iGluR Inhibitor

ZCAN262 (compound 6 ) is an AMPA modulator. ZCAN262 prevents AMPA-mediated excitotoxicity by targeting an allosteric binding site.

Pep2-AVKI is a selective peptide inhibitor of the binding of the AMPA receptor subunit (GluR2) at the C-terminal PDZ site to C-kinase (PICK1). Pep2-AVKI does not affect the binding of (AMPA-type glutamate receptor) GluA2 to GRIP or ABP. Pep2-AVKI does not increase the amplitude of AMPA currents. pep2-AVKI can be used to study neurological diseases.

Decanoic acid (Standard) is the analytical standard of Decanoic acid. This product is intended for research and analytical applications. Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy.

Indole-2-carboxylic acid (Standard) is the analytical standard of Indole-2-carboxylic acid. This product is intended for research and analytical applications. 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.

Bupivacaine liposome is a liposome-encapsulated form of Bupivacaine (HY-B0405). Bupivacaine is an NMDA receptor inhibitor. During the action potential, Bupivacaine blocks sodium channels, thereby inhibiting the generation and conduction of nerve impulses induced by painful stimuli. Bupivacaine liposome reduces the release rate of Bupivacaine, thus achieving a long-lasting pain relief effect.

AMPA receptor modulator-1 is a potent, orally active and selective AMPAR regulatory protein TARP γ-8 negative modulator with a pIC₅₀ of 9.7, more selective over GluA1/γ-2 (pIC₅₀=5).

Chlorphenesin carbamate (Standard) is the analytical standard of Chlorphenesin carbamate. This product is intended for research and analytical applications. Chlorphenesin carbamate is a centrally acting skeletal muscle relaxant. Chlorphenesin carbamate can be used for the research of pain and discomfort related to skeletal muscle trauma and inflammation. Chlorphenesin carbamate is a selective blocker of polysynaptic pathways at the spinal and supra-spinal levels. Antinociceptive effect.

Satoprodil (example 2) is a potent N-methyl-D-aspartate (NMDA) receptor negative allosteric modulator with an IC₅₀ value of 123 nM for NR2B.

Profadol (CI-572) hydrochloride is a potent analgesic agent. Profadol is a µ-opioid receptor (MOR) agonist. Profadol hydrochloride activates the γ-aminobutyric acid (GABA) receptors and inhibits the N-methyl-D-aspartate (NMDA) receptor. Profadol increases the mRNA and protein expression of MOR.

(S)-Alaproclate ((S)-GEA 654) is more potent than the R-(+)-enantiomer both in blocking the NMDA receptor currents in vitro and in antagonizing the cGMP increase in vivo.

Antidepressant agent 9 (Compound 24) is an orally active and BBB-penetrable NMDAR and SERT inhibitor with IC₅₀ values of 3.50 μM and 1044 nM, respectively. Antidepressant agent 9 has good metabolic stability and plasma exposure. Antidepressant agent 9 can exert antidepressant-like activity in the mouse forced swim test.

Sapunifiram is a cognitive enhancer. Sapunifiram can be used in studies related to amnesia.

P3LC7LC-P is a blood-brain barrier-permeable BRAG2 ligand with a K_D of 6.14 μM. P3LC7LC-P binds to BRAG2, thereby disrupting its interaction with the GluA2 subunit of the AMPA receptor and inhibiting glutamate-induced GluA2 endocytosis. P3LC7LC-P exerts neuroprotective effects in oxygen-glucose deprivation-induced and glutamate-induced neurotoxicity models, reduces ROS accumulation and inhibits apoptosis, and reduces cerebral infarct size in a rat model of transient middle cerebral artery occlusion. P3LC7LC-P can be used for the research of ischemic stroke.

R-(+)-EU-1180-453 is a positive allosteric modulator targeting NMDA receptors containing GluN2C and GluN2D subunits, with a pEC₅₀ value of 5.5 for both rat receptor subtypes, and it can cross the blood-brain barrier. R-(+)-EU-1180-453 increases the potency of glutamate, enhances receptor responses to maximally effective concentrations of agonists, and acts only on receptors bound to both co-agonists. R-(+)-EU-1180-453 is applicable to research related to Alzheimer's disease, Parkinson's disease, epilepsy, and neuropathic pain.

NMDAR/HDAC-IN-1 (Compound 9d) is a dual NMDAR and HDAC inhibitor with a K_i of 0.59 μM for NMDAR and IC₅₀ values of 2.67, 8.00, 2.21, 0.18 and 0.62 μM for HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8, respectively. NMDAR/HDAC-IN-1 efficiently penetrates the blood brain barrier.

Withanone (Standard) is the analytical standard of Withanone (HY-129692). This product is intended for research and analytical applications. 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.

5-Chloro-1,4-dihydro-2,3-quinoxalinedione (Compound 72) is a weak NMDA inhibitor with an IC₅₀ of 56.3 μM. 5-Chloro-1,4-dihydro-2,3-quinoxalinedione can be used for the research of neurological disease.

LSP-GR3 sodium is a novel chemically-modified RNA oligonucleotides, called splice modulating oligomers (SMOs), which potently and specifically modulate GluR alternative splicing to GluR3-flip expression throughout the CNS.

TAT-CBD3, a 15-amino acid peptide from CRMP2, fused to the TAT cell-penetrating motif of the HIV-1 protein, disrupts CRMP2-NMDAR interaction without change in NMDAR localization.

N20C hydrochloride is a selective and noncompetitive open NMDA receptor open channel blocker, with micromolar affinity, fast on-off blockade kinetics, and strong voltage dependence. Neuroprotective activity.