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Results for "

hyperexcitability

" in MedChemExpress (MCE) Product Catalog:

27

Inhibitors & Agonists

1

Peptides

1

Natural
Products

4

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-109061
    Lazertinib
    3 Publications Verification

    YH25448; GNS-1480

    		 Apoptosis Akt TRP Channel EGFR ERK Infection Neurological Disease Metabolic Disease Cancer
    Lazertinib (YH25448; GNS-1480) is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
    Lazertinib
  • HY-12646
    Rhosin hydrochloride
    Maximum Cited Publications
    40 Publications Verification

    		 Ras Apoptosis Cancer
    Rhosin hydrochloride is a potent, specific RhoA subfamily Rho GTPases inhibitor. Rhosin hydrochloride specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin hydrochloride induces cell apoptosis . Rhosin hydrochloride promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability .
    Rhosin hydrochloride
  • HY-12646A
    Rhosin
    Maximum Cited Publications
    40 Publications Verification

    		 Ras Apoptosis Cancer
    Rhosin is a potent, specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin induces cell apoptosis . Rhosin promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability .
    Rhosin
  • HY-147423
    Zandatrigine
    1 Publications Verification

    NBI-921352; XEN901

    		 Sodium Channel Neurological Disease
    Zandatrigine (NBI-921352; XEN901) is a selective, orally active, voltage-gated sodium channel NaV1.6/SCN8A inhibitor that can penetrate the blood-brain barrier. Zandatrigine inhibits sodium influx by non-covalently binding to the VSD4 structure of NaV1.6, blocking the persistent and resuscitative currents under pathological conditions. Zandatrigine can reduce neuronal hyperexcitability and reduce epileptic seizures. Zandatrigine is 134-756-fold selective for other isoforms such as NaV1.1 and NaV1.2, and has minimal effect on NaV1.1 expressed by inhibitory interneurons. Zandatrigine can be used to study NaV1.6-mediated neuroexcitability diseases such as SCN8A-related developmental epileptic encephalopathy (SCN8A-DEE) and adult focal epilepsy .
    Zandatrigine
  • HY-A0042
    Rufinamide

    CGP 33101; E 2080; RUF 331

    		 Sodium Channel Neurological Disease
    Rufinamide (CGP 33101) is an orally active antiepileptic compound that inhibits Na + current activation, inhibits neuronal hyperexcitability, and has anticonvulsant effects. Rufinamide is used in the study of Lennox-Gastaut syndrome .
    Rufinamide
  • HY-13106
    Olodanrigan
    4 Publications Verification

    EMA401; PD-126055; (S)-EMA400

    		 Angiotensin Receptor Cardiovascular Disease Neurological Disease Endocrinology
    Olodanrigan (EMA401) is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist. It is under development as a neuropathic pain therapeutic agent. Olodanrigan (EMA401) analgesic action appears to involve inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons .
    Olodanrigan
  • HY-15416
    NS309

    		Potassium Channel Cardiovascular Disease Neurological Disease
    NS309 is a potent and selective activator of the Ca 2+-activated SK/IK potassium channels, but displays no activity at BK channels .
    NS309
  • HY-W011602
    Triethyl citrate

    		Environmental Pollutants Biochemical Assay Reagents Neurological Disease
    Triethyl citrate is an orally active citrate compound. Triethyl citrate induces acute toxic effects, including weakness, depression, ataxia, hyperexcitability, restlessness, dripping urine, and irregular, labored breathing. Triethyl citrate can be used in research on plasticizers for food packaging materials .
    Triethyl citrate
  • HY-109061B
    Lazertinib mesylate
    3 Publications Verification

    YH25448 mesylate; GNS-1480 mesylate

    		 TRP Channel EGFR Akt ERK Apoptosis Cancer
    Lazertinib (YH25448; GNS-1480) mesylate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
    Lazertinib mesylate
  • HY-110162
    QO 58

    		Potassium Channel Neurological Disease
    QO 58 is a potent modulator of K(v)7 channels. QO-58 increases the current amplitudes, shifts the voltage-dependent activation curve in a more negative direction and slows the deactivation of K(v)7.2/K(v)7.3 currents. QO-58 has the potential for the research of diseases associated with neuronal hyperexcitability .
    QO 58
  • HY-123264
    RL648_81

    		Potassium Channel Neurological Disease
    RL648_81 is a specific KQT-like subfamily 2/3 (KCNQ2/3) activator with an EC50 of 190 nM. RL648_81 robustly shifts the V1/2 of KCNQ2/3 channels towards hyperpolarized potentials.RL648_81 does not shift the V1/2 of either KCNQ4 or KCNQ5.RL648_81 has?the?potential?for?neurologic disorders associated with neuronal hyperexcitability research .
    RL648_81
  • HY-179215
    OV329 hydrochloride

