti-parkinsonian activity. Ro 25-6981 hydrochloride has the potential for the research of parkinson's disease (PD) [2] .
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- HY-13993
-
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iGluR
|
Neurological Disease
|
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Ro 25-6981 is a potent, selective and activity-dependent NR2B subunit specific NMDA receptor antagonist. Ro 25-6981 shows anticonvulsant and anti-parkinsonian activity. Ro 25-6981 has the potential for the research of parkinson's disease (PD) [2] .
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- HY-13993A
-
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iGluR
|
Neurological Disease
|
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Ro 25-6981 Maleate is a potent, selective and activity-dependent NR2B subunit specific NMDA receptor antagonist. Ro 25-6981 Maleat shows anticonvulsant and anti-parkinsonian activity. Ro 25-6981 Maleate has the potential for the research of parkinson's disease (PD) [2] .
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- HY-12882AR
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NP-120 tartrate (Standard); RC-61-91 tartrate (Standard)
|
iGluR
Potassium Channel
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Neurological Disease
|
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Ifenprodil (tartrate) (Standard) is the analytical standard of Ifenprodil (tartrate). This product is intended for research and analytical applications. Ifenprodil tartrate is a typical noncompetitive NMDA receptor antagonist. Ifenprodil tartrate exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM) . Ifenprodil tartrate inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil tartrate has the potential to be a cerebral vasodilator [2].
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- HY-161211
-
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17β-HSD
iGluR
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Metabolic Disease
|
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HSD17B13-IN-7 (compound 1), a fluorophenol-containing compound, is a potent HSD17B13 inhibitor with IC50s of 0.18 μM and 0.25 μM β-estradiol and Leukotriene B4 as substrates, respectively. HSD17B13-IN-7 is a potent N-methyl-D-aspartate (NMDA) NR2B receptor antagonist. HSD17B13-IN-7 has the potential for non-alcoholic fatty liver disease research .
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- HY-P2307
-
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|
iGluR
NO Synthase
|
Neurological Disease
|
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Tat-NR2BAA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95 [2].
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- HY-P2307A
-
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iGluR
NO Synthase
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Neurological Disease
|
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Tat-NR2BAA TFA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA TFA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95 .
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- HY-117467
-
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iGluR
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Neurological Disease
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BMT-108908 is a negative allosteric modulator with selective activity on the NR2B subtype of the NMDA receptor. BMT-108908 has been shown to damage cognition in research, affecting cognitive functions in multiple areas. BMT-108908 failed to show a significant impact on the γ wave power of the EEG in the experiment, but it had a significant inhibitory and enhancement effect on the β wave and δ wave power .
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- HY-107708
-
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iGluR
Sigma Receptor
Potassium Channel
|
Neurological Disease
|
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threo Ifenprodil hemitartrate is a σ receptor agonist, with Kis of 59.1 and 2 nM for σ1 and σ2 receptors, respectively. threo Ifenprodil hemitartrate is also a NR2B subunit-selective NMDA receptor antagonist (IC50=0.22 μM). threo Ifenprodil hemitartrate is a hERG potassium channel inhibitor, with an IC 50 of 88 nM, showing antiarrhythmic activity [2] .
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- HY-105353
-
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iGluR
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Neurological Disease
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CEB-1604 is an NMDA receptor antagonist. CEB-1604 inhibits NMDA-induced currents in oocytes transfected with NMDA receptor isoforms (NR1/NR2A, NR1/NR2B, NR1/NR2C, NR1/NR2D) with IC50 values ranging from 5 to 12 μM. CEB-1604 abolishes NMDA-dependent epileptiform discharges in rat cortical wedge preparations and reduces the depolarizing effects of NMDA. CEB-1604 can be used in the research field of neurological damage diseases .
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- HY-17617
-
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Z-360
|
Cholecystokinin Receptor
Ephrin Receptor
Interleukin Related
VEGFR
HIF/HIF Prolyl-Hydroxylase
Akt
|
Neurological Disease
Cancer
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Nastorazepide (Z-360) is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide inhibits the specific binding of [ 3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide has antitumor activity against pancreatic cancer. Nastorazepide inhibits colorectal cancer liver metastasis and relieves pain [2] .
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-
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- HY-14575
-
|
Z-360 hemicalcium
|
Cholecystokinin Receptor
Ephrin Receptor
Interleukin Related
VEGFR
HIF/HIF Prolyl-Hydroxylase
Akt
|
Neurological Disease
Cancer
|
|
Nastorazepide (Z-360) hemicalcium is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide hemicalcium inhibits the specific binding of [ 3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide hemicalcium inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide hemicalcium has antitumor activity against pancreatic cancer. Nastorazepide hemicalcium inhibits colorectal cancer liver metastasis and relieves pain [2] .
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-
- HY-17617R
-
|
|
Cholecystokinin Receptor
Ephrin Receptor
Interleukin Related
VEGFR
HIF/HIF Prolyl-Hydroxylase
Akt
|
Neurological Disease
Cancer
|
|
Nastorazepide (Standard) is the analytical standard of Nastorazepide. This product is intended for research and analytical applications. Nastorazepide (Z-360) is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide inhibits the specific binding of [3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide has antitumor activity against pancreatic cancer. Nastorazepide inhibits colorectal cancer liver metastasis and relieves pain [2] .
