iGluR Inhibitor

Dynorphin A (1-10) (TFA), an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) (TFA) also blocks NMDA-activated current with an IC₅₀ of 42.0 μM.

LQFM215 is a proline transporter (PROT) inhibitor. LQFM215 inhibits proline transport by competitively binding to the active site of PROT. LQFM215 effectively reduces hyperlocomotion and enhances social interaction.

NP10679 is a selective, pH dependent GluN2B subunit-specific N-methyl-D-aspartate (NMDA) receptor inhibitor with high oral bioavailability and good brain penetration. NP10679 inhibits GluN2B with IC₅₀s of 23 and 142 nM at pH 6.9 and 7.6, respectively. NP10679 is a histamine H1 antagonist and a hERG channel inhibitor with IC₅₀s of 73 and 620 nM, respectively. NP10679 is a reversible inhibitor of human liver CYP enzymes.

gamma-DGG is a competitive AMPA receptor blocker.

Brophenexin (compound 8) is a potent NMDAR/TRPM4 interaction interface inhibitor. Brophenexin shows neuroprotective activity. Brophenexin prevents NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC₅₀ of 2.1 μM. Brophenexin protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss.

IEM-1460 blocks both AMPA and NMDA glutamate receptor with anticonvulsant effect in vivo.

FSC231 is a PSD‐95/DLG/ZO‐1 (PDZ) domain inhibitor of PICK1. FSC231 has analgesic effects.

Gly-Pro-Glu is a neuroactive peptide with a potent action on acetylcholine release. Gly-Pro-Glu is the N-terminal tripeptide of insulin-like growth factor-I. Gly-Pro-Glu inhibits glutamate binds to N-methyl-D-aspartate (NMDA) receptor with an IC₅₀ value of 14.7 μM. Gly-Pro-Glu can be used for the research of neuroprotection .

Decanoic acid-d₅ is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects.

IC87201, an inhibitor of PSD95-nNOS protein-protein interactions, suppresses NMDAR-dependent NO and cGMP formation.

Ganglioside GM1 (bovine) ammonium is a type of glycosphingolipid, mainly found on the cell membranes of the central nervous system of vertebrates. Ganglioside GM1 (bovine) ammonium exerts neuroprotective effects by reducing excessive activation of NMDAR, activating TrkA and ERK1/2, and inhibiting oxidative stress and cell apoptosis and autophagy. Ganglioside GM1 (bovine) ammonium can be used in the research of diseases such as traumatic brain injury, Parkinson's disease, Alzheimer's disease, and Huntington's disease.

Linalool (Standard) is the analytical standard of Linalool. This product is intended for research and analytical applications. Linalool is natural monoterpene in essential olis of coriander, acts as a competitive antagonist of Nmethyl d-aspartate (NMDA) receptor, with anti-tumor, anti-cardiotoxicity activity.Linalool is a PPARα ligand that reduces plasma TG levels and rewires the hepatic transcriptome and plasma metabolome.

TAT-GluA2 3Y is a blood-brain barrier-permeable AMPA receptor inhibitory peptide that crosses cell membranes via the HIV-1 TAT protein domain. TAT-GluA2 3Y blocks the endocytosis of AMPA receptors, including the internalization of GluA1/GluA2 subunits, by disrupting interactions with the AP2, Brag2 and Syt3-GluA2 complexes, while also inhibiting long-term depression. TAT-GluA2 3Y blocks hypoxia-mediated AMPAR internalization, alleviates A1R-induced persistent synaptic inhibition, and reduces cerebral ischemic volume, neurological deficits and spatial memory deficits. TAT-GluA2 3Y blocks the effect of NLRP3 deficiency on fear generalization, inhibits amphetamine-induced behavioral/neurochemical sensitization, weakens the unconditioned stimulus-conditioned stimulus association of morphine, and promotes the extinction of morphine CPP. TAT-GluA2 3Y can be used in studies related to fear generalization, ischemic stroke, hypoxia, drug addiction and opioid addiction.

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.

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.

Withanone is an active ingredient from the roots of Withania somnifera and a GRP75 inhibitor. Withanone has multifunctional neuroprotective effects in alleviating cognitive dysfunction. In neuron-like cells, Withanone can inhibit NMDA-induced excitotoxicity. Withanone can inhibit white adipose tissue browning by blocking the formation of the GRP75-ANT2-UCP1 complex, thereby alleviating cancer-related cachexia. Withanone can be used in the research of tumors and nervous system diseases.

DQP-997-74 (compound 2i) is a selective negative allosteric modulator of N-methyl-d-aspartate receptor (NMDAR), specifically targeting GluN2C/D (IC₅₀: 0.069 μM and 0.035 μM), with blood-brain barrier penetrability. Where DQP refers to dihydroquinoline-pyrazoline. DQP-997-74 acts synergistically with the agonist glutamate to exhibit time-dependent enhanced potency in inhibiting hypersynchronous activity driven by high-frequency excitatory synaptic transmission. DQP-997-74 reduces the number of epileptogenesis in a murine model of tuberous sclerosis complex (TSC)-induced epilepsy. DQP-997-74 can be used for research on NMDAR-related neurological diseases.

Neboglamine (CR-2249, XY-2401) hydrochloride is an orally active NMDA receptor glycine site positive modulator that can be used in schizophrenia research.

Bupivacaine (hydrochloride) (Standard) is the analytical standard of Bupivacaine (hydrochloride). This product is intended for research and analytical applications. Bupivacaine hydrochloride is a NMDA receptor inhibitor.Bupivacaine can block sodium, L-calcium, and potassium channels.Bupivacaine potently blocks SCN5A channels with the IC₅₀ of 69.5 μM. Bupivacaine hydrochloride can be used for the research of chronic pain.

Decanoic acid-d₃ is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects.