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Pathways Recommended:	Membrane Transporter/Ion Channel

Results for "

Nav1.5 sodium channel

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Sodium Channel (23) 5-HT Receptor (3) Akt (2) Apoptosis (2) Autophagy (2) Calcium Channel (6) CaMK (2) CRAC Channel (2) Dipeptidyl Peptidase (1) Drug Metabolite (2) G protein-coupled Bile Acid Receptor 1 (1) HCN Channel (2) Isotope-Labeled Compounds (1) Na+/Ca2+ Exchanger (2) Potassium Channel (3) Reference Standards (1) Serotonin Transporter (2) TRP Channel (4)
By Research Areas:	Cancer (4) Cardiovascular Disease (6) Inflammation/Immunology (4) Neurological Disease (22)

Inhibitors & Agonists

Bibliotecas de Screening

Fluorescent Dyes

Peptides

Isotope-Labeled Compounds

Targets Recommended: Sodium Phosphate Cotransporter Sodium Chloride Cotransporter (NCC) Sodium Channel Na+/H+ Exchanger (NHE) SGLT Na+/K+ ATPase Apical Sodium-Dependent Bile Acid Transporter

Cat. No.	Nombre del producto	Target	Áreas de investigación	Chemical Structure

HY-100001

SKF-96365 (hydrochloride) Maximum Cited Publications 27 Publications Verification	TRP Channel CRAC Channel Autophagy CaMK Akt Apoptosis Na+/Ca2+ Exchanger Calcium Channel	Neurological Disease Inflammation/Immunology Cancer
SKF-96365 hydrochloride is a TRPC channel antagonist and store-operated calcium entry (SOCE) inhibitor. SKF-96365 hydrochloride reduces calcium ion influx by inhibiting the activity and expression of TRPC6, STIM1 and Orai1. SKF-96365 hydrochloride inhibits voltage-gated sodium current (cardiac *I_Na/NaV1.5) and slows myocardial conduction. SKF-96365 hydrochloride inhibits phosphorylation/activation of CaMKIIγ* and suppresses the downstream AKT signaling pathway. SKF-96365 hydrochloride induces G₂/M phase cell cycle arrest, apoptosis and cytoprotective autophagy in colorectal cancer cells. SKF-96365 hydrochloride alleviates allergic rhinitis symptoms by reducing inflammatory cytokine levels. SKF-96365 hydrochloride reduces intracellular calcium overload, inhibits Homer1 expression, prevents nuclear damage and suppresses apoptosis. SKF-96365 hydrochloride inhibits the growth of colorectal cancer xenografts in nude mice . SKF-96365 hydrochloride is applicable to research related to allergic rhinitis, colorectal cancer, Parkinson's disease, persistent spontaneous nociception and hyperalgesia .

HY-17429

Flecainide acetate 3 Publications Verification R-818	Sodium Channel	Cardiovascular Disease
Flecainide acetate (R-818) is a class 1C antiarrhythmic agent especially used for the management of supraventricular arrhythmia; works by blocking the Nav1.5 sodium channel in the heart, causing prolongation of the cardiac action potential.

HY-16787

ICA-121431 4 Publications Verification	Sodium Channel	Cardiovascular Disease
ICA-121431 is a nanomolar potent and broad-spectrum *voltage-gated sodium channel* (Na_v) blocker, shows equipotent selectivity for human Na_v1.1 and Na_v1.3 subtypes with IC₅₀ values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Na_v1.2 (IC₅₀*=240 nM) and 1,000 fold selectivity against Na_v1.4, Na_v1.6, and the TTX-resistant human Na_v1.5* and Na_v1.8 channels (IC₅₀s >10 μM).

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-HT_1A (K_i = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (K_i = 237 nM), 5-HT_2C(K_i = 107 nM), and 5-HT₇ (K_i = 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 .

HY-148792

Relutrigine PRAX-562	Sodium Channel	Neurological Disease
Relutrigine (PRAX-562) is an orally active inhibitor of persistent sodium channel. Relutrigine potently and preferentially inhibits persistent I_Na induced by ATX-II (Nav 1.5 activator) or the SCN8A mutation N1768D with IC₅₀ values of 141 nM and 75 nM, respectively. Relutrigine exhibits potent use-dependent block and reduces neuronal intrinsic excitability. Relutrigine has effective anticonvulsant activity .

HY-16723

Funapide TV 45070; XEN402	Sodium Channel	Neurological Disease Inflammation/Immunology
Funapide (TV 45070; XEN402) is an orally active inhibitor of *voltage-gated sodium channels* (VGSC) in the peripheral nervous system with IC₅₀ values ??of 84 nM and 54 nM for Nav1.5 and Nav1.7**, respectively. Funapide has analgesic effects .

