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nAChR inhibitor

" in MedChemExpress (MCE) Product Catalog:

48

Inhibitors & Agonists

1

Screening Libraries

3

Peptides

13

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3

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-152170

    nAChR Neurological Disease
    bPiDI is a novel selective α6β2 nicotinic receptor antagonist. bPiDI inhibits nicotine-evoked striatal dopamine (DA) release through an interaction with α6β2-containing nAChRs .
    bPiDI
  • HY-B0118A

    ORG NC 45

    nAChR Neurological Disease Cancer
    Vecuronium (ORG NC 45) bromide is a non-depolarizing neuromuscular blocking agent that also acts as a nicotinic acetylcholine receptor (nAChR) inhibitor, a muscle relaxant, and can be used for pre-surgical anesthesia .
    Vecuronium bromide
  • HY-151129

    nAChR Neurological Disease
    nAChR-IN-1 (2,2,6,6-Tetramethylpiperidin-4-yl heptanoate) is a tetramethylpiperidine heptanoate, a selective nicotinic acetylcholine receptor (nAChR) inhibitor that inhibits nAChRs lacking α5, α6, or β3 subunits. nAChR-IN-1 has the effect of preventing nerve disorder, can be used for nicotinic acetylcholine receptor dysfunction or neurological disorders research .
    nAChR-IN-1
  • HY-14316A

    Ebanicline dihydrochloride; ABT-594 dihydrochloride

    nAChR Neurological Disease
    Tebanicline dihydrochloride (Ebanicline dihydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. It inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM .
    Tebanicline dihydrochloride
  • HY-B0118AR

    nAChR Neurological Disease Cancer
    Vecuronium (bromide) (Standard) is the analytical standard of Vecuronium (bromide). This product is intended for research and analytical applications. Vecuronium (ORG NC 45) bromide is a non-depolarizing neuromuscular blocking agent that also acts as a nicotinic acetylcholine receptor (nAChR) inhibitor, a muscle relaxant, and can be used for pre-surgical anesthesia .
    Vecuronium bromide (Standard)
  • HY-N12511

    nAChR Neurological Disease
    Aristoquinoline (Compound 1) is an alkaloid can be isolated from Aristotelia chilensis. Aristoquinoline has α3β4 nAChR inhibitory activity .
    Aristoquinoline
  • HY-107669

    nAChR Neurological Disease
    nAChR-IN-1 (hydrochloride) is a tetramethylpiperidine heptanoate, a selective nicotinic acetylcholine receptor (nAChR) inhibitor that inhibits nAChRs lacking α5, α6, or β3 subunits. nAChR-IN-1 has the effect of preventing nerve disorder, can be used for nicotinic acetylcholine receptor dysfunction or neurological disorders research .
    nAChR-IN-1 hydrochloride
  • HY-P5823

    nAChR Neurological Disease
    Azemiopsin is a potent nicotinic acetylcholine receptor (nAChR) inhibitor with IC50s of 0.18 μM and 22 μM against T. californica nAChR and human α7 nAChR, respectively. Azemiopsin blocks acetylcholine-induced currents in Xenopus oocytes heterologously expressing human muscle-type nAChR .
    Azemiopsin
  • HY-14316B

    Ebanicline hydrochloride; ABT-594 hydrochloride

    nAChR Neurological Disease
    Tebanicline hydrochloride (Ebanicline hydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. Tebanicline hydrochloride inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM .
    Tebanicline hydrochloride
  • HY-157958

    nAChR Neurological Disease
    α7 nAChR modulator-3 (Compound 6p) is a α7 nAChR positive allosteric Modulator with a IC50 value of 1.3 μM. α7 nAChR Modulator-3 can be used to inhibit auditory gating defects in a mouse schizophrenic model .
    α7 nAChR Modulator-3
  • HY-114791

