Search Result
Results for "
potentiation
" in MedChemExpress (MCE) Product Catalog:
6
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-101165
-
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iGluR
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Neurological Disease
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Cyclothiazide, a positive allosteric modulator of AMPA receptors, is used frequently to block the desensitization of both native and heterologously expressed AMPA receptors. Cyclothiazide is known to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current .
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- HY-N0403
-
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Apoptosis
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Inflammation/Immunology
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2,3,4',5-Tetrahydroxystilbene 2-O-β-D-glucoside (TSG) is an active product that can be extracted from Polygonum multiflorum Thunb. TSG has anti-inflammatory, antioxidative, anti-atherosclerotic, anti-apoptotic, and free radical scavenging activities, TSG is also indicated to facilitate long-term potentiation and learning and memory in both normal and pathological conditions .
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- HY-13058B
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mGluR
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Neurological Disease
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(R)-ADX-47273 is a potent mGluR5 positive allosteric modulator, with an EC50 of 168 nM for potentiation .
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- HY-103570
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mGluR
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Neurological Disease
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MCPG is a carboxylic phenyl glycine. MCPG can block metabotropic glutamate receptor (mGluR)(HY-15129) and has antagonistic activity of mGluR subtype. MCPG can be used to study the induction and maintenance of long-term potentiation (LTP) .
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- HY-101165R
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iGluR
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Neurological Disease
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Cyclothiazide (Standard) is the analytical standard of Cyclothiazide. This product is intended for research and analytical applications. Cyclothiazide, a positive allosteric modulator of AMPA receptors, is used frequently to block the desensitization of both native and heterologously expressed AMPA receptors. Cyclothiazide is known to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current .
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- HY-116143
-
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MAGL
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Metabolic Disease
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SAR127303 is an orally active, selective, competitive monoacylglycerol lipase (MAGL) covalent inhibitor with IC50s of 3.8 nM and 29 nM for mouse and human MAGL, respectively. SAR127303 potently elevates hippocampal levels of 2-AG in mice. SAR127303 decreased long term potentiation (LTP) of CA1 synaptic transmission and acetylcholine release in the hippocampus. SAR127303 produces antinociceptive effects in assays of inflammatory and visceral pain. SAR127303 slows down epileptogenesis .
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- HY-103495
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- HY-145440
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Bacterial
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Infection
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Colistin adjuvant-2 is a colistin adjuvant, shows increased colistin potentiation activity against Gram-negative bacteria .
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- HY-160931
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iGluR
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Neurological Disease
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NMDA receptor modulator 8 (Compound 3-6) is a modulator for NMDA receptor, with 50%-100% potentiation of NMDA receptor at 10 μM .
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- HY-120386
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iGluR
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Neurological Disease
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LY382884 is a selective antagonist for GluR5 kainate receptor. LY382884 prevents the induction of NMDA receptor independent long-term potentiation (LTP) .
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- HY-116561
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Others
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Neurological Disease
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Adamantylmethamphetamine hydrochloride is a psychotic compound, possessing a central action. Adamantylmethamphetamine hydrochloride has effects on hexobarbital sleeping time, spontaneous motor activity, and the potentiation of metrazole and antifatigue activity .
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- HY-123782
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Neprilysin
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Metabolic Disease
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(Rac)-UK-414495 (example 7) is a potent neutral endopeptidase (NEP) inhibitor. (Rac)-UK-414495 causes potentiation of cAMP in the sexual genitalia of the female .
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- HY-107683
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nAChR
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Neurological Disease
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LY-2087101 is an allosteric potentiator of α7 nAChRs. LY-2087101 causes potentiation of agonist-evoked α7 responses by binding within the nAChR transmembrane region .
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- HY-145439
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Bacterial
NF-κB
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Infection
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Colistin adjuvant-1 is a colistin adjuvant, shows increased colistin potentiation activity against Gram-negative bacteria. Colistin adjuvant-1 inhibits NF-κB with an IC50 of 0.209 μM .
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- HY-I0096
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Endogenous Metabolite
iGluR
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Neurological Disease
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Indole-2-carboxylic acid is a strong inhibitor of lipid peroxidation. Indole-2-carboxylic acid (I2CA) specifically and competitively inhibits the potentiation by glycine of NMDA-gated current .
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- HY-111129
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Adenosine Receptor
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Neurological Disease
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CP-66713 is a selective adenosine A2 receptor antagonist, with Ki of 22 nM. CP-66713 inhibits induction of long-term potentiation of evoked synaptic potentials. CP-66713 can be used in the study of neurological diseases .