HY-133012

GFB-8438	TRP Channel	Neurological Disease
GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC₅₀s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model .

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 .

HY-133910

Lu AE98134 1 Publications Verification	Sodium Channel	Neurological Disease
Lu AE98134, an activator of voltage-gated sodium channels, acts as a partly selective Na_v1.1 channels positive modulator. Lu AE98134 also increases the activity of Na_v1.2 and Na_v1.5 channels but not of Na_v1.4, Na_v1.6 and Na_v1.7 channels. Lu AE98134 can be used to analyze pathophysiological functions of the Na_v1.1 channel in various central nervous system diseases, including cognitive restoring in schizophrenia, et al .

HY-123824

GNE-0439	Sodium Channel	Neurological Disease
GNE-0439 is a novel Nav1.7-selective inhibitor with IC₅₀ of 0.34 uM and inhibits Nav1.5 with an IC₅₀ of 38.3 μM. GNE-0439 inhibits mutant N1742K channels (IC₅₀=0.37 uM) in membrane potential assays. GNE-0439 possesses a carboxylic acid group, binds outside of the channel pore, and is unique compared with known selective VSD4 binders .

HY-178494

Nav1.7-IN-19	Sodium Channel Potassium Channel	Neurological Disease
Nav1.7-IN-19 is a potent, selective and orally active Nav1.7 inhibitor with an IC₅₀ of 0.49 μM. Nav1.7-IN-19 shows high selectivity for Nav1.7, with selectivities of 312-fold and 662-fold against Nav1.1 and Nav1.5 in the inactivated state. Nav1.7-IN-19 exhibits weak inhibition on hERG potassium channels. Nav1.7-IN-19 exhibits analgesic effect and can be used for the research of neurological disease .

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 .

HY-P1218B

Phrixotoxin 3-NH2 TFA	Sodium Channel	Neurological Disease
Phrixotoxin 3-NH2 TFA is a derivative of Phrixotoxin 3 TFA (HY-P1218A). Phrixotoxin 3 TFA is a potent blocker of voltage-gated sodium channels, with IC₅₀s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and *NaV1.5, respectively. Phrixotoxin 3 TFA modulates voltage-gated sodium channels* with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current .

HY-125942

SKF-96365 Maximum Cited Publications 27 Publications Verification	CRAC Channel TRP Channel CaMK Akt Apoptosis Autophagy Na+/Ca2+ Exchanger Calcium Channel	Neurological Disease Inflammation/Immunology Cancer
SKF-96365 is a TRPC channel antagonist and store-operated calcium entry (SOCE) inhibitor. SKF-96365 reduces calcium ion influx by inhibiting the activity and expression of TRPC6, STIM1 and Orai1. SKF-96365 inhibits voltage-gated sodium current (cardiac *I_Na/NaV1.5) and slows myocardial conduction. SKF-96365 inhibits phosphorylation/activation of CaMKIIγ* and suppresses the downstream AKT signaling pathway. SKF-96365 induces G₂/M phase cell cycle arrest, apoptosis and cytoprotective autophagy in colorectal cancer cells. SKF-96365 alleviates allergic rhinitis symptoms by reducing inflammatory cytokine levels. SKF-96365 reduces intracellular calcium overload, inhibits Homer1 expression, prevents nuclear damage and suppresses apoptosis. SKF-96365 inhibits the growth of colorectal cancer xenografts in nude mice . SKF-96365 is applicable to research related to allergic rhinitis, colorectal cancer, Parkinson's disease, persistent spontaneous nociception and hyperalgesia .

HY-120774

GS-462808	Sodium Channel	Cardiovascular Disease
GS-462808 is an oral active late sodium current inhibitor (Late INai) of the cardiac **Nav1.5 channel with the IC₅₀** of 1.33 μM. GS-462808 can be used for study of arrhythmia .

HY-P1218

Phrixotoxin 3	Sodium Channel	Neurological Disease
Phrixotoxin 3 is a potent blocker of voltage-gated sodium channels, with IC₅₀s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and *NaV1.5, respectively. Phrixotoxin 3 modulates voltage-gated sodium channels* with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current .

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-HT_1A (K_i = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (K_i = 237 nM), 5-HT_2C(K_i = 107 nM), and 5-HT₇ (K_i = 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 .