    nAChR Neurological Disease
    Lobelanidine is an antagonist for nicotinic acetylcholine receptor (nAChR), which inhibits α7 nAChR response and α3β2/α3β4 nAChR responses, with IC50 of 2.8 and 8.2 μM .
    Lobelanidine
  • HY-107674

    nAChR Neurological Disease
    bPiDDB is a potent nAChR antagonist. bPiDDB potently (IC50=2 nM) inhibits nicotine-evoked striatal dopamine (DA) release through an interaction with α6β2-containing nAChRs .
    bPiDDB
  • HY-146066

    nAChR JAK STAT NO Synthase Inflammation/Immunology
    α7 nAchR-JAK2-STAT3 agonist 1 is a potent α7 nAchR-JAK2-STAT3 agonist, with an IC50 value of 0.32 μM for nitric oxide (NO). α7 nAchR-JAK2-STAT3 agonist 1 effectively suppresses the expression of iNOS, IL-1β, and IL-6 in murine RAW264.7 macrophages. α7 nAchR-JAK2-STAT3 agonist 1 can inhibit LPS-induced NO release, NF-κB activation and cytokine production. α7 nAchR-JAK2-STAT3 can be used for researching sepsis .
    α7 nAchR-JAK2-STAT3 agonist 1
  • HY-B0282S

    ACh-d4 (chloride)

    nAChR Calcium Channel Endogenous Metabolite Neurological Disease Cancer
    Acetylcholine-d4 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs)[1][2]. Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro[5].
    Acetylcholine-d4 chloride
  • HY-B0282S1

    ACh-d9(chloride)

    nAChR Calcium Channel Endogenous Metabolite Neurological Disease Cancer
    Acetylcholine-d9 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs)[1][2]. Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro[5].
    Acetylcholine-d9 chloride
  • HY-17590
    Radafaxine hydrochloride
    1 Publications Verification

    (S,S)-Hydroxybupropion hydrochloride; GW-353162A; BW-306U

    Monoamine Transporter Neurological Disease
    Radafaxine hydrochloride (GW-353162A) is a DAT (dopamine transporter) and NET(norepinephrine transporter) transporters inhibitor, and nAChR family modulator.
    Radafaxine hydrochloride
  • HY-W795027

    ATX-a

    nAChR Cholinesterase (ChE) Neurological Disease
    Anatoxin-a (ATX-a) is a neurotoxic alkaloid. Anatoxin-a acts as both a nicotinic acetylcholine receptor (nAChR) agonist and an Acetylcholinesterase (AChE) inhibitor .
    Anatoxin-a
  • HY-162497

    nAChR Others
    Insecticidal agent 12 (Compound F45) has insecticidal activity (LC50: 2.94 μg/mL). Insecticidal agent 12 is an nAChR inhibitor .
    Insecticidal agent 12
  • HY-13780
    Vinblastine sulfate
    10+ Cited Publications

    Vincaleukoblastine sulfate salt

    Microtubule/Tubulin Autophagy Cancer
    Vinblastine sulfate is a cytotoxic alkaloid used against various cancer types. Vinblastine sulfate inhibits the formation of microtubule and suppresses nAChR with an IC50 of 8.9 μM.
    Vinblastine sulfate
  • HY-B0282
    Acetylcholine chloride
    10+ Cited Publications

    ACh chloride

    nAChR Calcium Channel Endogenous Metabolite Neurological Disease Cancer
    Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro .
    Acetylcholine chloride
  • HY-B1240
    Droperidol
    3 Publications Verification

