channels isoforms

Pathways Recommended:	Membrane Transporter/Ion Channel

By Targets:	Calcium Channel (1) Potassium Channel (2) Sodium Channel (4) Apoptosis (1) Drug Metabolite (1) iGluR (1) Phosphodiesterase (PDE) (1)
By Research Areas:	Cardiovascular Disease (2) Neurological Disease (6)

Targets Recommended: Chloride Channel Calcium Channel HCN Channel CRAC Channel TRP Channel Sodium Channel Potassium Channel Piezo Channel

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-P5174

MitTx	Sodium Channel	Neurological Disease
MitTx is a complex formed by MitTx-α and MitTx-β. MitTx is an ASIC1 channel activator with EC₅₀ values of 9.4 and 23 nM for ASIC1a and ASIC1b isoforms, respectively. MitTx is highly selective for ASIC1 isoforms at neutral pH. Under acidic conditions, MitTx greatly enhances proton-evoked ASIC2a channel activation .

HY-N6778

Paxilline 5 Publications Verification	Potassium Channel Calcium Channel	Neurological Disease
Paxilline is an indole alkaloid mycotoxin from Penicillium paxilli, acts as a potent BK channels inhibitor by an almost exclusively closed-channel block mechanism. Paxilline also inhibits the sarco/endoplasmic reticulum Ca ²⁺ ATPase (SERCA) with IC₅₀s between 5 μM and 50 μM for differing isoforms. Paxilline possesses significant anticonvulsant activity .

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-P5771

Jingzhaotoxin-IX	Sodium Channel	Neurological Disease
Jingzhaotoxin-IX, a C-terminally amidated peptide composed of 35 amino acid residues, is a neurotoxin. Jingzhaotoxin-IX inhibits voltage-gated sodium channels (both tetrodotoxin-resistant and tetrodotoxin-sensitive isoforms) and Kv2.1 channel. Jingzhaotoxin-IX has no effect on delayed rectifier potassium channel Kv1.1, 1.2 and 1.3 .

HY-123825

GX-674	Sodium Channel	Cardiovascular Disease Neurological Disease
GX-674 is a potent, state-dependent, isoform-selective *voltage-gated sodium channel* 1.7 (Nav1.7) antagonist with an IC₅₀** of 0.1 nM at -40 mV .

HY-124906

JAMI1001A	iGluR	Neurological Disease
JAMI1001A is a positive allosteric modulator of AMPA receptor. JAMI1001A efficaciously modulates AMPA receptor deactivation and desensitization of both flip and flop receptor isoforms .

HY-135746

OR-1896 1 Publications Verification	Potassium Channel Phosphodiesterase (PDE) Drug Metabolite Apoptosis	Cardiovascular Disease
OR-1896 is an active long-lived metabolite of Levosimendan. OR-1896 is a highly selective phosphodiesterase (PDE) III isoform inhibitor and a powerful vasodilator. OR-1896 can open ATP-sensitive K ⁺ channels and has Ca ²⁺-sensitizing effect. OR-1896 mitigates cardiomyocyte apoptosis, cardiac remodeling and myocardial inflammation .

HY-12946A

BI 653048 phosphate
BI 653048 phosphate is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC₅₀ value of 55 nM . BI 653048 phosphate inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC₅₀>30 μM) . BI 653048 phosphate is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus .

HY-12946

BI 653048
BI 653048 is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC₅₀ value of 55 nM . BI 653048 inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC₅₀>30 μM) . BI 653048 is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus .

Cat. No.	Product Name

HY-L099

Targeted Diversity Library	2317 compounds
MCE Targeted Diversity Library contains 2317 compounds, covering more than 1000 targets and isoforms, such as GPCRs, Ion channel, variety of kinases, etc. 1-3 compounds with high potency and selectivity were carefully selected for each target and isoform. The bioactivity information of each compound has been clearly reported in the literatures. This library is a concise collection of small molecule compounds with comprehensive target coverage, which can be used for phenotypic screening at low cost.

Targeted Diversity Library

2317 compounds

MCE Targeted Diversity Library contains 2317 compounds, covering more than 1000 targets and isoforms, such as GPCRs, Ion channel, variety of kinases, etc. 1-3 compounds with high potency and selectivity were carefully selected for each target and isoform. The bioactivity information of each compound has been clearly reported in the literatures. This library is a concise collection of small molecule compounds with comprehensive target coverage, which can be used for phenotypic screening at low cost.

Cat. No.	Product Name	Target	Research Area

HY-P5174

MitTx	Sodium Channel	Neurological Disease
MitTx is a complex formed by MitTx-α and MitTx-β. MitTx is an ASIC1 channel activator with EC₅₀ values of 9.4 and 23 nM for ASIC1a and ASIC1b isoforms, respectively. MitTx is highly selective for ASIC1 isoforms at neutral pH. Under acidic conditions, MitTx greatly enhances proton-evoked ASIC2a channel activation .

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-P5771

Jingzhaotoxin-IX	Sodium Channel	Neurological Disease
Jingzhaotoxin-IX, a C-terminally amidated peptide composed of 35 amino acid residues, is a neurotoxin. Jingzhaotoxin-IX inhibits voltage-gated sodium channels (both tetrodotoxin-resistant and tetrodotoxin-sensitive isoforms) and Kv2.1 channel. Jingzhaotoxin-IX has no effect on delayed rectifier potassium channel Kv1.1, 1.2 and 1.3 .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N6778

Paxilline 5 Publications Verification	Alkaloids Structural Classification other families Microorganisms Neurological Disease Classification of Application Fields Terpenoids Source classification Diterpenoids Plants Disease Research Fields Indole Alkaloids	Potassium Channel Calcium Channel
Paxilline is an indole alkaloid mycotoxin from Penicillium paxilli, acts as a potent BK channels inhibitor by an almost exclusively closed-channel block mechanism. Paxilline also inhibits the sarco/endoplasmic reticulum Ca ²⁺ ATPase (SERCA) with IC₅₀s between 5 μM and 50 μM for differing isoforms. Paxilline possesses significant anticonvulsant activity .

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社
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Screening Libraries

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