HY-P1219

Jingzhaotoxin-III β-TRTX-Cj1α	Sodium Channel	Neurological Disease
Jingzhaotoxin-III is a potent and selective blocker of **Nav1.5 channels, with an IC₅₀** of 348 nM, and shows no effect on other sodium channel isoforms. Jingzhaotoxin-III can selectively inhibit the activation of cardiac sodium channel but not neuronal subtypes, and hopefully represents an important ligand for discriminating cardiac VGSC subtype .

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-HT_1A (K_i = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (K_i = 237 nM), 5-HT_2C(K_i = 107 nM), and 5-HT₇ (K_i = 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 .

HY-17429S

Flecainide-d4 acetate R-818-d₄	Sodium Channel	Cardiovascular Disease
Flecainide-d₄ (acetate) is the deuterium labeled Flecainide acetate. Flecainide acetate (R-818) is a class 1C antiarrhythmic agent especially used for the management of supraventricular arrhythmia; works by blocking the Nav1.5 sodium channel in the heart, causing prolongation of the cardiac action potential .

HY-175226

DPP8/9-IN-2	Dipeptidyl Peptidase Calcium Channel Sodium Channel Potassium Channel	Cancer
DPP8/9-IN-2 (Compound 21) is a DPP8/9 inhibitor with IC₅₀ values of 0.22 nM and 3 nM, respectively, and K_i values of 2.9 nM and 6 nM, respectively . DPP8/9-IN-2 has certain cardiotoxicity, with IC₅₀ values of 0.7 μM, 29.0 μM and 27.7 μM for hERG potassium channel, *Nav1.5* sodium channel and Cav1.2 calcium channel, respectively. DPP8/9-IN-2 can be used in the research of diseases such as tumors .

HY-P1681A

GpTx-1 TFA	Sodium Channel	Neurological Disease
GpTx-1 TFA is a peptide-based Na_V1.7 sodium channel antagonist isolated from the venom of the Chilean spider Grammostola porter. GpTx-1 TFA demonstrates potent inhibitory activity against the Na_V1.7 channel with an IC₅₀ value of 10 nM, while exhibiting excellent selectivity for Na_V1.4 (IC₅₀ = 0.301 μM) and *Na_V1.5* (IC₅₀ = 4.20 μM), showing >20-fold and >950-fold selectivity respectively .

HY-P1681

GpTx-1	Sodium Channel	Neurological Disease
GpTx-1 is a peptide-based Na_V1.7 sodium channel antagonist isolated from the venom of the Chilean spider Grammostola porter. GpTx-1 demonstrates potent inhibitory activity against the Na_V1.7 channel with an IC₅₀ value of 10 nM, while exhibiting excellent selectivity for Na_V1.4 (IC₅₀ = 0.301 μM) and *Na_V1.5* (IC₅₀ = 4.20 μM), showing >20-fold and >950-fold selectivity respectively .

HY-P1218A

Phrixotoxin 3 TFA	Sodium Channel	Neurological Disease
Phrixotoxin 3 TFA is a potent blocker of voltage-gated sodium channels, with IC₅₀s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and *NaV1.5, respectively. Phrixotoxin 3 TFA modulates voltage-gated sodium channels* with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current .

HY-15736

Sodium Channel inhibitor 1	Sodium Channel	Neurological Disease
Sodium Channel inhibitor 1 is a state-dependent voltage-gated Na_V1.7 inhibitor with an IC₅₀ of 0.087 μM. Sodium Channel inhibitor 1 can be used for research of pain .

HY-P5811

Ceratotoxin-1 CcoTx1; β-TRTX-cm1a	Sodium Channel	Neurological Disease
Ceratotoxin-1 (CcoTx1), a peptide toxin, is an voltage-gated sodium channel subtypes inhibitor. Ceratotoxin-1 inhibits Nav1.1/β1, Nav1.2/β1, Nav1.4/β1, and *Nav1.5/β1* with IC₅₀ of 523 nM, 3 nM, 888 nM, and 323 nM, respectively. Ceratotoxin-1 also inhibits Nav1.8/β1 .

HY-W699451

MTSET chloride	Sodium Channel	Others
MTSET chloride is a membrane-impermeable, thiol-specific reagent that primarily acts as an inhibitor of the *Nav1.5* sodium channel. MTSET chloride reduces the peak sodium current amplitude of most mutant Nav1.5 channels, induces a hyperpolarizing shift in steady-state inactivation, and slows the recovery process, but shows no activity against wild-type and non-inactivating Nav1.5 channel mutants. MTSET chloride reacts covalently with T336C mutant P2X2 receptors, partially reversibly blocks ATP-induced cation currents, and exerts no effect on wild-type P2X2 receptors .