    Dehydrobenzperidol

    Dopamine Receptor GABA Receptor nAChR Neurological Disease
    Droperidol (Dehydrobenzperidol) is a butyrophenone pamine-2 receptor antagonist that inhibits the activation of GABA(A) and neuronal nicotinic receptors (nAChR), with IC50 values of 12.6 nM and 5.8 μM. Droperidol has anesthetic and sedative properties .
    Droperidol
  • HY-149483

    nAChR Neurological Disease
    CVN417 is an orally active α6 subunit-containing nAChR antagonist, modulating phasic dopaminergic neurotransmission in an impulse-dependent manner. CVN417 inhibits Ca(2+) effluents mediated by nAChR subunits with IC50s of 0.086 μM (α6), 2.56 μM (α3) and 0.657 μM (α4), respectively. CVN417 attenuates resting tremor in Rodent models, displays the potential to improve movement dysfunction, in conditions such as Parkinson's disease .
    CVN417
  • HY-B1700A

    nAChR Neurological Disease
    Mivacurium dichloride is a benzylisoquinoline derivative and is a short-acting non-depolarizing neuromuscular blocking agent and skeletal muscle relaxant. Mivacurium dichloride couples with the nAChR to reduce or inhibit the depolarizing effect of acetylcholine on the terminal disc of the muscle cell .
    Mivacurium dichloride
  • HY-135783

    nAChR Neurological Disease
    AT 1001 is a high-affinity and selective antagonist of the α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) (Ki=2.64 nM). AT 1001 reversibly blocks inward currents induced by Epibatidine (HY-101078) in HEK cells transfected with α3β4 nAChR. AT-1001 dose-dependently inhibits nicotine self-administration behavior in rats without affecting food-reinforced responding. AT 1001 can be utilized in the research of nicotine addiction and smoking cessation therapies .
    AT 1001
  • HY-13780R

    Microtubule/Tubulin Autophagy Cancer
    Vinblastine (sulfate) (Standard) is the analytical standard of Vinblastine (sulfate). This product is intended for research and analytical applications. Vinblastine sulfate is a cytotoxic alkaloid used against various cancer types. Vinblastine sulfate inhibits the formation of microtubule and suppresses nAChR with an IC50 of 8.9 μM.
    Vinblastine sulfate (Standard)
  • HY-P1271

    nAChR Cardiovascular Disease
    Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .
    Catestatin
  • HY-P1271A

    nAChR Cardiovascular Disease
    Catestatin TFA is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin TFA is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin TFA is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .
    Catestatin TFA
  • HY-105858

    H-Ile-Trp-OH; IW-2143

    nAChR Neurological Disease
    BNC210 (H-Ile-Trp-OH) is an orally active α7 nAChR negative alteration modulator (NAM) with no apparent side effects. BNC210 exhibits acute anxiolytic activity in rodent models of anxiety. BNC210 inhibits rat and human α7 nAChR currents (in stably transfected cell lines) induced by acetylcholine, nicotine, choline, and the a7-specific agonist PNU-282987 with IC50 values in the range of 1.2 to 3 μM. BNC210 can be used in studies of anxiety, trauma, and stressor-related disorders .
    BNC210
  • HY-161671

    nAChR Neurological Disease
    GAT2711 (compound 3h) is a full agonist of α9 nAChR with an EC50 of 230 nM. GAT2711 inhibits ATP-induced IL-1β release in THP-1 cells and exhibits analgesic activity in α7 knockout mice .
    GAT2711
  • HY-105118A

    CGS-9343B; KW 5617

    Calmodulin Neurological Disease Metabolic Disease Inflammation/Immunology
    Zaldaride maleate (CGS-9343B) is a potent, orally active and selective inhibitor of calmodulin. Zaldaride maleate inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase activity, with an IC50 of 3.3 nM . Zaldaride maleate prevents estrogen-induced transcription activation by ER, reversibly blocks voltage-activated Na +, Ca 2+ and K + currents in PC12 cells and inhibits nAChR .
    Zaldaride maleate
  • HY-126638