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- HY-13058
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mGluR
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Neurological Disease
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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 .
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- HY-100372
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(RS)-ECPG
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mGluR
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Neurological Disease
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E4CPG ((RS)-ECPG) is a Group I/Group II metabotropic glutamate receptor (mGluR) antagonist. E4CPG can inhibit the paired-pulse ratio of monosynaptic inhibitory postsynaptic currents (IPSC) potentiation .
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- HY-103409
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Dopamine Receptor
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Neurological Disease
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ABT-724 trihydrochloride is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM), and has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile .
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- HY-14330
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Dopamine Receptor
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Neurological Disease
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ABT-724 is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM). ABT-724 has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 could be useful for the treatment of erectile dysfunction and has favorable side-effect profile .
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- HY-Y0378
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(R)-Leucine
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Endogenous Metabolite
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Neurological Disease
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D-Leucine is a more potent anti-seizure agent than L-leucine. D-leucine potently terminates seizures even after the onset of seizure activity. D-leucine, but not L-leucine, reduces long-term potentiation but had no effect on basal synaptic transmission in vitro .
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- HY-P10235
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Amylin Receptor
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Neurological Disease
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Cyclic AC253 is an antagonist for amylin receptor, with IC50 of 0.3 μM. Cyclic AC253 exhibits neuroprotective efficacy against Aβ toxicity and abrogates Aβ-induced impairment of hippocampal long-term potentiation. Cyclic AC253 penetrate blood-brain barrier (BBB) .
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- HY-101037
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N-Methylglycine; Sarcosin
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Endogenous Metabolite
GlyT
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Cancer
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Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia .
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- HY-N7119
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Others
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Inflammation/Immunology
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Cimicifugoside, a triterpenoid isolated from Cimicifuga simplex, is a novel specific nucleoside transport inhibitor that displays synergistic potentiation of methotrexate cytotoxicity . Cimicifugoside shows immunosuppressive activity, which is preferentially directed toward B-cell function with larger doses being required for suppression of T-cell function .
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- HY-13017S
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VX-770-d9
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CFTR
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Cancer
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Ivacaftor-d9 is a potent CFTR modulator and exhibits an EC50 value of 255 nM for CFTR potentiation in G551D/F508del HBE Cells. Ivacaftor-D9 acts as an orally active and improved deuterated Ivacaftor analog for cystic fibrosis research[1].
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- HY-13017S1
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VX-770-d19
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CFTR
Autophagy
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Endocrinology
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Ivacaftor-d9 is a potent CFTR modulator and exhibits an EC50 value of 255 nM for CFTR potentiation in G551D/F508del HBE Cells. Ivacaftor-D9 acts as an orally active and improved deuterated Ivacaftor analog for cystic fibrosis research .
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- HY-Y0378S
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(R)-Leucine-d10
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Isotope-Labeled Compounds
Endogenous Metabolite
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Neurological Disease
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D-Leucine-d10 is the deuterium labeled D-Leucine. D-Leucine is a more potent anti-seizure agent than L-leucine. D-leucine potently terminates seizures even after the onset of seizure activity. D-leucine, but not L-leucine, reduces long-term potentiation but had no effect on basal synaptic transmission in vitro[1].
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- HY-I0096S
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- HY-101037S1
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N-Methylglycine-d3; Sarcosin-d3
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Isotope-Labeled Compounds
Endogenous Metabolite
GlyT
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Cancer
|
Sarcosine-d3 is the deuterium labeled Sarcosine. Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia[1][2].
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- HY-109008
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OP0595 free acid
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Beta-lactamase
Bacterial
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Infection
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Nacubactam (OP0595 free acid) is a potent non-β-lactam-β-lactamase inhibitor with activity against class A and class C β-lactamases. Nacubactam (OP0595 free acid) acts as a penicillin binding protein (PBP) 2-active antibacterial, and gives β-lactamase-independent potentiation of β-lactams targeting other PBPs .
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- HY-148250
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iGluR
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Neurological Disease
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TP-050 is a potent, orally active and selective NMDAR agonist with an EC50 value of 0.51 µM and 9.6 µM for GluN2A and GluN2D, respecticely. TP-050 can cross the blood-brain barrier (BBB). TP-050 induces hippocampal long-term (LPT) potentiation enhancemen and enhances neuronal signal transmission .