HY-17429R

Flecainide acetate (Standard) R-818 (Standard)	Reference Standards Sodium Channel	Cardiovascular Disease
Flecainide (acetate) (Standard) is the analytical standard of Flecainide (acetate). This product is intended for research and analytical applications. Flecainide acetate (R-818) is a class 1C antiarrhythmic agent especially used for the management of supraventricular arrhythmia; works by blocking the Nav1.5 sodium channel in the heart, causing prolongation of the cardiac action potential.

HY-178344

Multi-target kinase-IN-6	Calcium Channel Sodium Channel	Cardiovascular Disease
Multi-target kinase-IN-6 is a Multiple target kinase inhibitor. Multi-target kinase-IN-6 can inhibit cardiac RyR2- and NaV1.5-channels but stimulate SERCA2a pump activity. Multi-target kinase-IN-6 can be used for the research of cardiovascular disease, such as heart failure .

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-HT_2A 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 K_B of 0.18 nM for Gq dissociation) at the 5-HT_2A receptor. 2-Bromo-LSD D-Tartrate exhibits partial agonist activity at multiple aminergic GPCRs, including 5-HT_2A. 2-Bromo-LSD D-Tartrate lacks 5-HT_2B 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 .

Cat. No.	Nombre del producto

HY-L923

Ion Channel Lead-like Compound Library	9000 compounds
Ion channels are key proteins on the cell membrane that regulate the flow of ions across membranes. They participate in nearly all physiological processes, including nerve conduction, muscle contraction, heart rhythm, and pain perception. Abnormalities in their function can lead to various serious diseases such as arrhythmia, epilepsy, hypertension, neuropathic pain, and cancer. Therefore, ion channels are highly valuable drug targets—over 15% of approved drugs target ion channels currently, demonstrating their irreplaceable therapeutic value in cardiovascular, neurological, and analgesic fields. MCE has collected a library of over 5,000 reported ion channel-related bioactive compounds targeting major sites such as Na+ channels, K+ channels, Ca2+ channels, GABA receptors, iGluRs, and others. Using AI models, these compounds are characterized through both 2D representations (molecular fingerprints, pharmacophores) and 3D representations (3D conformation) to screen for a collection of lead-like compounds highly similar to known active molecules. Additionally, an hERG channel prediction algorithm integrating XGB and ISE mapping strategy is employed to assess and exclude potential cardiotoxicity in the library.. This step significantly reduces safety risks in subsequent screenings, particularly for ion channel drug development related to cardiovascular systems (e.g., Nav1.5, Cav1.2), effectively minimizing failures due to hERG inhibition and serving as a valuable tool for ion channel drug screening.

Ion Channel Lead-like Compound Library

9000 compounds

Ion channels are key proteins on the cell membrane that regulate the flow of ions across membranes. They participate in nearly all physiological processes, including nerve conduction, muscle contraction, heart rhythm, and pain perception. Abnormalities in their function can lead to various serious diseases such as arrhythmia, epilepsy, hypertension, neuropathic pain, and cancer. Therefore, ion channels are highly valuable drug targets—over 15% of approved drugs target ion channels currently, demonstrating their irreplaceable therapeutic value in cardiovascular, neurological, and analgesic fields.

MCE has collected a library of over 5,000 reported ion channel-related bioactive compounds targeting major sites such as Na+ channels, K+ channels, Ca2+ channels, GABA receptors, iGluRs, and others. Using AI models, these compounds are characterized through both 2D representations (molecular fingerprints, pharmacophores) and 3D representations (3D conformation) to screen for a collection of lead-like compounds highly similar to known active molecules. Additionally, an hERG channel prediction algorithm integrating XGB and ISE mapping strategy is employed to assess and exclude potential cardiotoxicity in the library.. This step significantly reduces safety risks in subsequent screenings, particularly for ion channel drug development related to cardiovascular systems (e.g., Nav1.5, Cav1.2), effectively minimizing failures due to hERG inhibition and serving as a valuable tool for ion channel drug screening.

Cat. No.	Nombre del producto	Type

HY-W699451

MTSET chloride	Fluorescent Dyes
MTSET chloride is a membrane-impermeable, thiol-specific reagent that primarily acts as an inhibitor of the *Nav1.5* sodium channel. MTSET chloride reduces the peak sodium current amplitude of most mutant Nav1.5 channels, induces a hyperpolarizing shift in steady-state inactivation, and slows the recovery process, but shows no activity against wild-type and non-inactivating Nav1.5 channel mutants. MTSET chloride reacts covalently with T336C mutant P2X2 receptors, partially reversibly blocks ATP-induced cation currents, and exerts no effect on wild-type P2X2 receptors .