    		GABA Receptor Neurological Disease
    OV329 hydrochloride is a potent GABA aminotransferase inactivator. OV329 hydrochloride is a Vigabatrin (HY-15399) analogue. OV329 hydrochloride can increase brain GABA levels and block abnormal intracerebral hyperexcitability. OV329 hydrochloride exhibits anticonvulsant and antiepileptic activities. OV329 hydrochloride can be used for the research of neurological disease, such as seizure .
    OV329 hydrochloride
  • HY-179215A
    OV329

    		GABA Receptor Neurological Disease
    OV329 is a potent GABA aminotransferase inactivator. OV329 is a Vigabatrin (HY-15399) analogue. OV329 can increase brain GABA levels and block abnormal intracerebral hyperexcitability. OV329 exhibits anticonvulsant and antiepileptic activities. OV329 can be used for the research of neurological disease, such as seizure .
    OV329
  • HY-P5183
    Hm1a

    		Sodium Channel Neurological Disease
    Hm1a is a venom peptide and a selective hNaV1.1 activator with an EC50 of 7.5 nM. Hm1a enhances hNaV1.1 and hNaV1.3 channel currents via delayed inactivation. Hm1a restores action potential firing in Dravet syndrome GABAergic inhibitory interneurons, reduces interictal epileptiform discharges and whole-brain hyperexcitability, lowers seizure frequency, and rescues premature death in Dravet syndrome mice. Hm1a can be used for the research of neurological disease, such as Dravet syndrome .
    Hm1a
  • HY-13106A
    Olodanrigan sodium

    EMA401 sodium; PD-126055 sodium

    		 Angiotensin Receptor Neurological Disease Endocrinology
    Olodanrigan (EMA401) sodium is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist. Olodanrigan sodium is under development as a neuropathic pain therapeutic agent. Olodanrigan sodium analgesic action appears to involve inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons .
    Olodanrigan sodium
  • HY-B0828
    Triazophos

    		Parasite Cholinesterase (ChE) Others
    Triazophos, a non-systemic insecticide and acaricide that acts as an acetylcholinesterase (AChE) inhibitor, covalently and irreversibly binds to the acetylcholine binding site, thus blocking the hydrolysis of acetylcholine and leading to hyperexcitability; it is effective against a variety of soil insects and mites, including aphids, thrips, midges, beetles, Lepidoptera larvae, cutworms, and spider mites in crops such as ornamentals, cotton, rice, maize, soybeans, oil palms, olives, and coffee.
    Triazophos
  • HY-120484
    A-1048400

    		Calcium Channel Neurological Disease
    A-1048400 is an orally active and selective calcium channel inhibitor with an IC50 value of 1.4 μM for N-type channels, 1.2 μM for T-type channel. A-1048400 inhibits neurotransmitter release and reduces membrane hyperexcitability, exerting potent analgesic activity. A-1048400 is promising for research of neuropathic pain (e.g., pain induced by spinal nerve ligation and chronic constriction injury) .
    A-1048400
  • HY-174146
    5-HT1A agonist 1

    		5-HT Receptor Neurological Disease
    5-HT1A agonist 1 (Compound Ex.37) is a highly selective 5-HT1a receptor agonist (EC50=0.18 nM). 5-HT1A agonist 1 mimicks serotonin binding to the receptor, promotes postsynaptic membrane hyperpolarization, inhibits neuronal hyperexcitability, and reduces the release of anxiety-related neurotransmitters. 5-HT1A agonist 1 is promising for research of neuropsychiatric diseases .
    5-HT1A agonist 1
  • HY-A0042R
    Rufinamide (Standard)

    CGP 33101 (Standard); E 2080 (Standard); RUF 331 (Standard)

    		 Sodium Channel Reference Standards Neurological Disease
    Rufinamide (Standard) is the analytical standard of Rufinamide (HY-A0042). This product is intended for research and analytical applications. Rufinamide (CGP 33101) is an orally active antiepileptic compound that inhibits Na + current activation, inhibits neuronal hyperexcitability, and has anticonvulsant effects. Rufinamide is used in the study of Lennox-Gastaut syndrome .
    Rufinamide (Standard)
  • HY-A0042S
    Rufinamide-d2

    CGP 33101-d2; E 2080-d2; RUF 331-d2

    		 Isotope-Labeled Compounds Sodium Channel Neurological Disease
    Rufinamide-d2 (CGP 33101-d2) is the deuterium labeled Rufinamide (HY-A0042). Rufinamide (CGP 33101) is an orally active antiepileptic compound that inhibits Na + current activation, inhibits neuronal hyperexcitability, and has anticonvulsant effects. Rufinamide is used in the study of Lennox-Gastaut syndrome .
    Rufinamide-d2
  • HY-A0042S1
    Rufinamide-15N,d2