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- HY-Y0378R
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Endogenous Metabolite
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Neurological Disease
|
D-Leucine (Standard) is the analytical standard of D-Leucine. This product is intended for research and analytical applications. D-Leucine is a more potent anti-seizure agent than L-leucine. D-leucine potently terminates seizures even after the onset of seizure activity. D-leucine, but not L-leucine, reduces long-term potentiation but had no effect on basal synaptic transmission in vitro .
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- HY-101037R
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Endogenous Metabolite
GlyT
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Cancer
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Sarcosine (Standard) is the analytical standard of Sarcosine. This product is intended for research and analytical applications. Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia .
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- HY-101037S
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N-Methylglycine-15N; Sarcosin-15N
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Endogenous Metabolite
GlyT
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Cancer
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Sarcosine- 15N is the 15N-labeled Sarcosine. Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia[1][2].
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- HY-120645
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Opioid Receptor
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Neurological Disease
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BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (µ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [ 35S]GTPγS binding in mouse brain membranes .
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- HY-155687
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Phosphodiesterase (PDE)
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Neurological Disease
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PDE5-IN-10 (compound 4b) is a potent PDE5 inhibitor with an IC50 of 20 nM. PDE5-IN-10 improves in vitro microsomal stability (t1/2 = 44.6 min) as well as excellent efficacy in restoring long-term potentiation. PDE5-IN-10 can be used for Alzheimer’s disease (AD) research .
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- HY-130553
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β-NAAG; β-N-Acetylaspartylglutamic acid
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Aminopeptidase
mGluR
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Neurological Disease
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β-Spaglumic acid (β-NAAG) is a competitive NAAG peptidase inhibitor (Ki=1 µM) that protects spinal cord neurons from excitotoxicity and hypoxic damage. β-Spaglumic acid is also a selective mGluR3 antagonist (mGluR3 receptor functions to regulate activity-dependent synaptic potentiation in the hippocampus). β-Spaglumic acid can be used in neuroprotection-related studies .
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- HY-N2922
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Amyloid-β
NF-κB
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Neurological Disease
Inflammation/Immunology
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β-Amyrin shows effectively counteract amyloid β (Aβ)-induced impairment of long-term potentiation (LTP). β-Amyrin is a promising candidate for Alzheimer's disease (AD) research. β-Amyrin exhibits anti-inflammatory effects, protective activity against pulmonary fibrosis, and notable antibacterial capabilities. β-Amyrin is an orally active natural triterpenoid compound .
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- HY-N2922R
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Amyloid-β
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Neurological Disease
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β-Amyrin shows effectively counteract amyloid β (Aβ)-induced impairment of long-term potentiation (LTP). β-Amyrin is a promising candidate for Alzheimer's disease (AD) research. β-Amyrin exhibits anti-inflammatory effects, protective activity against pulmonary fibrosis, and notable antibacterial capabilities. β-Amyrin is an orally active natural triterpenoid compound .
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- HY-19411
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nAChR
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Neurological Disease
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SSR180711 hydrochloride is an orally active, selective and reversible α7 acetylcholine nicotinic receptor (n-AChRs) partial agonist. SSR180711 hydrochloride can act on rat α7 n-AChR (Ki=22 nM; IC50=30 nM) and human α7 n-AChR (Ki=14 nM; IC50=18 nM). SSR180711 hydrochloride increases glutamatergic neurotransmission, ACh release and long-term potentiation (LTP) in the hippocampus .
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- HY-121299
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mCPBG
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5-HT Receptor
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Neurological Disease
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m-Chlorophenylbiguanide (mCPBG) is a potent high-affinity agonist of the 5-HT3 receptor, exhibiting an inhibitory effect on long-term potentiation (LTP) in the mossy fiber-CA3 system. mCPBG attenuates the magnitude of LTP at concentrations of 0.3-1 microM, demonstrating its role in modulating synaptic plasticity. Additionally, the impact of mCPBG on LTP is reversible by the GABAA receptor antagonist bicuculline, indicating a connection between its action and GABAergic neurotransmission.
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- HY-100617A
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(RS)-4-Carboxyphenylglycine
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mGluR
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Others
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(RS)-4CPG ((RS)-4-Carboxyphenylglycine) is a type I metabotropic glutamate receptor antagonist with activity in blocking LTP induction. In mice lacking IP3R1, (RS)-4CPG (500μM) nearly blocked long-term potentiation (LTP) induced by type I metabotropic glutamate receptor activation, with LTP of 117.6±1.7% (n = 8) in IP3R1(-/-) mice and 116.9±1.8% (n = 5) in IP3R1(+/+) mice.