MTSET chloride

Fluorescent Dyes

MTSET chloride is a membrane-impermeable, thiol-specific reagent that primarily acts as an inhibitor of the Nav1.5 sodium channel. MTSET chloride reduces the peak sodium current amplitude of most mutant Nav1.5 channels, induces a hyperpolarizing shift in steady-state inactivation, and slows the recovery process, but shows no activity against wild-type and non-inactivating Nav1.5 channel mutants. MTSET chloride reacts covalently with T336C mutant P2X2 receptors, partially reversibly blocks ATP-induced cation currents, and exerts no effect on wild-type P2X2 receptors .

Cat. No.	Nombre del producto	Target	Research Area

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 .

HY-P1218B

Phrixotoxin 3-NH2 TFA	Sodium Channel	Neurological Disease
Phrixotoxin 3-NH2 TFA is a derivative of Phrixotoxin 3 TFA (HY-P1218A). Phrixotoxin 3 TFA is a potent blocker of voltage-gated sodium channels, with IC₅₀s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and *NaV1.5, respectively. Phrixotoxin 3 TFA modulates voltage-gated sodium channels* with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current .

HY-P1218

Phrixotoxin 3	Sodium Channel	Neurological Disease
Phrixotoxin 3 is a potent blocker of voltage-gated sodium channels, with IC₅₀s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and *NaV1.5, respectively. Phrixotoxin 3 modulates voltage-gated sodium channels* with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current .

HY-P1219

Jingzhaotoxin-III β-TRTX-Cj1α	Sodium Channel	Neurological Disease
Jingzhaotoxin-III is a potent and selective blocker of **Nav1.5 channels, with an IC₅₀** of 348 nM, and shows no effect on other sodium channel isoforms. Jingzhaotoxin-III can selectively inhibit the activation of cardiac sodium channel but not neuronal subtypes, and hopefully represents an important ligand for discriminating cardiac VGSC subtype .

HY-P1681A

GpTx-1 TFA	Sodium Channel	Neurological Disease
GpTx-1 TFA is a peptide-based Na_V1.7 sodium channel antagonist isolated from the venom of the Chilean spider Grammostola porter. GpTx-1 TFA demonstrates potent inhibitory activity against the Na_V1.7 channel with an IC₅₀ value of 10 nM, while exhibiting excellent selectivity for Na_V1.4 (IC₅₀ = 0.301 μM) and *Na_V1.5* (IC₅₀ = 4.20 μM), showing >20-fold and >950-fold selectivity respectively .

HY-P1681

GpTx-1	Sodium Channel	Neurological Disease
GpTx-1 is a peptide-based Na_V1.7 sodium channel antagonist isolated from the venom of the Chilean spider Grammostola porter. GpTx-1 demonstrates potent inhibitory activity against the Na_V1.7 channel with an IC₅₀ value of 10 nM, while exhibiting excellent selectivity for Na_V1.4 (IC₅₀ = 0.301 μM) and *Na_V1.5* (IC₅₀ = 4.20 μM), showing >20-fold and >950-fold selectivity respectively .

HY-P1218A

Phrixotoxin 3 TFA	Sodium Channel	Neurological Disease
Phrixotoxin 3 TFA is a potent blocker of voltage-gated sodium channels, with IC₅₀s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and *NaV1.5, respectively. Phrixotoxin 3 TFA modulates voltage-gated sodium channels* with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current .

HY-P5811

Ceratotoxin-1 CcoTx1; β-TRTX-cm1a	Sodium Channel	Neurological Disease
Ceratotoxin-1 (CcoTx1), a peptide toxin, is an voltage-gated sodium channel subtypes inhibitor. Ceratotoxin-1 inhibits Nav1.1/β1, Nav1.2/β1, Nav1.4/β1, and *Nav1.5/β1* with IC₅₀ of 523 nM, 3 nM, 888 nM, and 323 nM, respectively. Ceratotoxin-1 also inhibits Nav1.8/β1 .

Cat. No.	Nombre del producto	Chemical Structure

HY-W052508S

Norquetiapine-d8
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-HT_1A (K_i = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (K_i = 237 nM), 5-HT_2C(K_i = 107 nM), and 5-HT₇ (K_i = 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

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-HT_1A (K_i = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (K_i = 237 nM), 5-HT_2C(K_i = 107 nM), and 5-HT₇ (K_i = 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 .

HY-17429S

Flecainide-d4 acetate
Flecainide-d₄ (acetate) is the deuterium labeled Flecainide acetate. Flecainide acetate (R-818) is a class 1C antiarrhythmic agent especially used for the management of supraventricular arrhythmia; works by blocking the Nav1.5 sodium channel in the heart, causing prolongation of the cardiac action potential .

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