    NSC 324645

    Parasite Infection
    Marcfortine A is an indole alkaloid originally isolated from P. roqueforti. It has nematocidal activity against the parasitic nematode H. contortus (LD99=0.06 μg/mL) and inhibits motility of adult worms (EC50=2 μM). Marcfortine A eliminates H. contortus, T. colubriformis, and O. ostertagi from experimentally infected jirds (ED95s=0.33, 0.11, and 2.5 mg/animal, respectively). It dose-dependently inhibits nicotine-induced calcium mobilization in SH-SY5Y and TE-671 cells expressing α3 subunit-containing human nicotinic acetylcholine receptors (nAChRs) and muscle-type nAChRs, respectively.
    Marcfortine A
  • HY-105118

    CGS-9343B free base; KW 5617 free base

    Calmodulin Neurological Disease Metabolic Disease Inflammation/Immunology
    Zaldaride (CGS-9343B free base) is a potent, orally active and selective inhibitor of calmodulin. Zaldaride inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase activity, with an IC50 of 3.3 nM . Zaldaride prevents estrogen-induced transcription activation by ER, reversibly blocks voltage-activated Na +, Ca 2+ and K + currents in PC12 cells and inhibits nAChR .
    Zaldaride
  • HY-N10132

    nAChR Infection Neurological Disease
    Microgrewiapine A is an antagonist of nAChR. Microgrewiapine A inhibits hα4β2 and hα3β4 activity with 60% and 70% inhibition, respectively. Microgrewiapine A has selective cytotoxic against HT-29 human colon cancer cells with an IC50 of 6.8 μM .
    Microgrewiapine A
  • HY-B0282R

    nAChR Calcium Channel Endogenous Metabolite Neurological Disease Cancer
    Acetylcholine (chloride) (Standard) is the analytical standard of Acetylcholine (chloride). This product is intended for research and analytical applications. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro .
    Acetylcholine chloride (Standard)
  • HY-B1700AR

    nAChR Neurological Disease
    Mivacurium (dichloride) (Standard) is the analytical standard of Mivacurium (dichloride). This product is intended for research and analytical applications. Mivacurium dichloride is a benzylisoquinoline derivative and is a short-acting non-depolarizing neuromuscular blocking agent and skeletal muscle relaxant. Mivacurium dichloride couples with the nAChR to reduce or inhibit the depolarizing effect of acetylcholine on the terminal disc of the muscle cell .
    Mivacurium dichloride (Standard)
  • HY-B0379A

    nAChR Neurological Disease
    Adiphenine hydrochloride is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC50s of 1.9, 1.8, 3.7, and 6.3 μM for α1, α3β4, α4β2, and α4β4, respectively. Adiphenine hydrochloride has anticonvulsant effects .
    Adiphenine hydrochloride
  • HY-126047B

    NF-κB Amyloid-β nAChR Neurological Disease Inflammation/Immunology
    (R)-(+)-Anatabine is an less active R-enantiomer of Anatabine. Anatabine is a potent α4β2 nAChR agonist . Anatabine inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment .
    (R)-(+)-Anatabine
  • HY-A0009
    Galanthamine hydrobromide
    10+ Cited Publications

    Galantamine hydrobromide

    Cholinesterase (ChE) nAChR Neurological Disease
    Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
    Galanthamine hydrobromide
  • HY-163980

    Cholinesterase (ChE) nAChR Others
    AChE-IN-73 (compound 6) is an insecticide with higher toxicity than HY-B0815. The LC50 for C. pipiens is 78.0 mg/L. AChE-IN-73 has high affinity for acetylcholinesterase (AChE) and nicotinic acetylcholine receptors (nAChR), with binding energies of -8.11 kcal/mol and -6.27 kcal/mol, respectively. AChE-IN-73 is a potentially potent mosquito inhibitor .
    AChE-IN-73
  • HY-19918A

    NF-κB Amyloid-β nAChR Neurological Disease Inflammation/Immunology
    Anatabine dicitrate is a tobacco alkaloid that can cross the blood-brain barrier. Anatabine dicitrate is a potent α4β2 nAChR agonist. Anatabine dicitrate inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine dicitrate has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment .
    Anatabine dicitrate
  • HY-116522
    AR420626
    3 Publications Verification