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- HY-107601
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ACET
|
iGluR
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Neurological Disease
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UBP316 (ACET) is a highly potent and selective kainate receptor GluK1 (GluR5) antagonist, with a Kb value of 1.4 nM. UBP316 is effective at blocking the depression of both field excitatory postsynaptic potentials (fEPSPs) and monosynaptically-evoked GABAergic transmission induced by ATPA, a GluK1 selective agonist .
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- HY-156104
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PROTACs
CaMK
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Neurological Disease
|
CaMKIIα-PHOTAC is a photochemically targeted chimera (PHOTAC) targeting Ca2+/calmodulin-dependent protein kinase II α (CaMKIIα). Molecules such as PHOTAC can catalyze the ubiquitination and degradation of target proteins through the endogenous proteasome under specific wavelengths of light. CaMKIIα-PHOTAC reduces synaptic function under light conditions, and it attenuates the intensity of evoked field excitatory postsynaptic potentials in the mouse hippocampus in response to physiological stimuli. CaMKIIα-PHOTAC plays a critical role in maintaining long-term potentiation and memory capacity in subcellular dendritic domains .
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- HY-16728A
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GLYX-13 acetate
|
iGluR
|
Neurological Disease
|
Rapastinel acetate (GLYX-13 acetate) is an N-methyl-D-aspartate (NMDA) receptor modulator with long-acting antidepressant activity. Rapastinel acetate exerts its antidepressant effects by enhancing long-term potentiation (LTP) of synaptic transmission. Rapastinel acetate transiently enhances NMDAR-mediated currents in pyramidal neurons in the hippocampus and medial prefrontal cortex by binding to unique sites on the NMDAR complex. Rapastinel acetate significantly enhanced NMDAR-mediated currents at a concentration of 1 μmol/l and significantly reduced the currents at a concentration of 10 μmol/l. The mechanism of action of Rapastinel acetate is related to the reduction of affinity to intracellular calcium inactivation sites, which provides a theoretical basis for enhancing conductance mediated by NMDAR .
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- HY-116673
-
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Histone Acetyltransferase
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Neurological Disease
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TTK21 is an activator of the histone acetyltransferases CBP/p300. TTK21 passes the blood–brain barrier, induces no toxicity, and reaches different parts of the brain when conjugated to glucose-based carbon nanosphere (CSP). TTK21 has beneficial implications for the brain functions of neurogenesis and long-term memory .CSP-TTK21 can ameliorate Aβ-impaired long-term potentiation (LTP). CSP-TTK21 may enhance the transcription of genes that promote synaptic health and cognitive function . CSP-TTK21 is orally effective and leads to improvements in motor functions, histone acetylation dynamics in a spinal injury rat model .
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Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P10235
-
|
Amylin Receptor
|
Neurological Disease
|
Cyclic AC253 is an antagonist for amylin receptor, with IC50 of 0.3 μM. Cyclic AC253 exhibits neuroprotective efficacy against Aβ toxicity and abrogates Aβ-induced impairment of hippocampal long-term potentiation. Cyclic AC253 penetrate blood-brain barrier (BBB) .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-13017S
-
|
Ivacaftor-d9 is a potent CFTR modulator and exhibits an EC50 value of 255 nM for CFTR potentiation in G551D/F508del HBE Cells. Ivacaftor-D9 acts as an orally active and improved deuterated Ivacaftor analog for cystic fibrosis research[1].
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- HY-Y0378S
-
|
D-Leucine-d10 is the deuterium labeled D-Leucine. D-Leucine is a more potent anti-seizure agent than L-leucine. D-leucine potently terminates seizures even after the onset of seizure activity. D-leucine, but not L-leucine, reduces long-term potentiation but had no effect on basal synaptic transmission in vitro[1].
|
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- HY-101037S1
-
|
Sarcosine-d3 is the deuterium labeled Sarcosine. Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia[1][2].
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- HY-101037S
-
|
Sarcosine- 15N is the 15N-labeled Sarcosine. Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia[1][2].
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- HY-13017S1
-
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Ivacaftor-d9 is a potent CFTR modulator and exhibits an EC50 value of 255 nM for CFTR potentiation in G551D/F508del HBE Cells. Ivacaftor-D9 acts as an orally active and improved deuterated Ivacaftor analog for cystic fibrosis research .
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- HY-I0096S
-
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Indole-2-carboxylic acid- 13C is the 13C-labeled Indole-2-carboxylic acid. Indole-2-carboxylic acid is a strong inhibitor of lipid peroxidation. Indole-2-carboxylic acid (I2CA) specifically and competitively inhibits the potentiation by glycine of NMDA-gated current[1][2].
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