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Results for "

human NaV1.5

" in MedChemExpress (MCE) Product Catalog:

11

Inhibitors & Agonists

1

Peptides

1

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-16787
    ICA-121431
    4 Publications Verification

    		 Sodium Channel Cardiovascular Disease
    ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 μM).
    ICA-121431
  • HY-W052508
    Norquetiapine
    1 Publications Verification

    N-Desalkylquetiapine

    		 Drug Metabolite 5-HT Receptor HCN Channel Serotonin Transporter Neurological Disease
    Norquetiapine ( N-Desalkylauetiapine), a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC50 of 13.9 μM. Norquetiapine selectively inhibits noradrenaline reuptake, is a partial 5-HT1A (Ki = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (Ki = 237 nM), 5-HT2C(Ki = 107 nM), and 5-HT7 (Ki = 76 nM) receptors. Norquetiapine blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine can be used for the study of depression and inflammation .
    Norquetiapine
  • HY-A0079
    Tetracaine

    Amethocaine

    		 Sodium Channel Calcium Channel Neurological Disease
    Tetracaine (Amethocaine) is a sodium channel inhibitor and ryanodine receptor (RyR) inhibitor. Tetracaine blocks sodium conduction across nerve cell membranes, preventing rapid sodium ion influx and depolarization. Tetracaine exhibits biphasic effects on spontaneous sarcoplasmic reticulum Ca 2+ release in Ca 2+-overloaded ventricular myocytes, and increases sarcoplasmic reticulum Ca 2+ load. Tetracaine can be used in research related to eye diseases .
    Tetracaine
  • HY-P1073
    ProTx-I

    		Calcium Channel Potassium Channel Sodium Channel TRP Channel Neurological Disease Cancer
    ProTx-I is a toxin derived from Thrixopelma pruriens and a peptide inhibitor targeting TTX-resistant sodium channels. ProTx-I interacts with voltage sensors of multiple domains such as NaV1.7, reduces neuronal excitability through allosteric modulation of channel gating and alteration of voltage dependence. The IC50 values of ProTx-I against human NaV1.7, NaV1.2, NaV1.6, and NaV1.5 are 95 nM, 104 nM, 21 nM, and 358 nM, respectively; ProTx-I also potently inhibits Ba 2+ currents of hCav3.1, while its inhibitory potency against hCav3.2 is approximately 160-fold lower. ProTx-I is applicable to the research of chronic pain .
    ProTx-I
  • HY-W052508S
    Norquetiapine-d8

    N-Desalkylquetiapine-d8

    		 Isotope-Labeled Compounds Others Neurological Disease Inflammation/Immunology
    Norquetiapine-d8 (N-Desalkylquetiapine-d8) is the deuterium labeled Norquetiapine.Norquetiapine ( N-Desalkylauetiapine), a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC50 of 13.9 μM. Norquetiapine selectively inhibits noradrenaline reuptake, is a partial 5-HT1A (Ki = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (Ki = 237 nM), 5-HT2C(Ki = 107 nM), and 5-HT7 (Ki = 76 nM) receptors. Norquetiapine blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine can be used for the study of depression and inflammation .
    Norquetiapine-d8
  • HY-W040555
    Norquetiapine dihydrochloride
    1 Publications Verification

    N-Desalkylquetiapine dihydrochloride

    		 Drug Metabolite 5-HT Receptor HCN Channel Serotonin Transporter Neurological Disease
    Norquetiapine ( N-Desalkylauetiapine) dihydrochloride, a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC50 of 13.9 μM. Norquetiapine dihydrochloride selectively inhibits noradrenaline reuptake, is a partial 5-HT1A (Ki = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (Ki = 237 nM), 5-HT2C(Ki = 107 nM), and 5-HT7 (Ki = 76 nM) receptors. Norquetiapine dihydrochloride blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine dihydrochloride shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine dihydrochloride can be used for the study of depression and inflammation .
    Norquetiapine dihydrochloride
  • HY-15736
    Sodium Channel inhibitor 1

    		Sodium Channel Neurological Disease
    Sodium Channel inhibitor 1 is a state-dependent voltage-gated NaV1.7 inhibitor with an IC50 of 0.087 μM. Sodium Channel inhibitor 1 can be used for research of pain .
    Sodium Channel inhibitor 1
  • HY-118048
    NAV 26

    		Sodium Channel Neurological Disease
    NAV 26 (Compound 26) is a selective NaV1.7 inhibitor with an IC50 of 0.37 μM. NAV 26 is applicable for pain-related research .
    NAV 26
  • HY-126005
    VGSC blocker-1

    		Sodium Channel Cancer
    VGSC blocker-1 is a potent and small molecule blocker of neonatal isoform of the VGSC subtype, Nav1.5 (nNav1.5). VGSC blocker-1 blocks INa peak currents 34.9% at 1 μM and inhibits cell invasion 0.3% at 1 μM in human breast cancer cell line MDA-MB-231, without affecting the cell viability .
    VGSC blocker-1
  • HY-121675A
    2-Bromo-LSD D-Tartrate

    BOL-148 D-Tartrate; Bromolysergide D-Tartrate

    		 5-HT Receptor G protein-coupled Bile Acid Receptor 1 Neurological Disease
    2-Bromo-LSD D-Tartrate (BOL-148 D-Tartrate) is a blood-brain barrier-permeable 5-HT2A partial agonist and competitive partial antagonist. 2-Bromo-LSD D-Tartrate acts as both a potent partial agonist (with an EC50 of 0.81 nM for Gq dissociation) and a potent partial antagonist (with a KB of 0.18 nM for Gq dissociation) at the 5-HT2A receptor. 2-Bromo-LSD D-Tartrate exhibits partial agonist activity at multiple aminergic GPCRs, including 5-HT2A. 2-Bromo-LSD D-Tartrate lacks 5-HT2B agonist activity. 2-Bromo-LSD D-Tartrate induces dendritogenesis and spinogenesis. 2-Bromo-LSD D-Tartrate reverses the behavioral effects of chronic stress and increases active coping behaviors in mice .
    2-Bromo-LSD D-Tartrate
  • HY-182710
    DA-0218

    		Sodium Channel Neurological Disease
    DA-0218 is a Nav1.7 inhibitor. DA-0218 exerts state-dependent inhibitory effects. DA-0218 alleviates formalin-induced inflammatory pain behavior and Paclitaxel-induced mechanical hyperalgesia in mice. DA-0218 inhibits Histamine-induced acute pruritus and lymphoma-induced chronic pruritus in mice. DA-0218 can be used in research related to inflammatory pain, neuropathic pain, acute pruritus and chronic pruritus .
    DA-0218

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