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- HY-N1916
-
|
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Glutathione S-transferase
P-glycoprotein
Apoptosis
iGluR
CaMK
p38 MAPK
Reactive Oxygen Species (ROS)
Bacterial
|
Infection
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Coniferyl ferulate is an orally active phenolic acid compound. Coniferyl ferulate is a potent inhibitor of glutathione S-transferase (GST) (IC50 = 0.3 μM), which downregulates P-gp expression, induces apoptosis in B-MD-C1 (ADR+/+) cells, and reverses multidrug resistance. Coniferyl ferulate blocks the NMDAR/NR2B-CaMKII-MAPKs signaling pathway, inhibits ROS production and mitochondrial apoptosis, while reshapes the intestinal microbiota and microbial metabolism, ameliorates colonic inflammation and alleviates depressive symptoms in mice. Coniferyl ferulate can alleviate the toxicity of xylene to hematopoietic stem and progenitor cells by targeting Mgst2. Coniferyl ferulate exhibits antibacterial activity against the Gram-positive Bacillus subtilis and Staphylococcus aureus [2] .
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-
-
- HY-12882
-
Ifenprodil
Maximum Cited Publications
10 Publications Verification
NP-120; RC-61-91
|
iGluR
Adrenergic Receptor
Potassium Channel
Calcium Channel
Influenza Virus
|
Infection
Neurological Disease
|
|
Ifenprodil (NP-120), a cerebral vasodilator, is a noncompetitive NMDA receptor antagonist. Ifenprodil exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM) . Ifenprodil is an α1 adrenergic receptor antagonist. Ifenprodil inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil has reliable inhibitory effects against A/H1N1 strains (EC50 of 6.6 µM). Ifenprodil has neuroprotective, anticonvulsant and antinociceptive effects. Ifenprodil can be used for the study of cerebrovascular diseases and peripheral arterial obliterative disease [2] .
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-
-
- HY-12882A
-
|
NP-120 tartrate; RC-61-91 tartrate
|
iGluR
Adrenergic Receptor
Potassium Channel
Calcium Channel
Influenza Virus
|
Infection
Neurological Disease
|
|
Ifenprodil (NP-120) tartrate, a cerebral vasodilator, is a noncompetitive NMDA receptor antagonist. Ifenprodil tartrate exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM) . Ifenprodil tartrate is an α1 adrenergic receptor antagonist. Ifenprodil tartrate inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil tartrate has reliable inhibitory effects against A/H1N1 strains (EC50 of 6.6 µM). Ifenprodil tartrate has neuroprotective, anticonvulsant and antinociceptive effects. Ifenprodil tartrate can be used for the study of cerebrovascular diseases and peripheral arterial obliterative disease [2] .
|
-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P0117
-
|
Tat-NR2Bct; NA-1
|
iGluR
NO Synthase
|
Neurological Disease
|
|
Tat-NR2B9c (Tat-NR2Bct; NA-1) is a postsynaptic density-95 (PSD-95) inhibitor, with EC50 values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC50 values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy [2] .
|
-
- HY-P0117A
-
|
Tat-NR2Bct TFA; NA-1 TFA
|
iGluR
NO Synthase
|
Neurological Disease
|
|
Tat-NR2B9c TFA (Tat-NR2Bct TFA) is a postsynaptic density-95 (PSD-95) inhibitor, with EC50 values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c TFA disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC50 values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c TFA also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy .
|
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- HY-P2307
-
|
|
iGluR
NO Synthase
|
Neurological Disease
|
|
Tat-NR2BAA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95 [2].
|
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- HY-P5947
-
|
|
HIV
|
Neurological Disease
|
|
Tat-HA-NR2B9 contains a fragment of the cellmembrane transduction domain of HIV-1 Tat, a influenza virus hemagglutinin (HA) epitope-tag, and the C-terminal 9 amino acids of NR2B (NR2B9c). Tat-HA-NR2B9 reduces infarct size and improves neurological functions in ischemia-induced cerebral injury in the rats
|
-
- HY-P2307A
-
|
|
iGluR
NO Synthase
|
Neurological Disease
|
|
Tat-NR2BAA TFA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA TFA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95 .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-N1916
-
-
-
- HY-12882A
-
-
-
- HY-12882AR
-
|
NP-120 tartrate (Standard); RC-61-91 tartrate (Standard)
|
Alkaloids
Piperidine Alkaloids
Crassulaceae
Source classification
Sedum sarmentosum Bunge
Plants
|
iGluR
Potassium Channel
|
|
Ifenprodil (tartrate) (Standard) is the analytical standard of Ifenprodil (tartrate). This product is intended for research and analytical applications. Ifenprodil tartrate is a typical noncompetitive NMDA receptor antagonist. Ifenprodil tartrate exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM) . Ifenprodil tartrate inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil tartrate has the potential to be a cerebral vasodilator [2].
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