    CGP 33101-15N,d2; E 2080-15N,d2; RUF 331-15N,d2

    		 Isotope-Labeled Compounds Sodium Channel Neurological Disease
    Rufinamide- 15N,d2 (CGP 33101- 15N,d2) is the deuterium and 15N labeled Rufinamide (HY-A0042).Rufinamide (CGP 33101) is an orally active antiepileptic compound that inhibits Na + current activation, inhibits neuronal hyperexcitability, and has anticonvulsant effects. Rufinamide is used in the study of Lennox-Gastaut syndrome .
    Rufinamide-15N,d2
  • HY-A0042S2
    Rufinamide-15N,d2-1

    CGP 33101-15N,d2-1; E 2080-15N,d2-1; RUF 331-15N,d2-1

    		 Isotope-Labeled Compounds Sodium Channel Neurological Disease
    Rufinamide- 15N,d2-1 (CGP 33101- 15N,d2-1) is 15N- and deuterium-labeled Rufinamide (HY-A0042).Rufinamide (CGP 33101) is an orally active antiepileptic compound that inhibits Na + current activation, inhibits neuronal hyperexcitability, and has anticonvulsant effects. Rufinamide is used in the study of Lennox-Gastaut syndrome .
    Rufinamide-15N,d2-1
  • HY-100196AR
    Pyrroloquinoline quinone disodium salt (Standard)

    PQQ disodium salt (Standard); Methoxatin disodium salt (Standard)

    		 Reference Standards Endogenous Metabolite Inflammation/Immunology
    Triazophos (Standard) is the analytical standard of Triazophos. This product is intended for research and analytical applications. Triazophos, a non-systemic insecticide and acaricide that acts as an acetylcholinesterase (AChE) inhibitor, covalently and irreversibly binds to the acetylcholine binding site, thus blocking the hydrolysis of acetylcholine and leading to hyperexcitability; it is effective against a variety of soil insects and mites, including aphids, thrips, midges, beetles, Lepidoptera larvae, cutworms, and spider mites in crops such as ornamentals, cotton, rice, maize, soybeans, oil palms, olives, and coffee.
    Pyrroloquinoline quinone disodium salt (Standard)
  • HY-B0828R
    Triazophos (Standard)

    		Parasite Reference Standards Others
    Triazophos (Standard) is the analytical standard of Triazophos. This product is intended for research and analytical applications. Triazophos, a non-systemic insecticide and acaricide that acts as an acetylcholinesterase (AChE) inhibitor, covalently and irreversibly binds to the acetylcholine binding site, thus blocking the hydrolysis of acetylcholine and leading to hyperexcitability; it is effective against a variety of soil insects and mites, including aphids, thrips, midges, beetles, Lepidoptera larvae, cutworms, and spider mites in crops such as ornamentals, cotton, rice, maize, soybeans, oil palms, olives, and coffee.
    Triazophos (Standard)
  • HY-182459
    Org 34167 (freebase)

    		HCN Channel Neurological Disease
    Org 34167 freebase is a blood-brain barrier permeable HCN channel modulator. Org 34167 freebase possesses high Caco-2 cell permeability. Org 34167 freebase modulates HCN channel function to alter activation properties and suppress neuronal hyperexcitability. Org 34167 freebase induces tremors in mice at specific doses. Org 34167 freebase acts as a research tool for studies on developmental and epileptic encephalopathies as well as depression .
    Org 34167 (freebase)
  • HY-B0828S
    Triazophos-d5

    Hostathion 40EC-d5; Hostathion-d5; Hostation-d5

    		 Isotope-Labeled Compounds Parasite Cholinesterase (ChE) Others
    Triazophos-d5 (Hostathion 40EC-d5) is the deuterium labeled Triazophos(HY-B0828) . Triazophos, a non-systemic insecticide and acaricide that acts as an acetylcholinesterase (AChE) inhibitor, covalently and irreversibly binds to the acetylcholine binding site, thus blocking the hydrolysis of acetylcholine and leading to hyperexcitability; it is effective against a variety of soil insects and mites, including aphids, thrips, midges, beetles, Lepidoptera larvae, cutworms, and spider mites in crops such as ornamentals, cotton, rice, maize, soybeans, oil palms, olives, and coffee.
    Triazophos-d5
  • HY-109061A
    Lazertinib mesylate hydrate

    YH25448 mesylate hydrate; GNS-1480 mesylate hydrate

    		 Apoptosis Akt TRP Channel EGFR ERK Cancer
    Lazertinib (YH25448; GNS-1480) mesylate hydrate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate hydrate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate hydrate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate hydrate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate hydrate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
    Lazertinib mesylate hydrate

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