    Free Fatty Acid Receptor Histone Methyltransferase HDAC mTOR CaMK p38 MAPK Epigenetic Reader Domain GLUT nAChR TNF Receptor Metabolic Disease Inflammation/Immunology Cancer
    AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3) (IC50=117 nM). AR420626 has anti-inflammatory, anticancer and antidiabetic activities. AR420626 improves neurogenic diarrhea by inhibiting nAChR mediated neural pathways. AR420626 inhibits the growth of HepG2 xenografts and inhibits the proliferation of hepatoma cells by inducing apoptosis. AR420626 also suppresses allergic asthma and eczema and has the ability to activate GPR41 to increase Ca 2+ signal-mediated glucose uptake and improve diabetes .
    AR420626
  • HY-B0379AR

    nAChR Neurological Disease
    Adiphenine (hydrochloride) (Standard) is the analytical standard of Adiphenine (hydrochloride). This product is intended for research and analytical applications. Adiphenine hydrochloride is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC50s of 1.9, 1.8, 3.7, and 6.3 μM for α1, α3β4, α4β2, and α4β4, respectively. Adiphenine hydrochloride has anticonvulsant effects .
    Adiphenine hydrochloride (Standard)
  • HY-A0009S

    Galantamine-d3 hydrobromide

    Isotope-Labeled Compounds Cholinesterase (ChE) nAChR Neurological Disease
    Galanthamine-d3 (hydrobromide) is deuterium labeled Galanthamine (hydrobromide). Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD)[1][2][3].
    Galanthamine-d3 hydrobromide
  • HY-A0009R

    Galantamine hydrobromide (Standard)

    nAChR Cholinesterase (ChE) Neurological Disease
    Galanthamine (hydrobromide) (Standard) is the analytical standard of Galanthamine (hydrobromide). This product is intended for research and analytical applications. Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
    Galanthamine hydrobromide (Standard)
  • HY-118990

    Others Neurological Disease
    Lobelane hydrochloride is a biologically active compound that has the activity of inhibiting vesicular monoamine transporter-2 (VMAT2). Lobelane hydrochloride has a low affinity for nicotinic acetylcholine receptors (nAChR), thereby enhancing its selectivity for VMAT2. Synthetic structural changes of lobelane hydrochloride have led to some related analogs that show mild changes in affinity for VMAT2. The most potent synthetic lobelane hydrochloride obtained after structural modification has a K(i) value of 630 nM, showing significant VMAT2 selectivity. The biological activity of lobelane hydrochloride suggests that it has the potential to be used in the development of compounds to inhibit methamphetamine abuse .
    Lobelane hydrochloride
  • HY-126049

    (S)-(-)-Oxiracetam; (S)-ISF2522

    Apoptosis Neurological Disease
    (S)-oxiracetam (S-ORC) is an inhibitor targeting apoptosis. S-ORC reduces brain infarct size and lessens neurological dysfunction in middle cerebral artery occlusion/reperfusion (MCAO/R) models. S-ORC prevents neuronal apoptosis via activating PI3K/Akt/GSK3β signaling pathway via α7 nAChR after ischemic stroke. S-ORC can prevent neuronal death after ischemic stroke .
    (S)-Oxiracetam
  • HY-15310
    Ivermectin
    Maximum Cited Publications
    24 Publications Verification

    MK-933; CD-5024; K-237

    Flavivirus Dengue virus Parasite HIV Mitophagy HSV SARS-CoV Antibiotic Autophagy Bacterial Infection Cancer
    Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import . Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19 .
    Ivermectin
  • HY-15310R

    Dengue virus Flavivirus Parasite HIV Mitophagy HSV SARS-CoV Antibiotic Autophagy Bacterial Infection Cancer
    Ivermectin (Standard) is the analytical standard of Ivermectin. This product is intended for research and analytical applications. Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import . Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19 .
    Ivermectin (Standard)

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