Search Result

Isoforms Recommended:	Na_v1.5

Results for "

NaV1.5

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Na+/Ca2+ Exchanger (2) Sodium Channel (30) 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) Potassium Channel (3) Reference Standards (1) Serotonin Transporter (2) Small Interfering RNA (siRNA) (3) TRP Channel (4)
By Research Areas:	Cancer (5) Cardiovascular Disease (8) Inflammation/Immunology (4) Neurological Disease (27)
Oligonucleotides:	Rat Pre-designed siRNA Sets (1) Mouse Pre-designed siRNA Sets (1) Human Pre-designed siRNA Sets (1) siRNAs (3)

Inhibitors & Agonists

Screening Libraries

Peptides

Isotope-Labeled Compounds

Oligonucleotides

Targets Recommended: Sodium Channel NKCC Na+/HCO3- Cotransporter Na+/Ca2+ Exchanger Na+/K+ ATPase Na+/H+ Exchanger (NHE)

Cat. No.	Product Name	Target	Research Areas	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-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-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-126429

Nav1.1 activator 1	Sodium Channel	Neurological Disease
Nav1.1 activator 1 (compound 4), a highly potent *Na_v1.1* activator with BBB penetration, increases decay time constant τ of Na_v1.1 currents at 0.03 μM along with significant selectivity against Na_v1.2, Na_v1.5, and Na_v1.6 .

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-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-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-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-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-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-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-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-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-RS12541

SCN5A Human Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
SCN5A Human Pre-designed siRNA Set A contains three designed siRNAs for SCN5A gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

SCN5A Human Pre-designed siRNA Set A SCN5A Human Pre-designed siRNA Set A

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-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-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-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-181063

Nav1.5-IN-1	Sodium Channel	Cardiovascular Disease
Nav1.5-IN-1 is a selective *Nav1.5* inhibitor with an IC₅₀ of 1.38 μM. Nav1.5-IN-1 shows selectivity over other Nav subtypes. Nav1.5-IN-1 reduces cardiac conduction in isolated rat hearts.Nav1.5-IN-1 can be used for the research of arrhythmias .

HY-118048

NAV 26	Sodium Channel	Neurological Disease
NAV 26 (Compound 26) is a selective *Na_V1.7* inhibitor with an IC₅₀ of 0.37 μM. NAV 26 is applicable for pain-related research .

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-P5872

Jingzhaotoxin XI JZTX-XI	Sodium Channel	Neurological Disease
Jingzhaotoxin XI (JZTX-XI) is a sodium conductance inhibitor with an IC₅₀ of 124 nM. Jingzhaotoxin XI slows the fast inactivation (EC₅₀=1.18±0.2 μM) of Na_v1.5 expressed in Chinese hamster ovary (CHO-K1) cells .

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-P5801

Phlo1a μ-TrTx-Phlo1a	Sodium Channel	Neurological Disease
Phlo1a (μ-TrTx-Phlo1a) is a peptide toxin contains 35-amino acid residues. Phlo1b is a selective *Nav1.7* inhibitor. Phlo1a has a weak inhibitory effect on Nav1.2 and Nav1.5 .

HY-P5800

Phlo1b μ-TrTx-Phlo1b	Sodium Channel	Neurological Disease
Phlo1b (μ-TrTx-Phlo1b) is a peptide toxin contains 35-amino acid residues. Phlo1b is a selective *Nav1.7* inhibitor. Phlo1b has a weak inhibitory effect on Nav1.2 and Nav1.5 .

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 .

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-RS12542

Scn5a Mouse Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
Scn5a Mouse Pre-designed siRNA Set A contains three designed siRNAs for Scn5a gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Scn5a Mouse Pre-designed siRNA Set A Scn5a Mouse Pre-designed siRNA Set A

HY-RS12543

Scn5a Rat Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
Scn5a Rat Pre-designed siRNA Set A contains three designed siRNAs for Scn5a gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

Scn5a Rat Pre-designed siRNA Set A Scn5a Rat Pre-designed siRNA Set A

HY-182334

azo-Q2a	Sodium Channel	Cardiovascular Disease
azo-Q2a is a photoswitchable *Na_V1.5* inhibitor. azo-Q2a exists as the trans isomer with low activity in the dark or under 480 nm illumination, and exists as the cis isomer with higher inhibitory potency under 365 nm illumination. azo-Q2a reduces the heart rate of living zebrafish larvae in a light-dependent manner. azo-Q2a can be used for the study of arrhythmias .

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 .

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.	Product Name

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.	Product Name	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-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-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-P5872

Jingzhaotoxin XI JZTX-XI	Sodium Channel	Neurological Disease
Jingzhaotoxin XI (JZTX-XI) is a sodium conductance inhibitor with an IC₅₀ of 124 nM. Jingzhaotoxin XI slows the fast inactivation (EC₅₀=1.18±0.2 μM) of Na_v1.5 expressed in Chinese hamster ovary (CHO-K1) cells .

HY-P5801

Phlo1a μ-TrTx-Phlo1a	Sodium Channel	Neurological Disease
Phlo1a (μ-TrTx-Phlo1a) is a peptide toxin contains 35-amino acid residues. Phlo1b is a selective *Nav1.7* inhibitor. Phlo1a has a weak inhibitory effect on Nav1.2 and Nav1.5 .

HY-P5800

Phlo1b μ-TrTx-Phlo1b	Sodium Channel	Neurological Disease
Phlo1b (μ-TrTx-Phlo1b) is a peptide toxin contains 35-amino acid residues. Phlo1b is a selective *Nav1.7* inhibitor. Phlo1b has a weak inhibitory effect on Nav1.2 and Nav1.5 .

Cat. No.	Product Name	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 .

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 .

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent: