Search Result

Pathways Recommended:	Membrane Transporter/Ion Channel

Results for "

channels isoforms

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Adrenergic Receptor (1) Angiotensin-converting Enzyme (ACE) (1) Apoptosis (2) Bacterial (1) Calcium Channel (3) Cytochrome P450 (2) Deubiquitinase (1) Drug Metabolite (2) Glucocorticoid Receptor (2) HCV Protease (2) iGluR (1) Isotope-Labeled Compounds (1) Opioid Receptor (1) Phosphodiesterase (PDE) (3) Potassium Channel (3) Reactive Oxygen Species (ROS) (1) Sodium Channel (5)
By Research Areas:	Cancer (1) Cardiovascular Disease (4) Endocrinology (1) Infection (3) Inflammation/Immunology (2) Neurological Disease (10)

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-N6778

Paxilline 5+ Cited Publications	Potassium Channel Calcium Channel Reactive Oxygen Species (ROS)	Neurological Disease
Paxilline is an indole alkaloid mycotoxin derived from Penicillium paxilli, which effectively inhibits the BK channel through a channel-blocking mechanism. Paxilline also inhibits sarco/endoplasmic reticulum Ca ²⁺-stimulated ATPase (SERCA), with IC₅₀ values ranging from 5 μM to 50 μM for different SERCA isoforms. Paxilline exhibits significant anticonvulsant and neuroprotective effects, as well as certain antioxidant activity .

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 Na_V1.6/SCN8A inhibitor that can penetrate the blood-brain barrier. Zandatrigine inhibits sodium influx by non-covalently binding to the VSD4 structure of Na_V1.6, 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 Na_V1.1 and Na_V1.2, and has minimal effect on Na_V1.1 expressed by inhibitory interneurons. Zandatrigine can be used to study Na_V1.6-mediated neuroexcitability diseases such as SCN8A-related developmental epileptic encephalopathy (SCN8A-DEE) and adult focal epilepsy .

HY-132184

5,6-Epoxyeicosatrienoic acid 5,6-EET; (±)5,6-EpETrE	Adrenergic Receptor Calcium Channel	Endocrinology
5,6-Epoxyeicosatrienoic acid (5,6-EET; (±)5,6-EpETrE) is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5,6-Epoxyeicosatrienoic acid degrades into 5,6-DiHET and 5,6-δ-lactone, which can be converted to 5,6-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5,6-Epoxyeicosatrienoic acid has been implicated in the mobilization of calcium and hormone secretion. 5,6-Epoxyeicosatrienoic acid is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhibits isoforms Cav3.1, Cav3.2 (IC₅₀=0.54 μM), and Cav3. and decreases nifedipine-resistant phenylephrine-induced vasoconstriction in isolated mouse mesenteric arteries via Cav3.2 blockade when used at a concentration of 3 μM. In addition, it is a substrate of COX-1 and COX-2.

HY-135746

OR-1896 2 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-W074537

P7-2104	Phosphodiesterase (PDE)	Neurological Disease
P7-2104 is a selective CNS-penetrant PDE7A inhibitor with an IC₅₀ of of 31 nM. P7-2104 exhibits selectivity over hERG channels and most CYP450 isoforms. P7-2104 can be used for PDE7-targeted PET neuroimaging, and for the research of neurodegenerative disorders .

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-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-12946

BI 653048	Glucocorticoid Receptor Cytochrome P450 HCV Protease	Infection Inflammation/Immunology
BI 653048, a chemical probe, 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 (Compound 103) is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus .

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-108043

AZD-2327	Opioid Receptor	Neurological Disease
AZD-2327 is a potent and selective δ-opioid receptor agonist. AZD-2327 binds to the human opioid receptor (K_i of 0.49 and 0.75 nM and EC₅₀ of 24 and 9.2 nM at the C27 and F27 isoforms, respectively). AZD-2327 shows selectivity of >1000-fold over the human μ- and κ-opioid receptor subtypes as well as >130 other receptors and channels. AZD-2327 exhibits antidepressant and anxiolytic activities and can be used for the research of neurological disease .

HY-12946A

BI 653048 phosphate	Glucocorticoid Receptor Cytochrome P450 HCV Protease	Infection Inflammation/Immunology
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-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-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-130309

(±)8(9)-EpETE (±)8,9-EEQ; (±)8,9-epoxy Eicosatetraenoic acid	Angiotensin-converting Enzyme (ACE)	Cardiovascular Disease
Eicosapentaenoic acid (EPA) is converted to epoxyeicosatetraenoic acids (EpETEs) by several cytochrome P450 isoforms. The major product of this epoxygenase pathway, (±)17(18)-EpETE, relaxes vascular and airway smooth muscle by activating large conductance Ca ²⁺-activated K ⁺ (BKCa) channels by directly interacting with BKα channel subunits. (±)8(9)-EpETE is an epoxygenase pathway product produced from EPA by CYP450 both in vitro and in vivo.

HY-118030

RQ-00311651	Calcium Channel	Neurological Disease
RQ-00311651 is a T-type calcium channel blocker that specifically targets the Cav3.2 isoform with a role in neuropathic and visceral pain. RQ-00311651 significantly inhibits T currents in HEK293 cells expressing human Cav3.1 or Cav3.2. RQ-00311651 also inhibited high potassium-induced calcium signaling. RQ-00311651 also inhibits antiallergic properties in rats and mice with neuropathic pain induced by spinal nerve injury or Paclitaxel (HY-B0015). Oral and intraperitoneal injection (10-20 mg/kg) inhibits Cerulein (HY-A0190)-induced acute pancreatitis and cyclophosphamide-induced cystitis in mice .

HY-135746S

OR-1896-d3	Isotope-Labeled Compounds Phosphodiesterase (PDE) Apoptosis Potassium Channel Drug Metabolite	Cardiovascular Disease
OR-1896-d₃ is the deuterium labeled OR-1896 (HY-135746). 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 Ca2+-sensitizing effect. OR-1896 mitigates cardiomyocyte apoptosis, cardiac remodeling and myocardial inflammation .

HY-183606

Mycobacterium tuberculosis-IN-9	Bacterial	Infection
Mycobacterium tuberculosis-IN-9 is an orally active Mycobacterium tuberculosis BioA inhibitor with a K_i value of 0.2 nM. Mycobacterium tuberculosis-IN-9 targets the biotin biosynthesis pathway. Mycobacterium tuberculosis-IN-9 inhibits the growth of Mycobacterium tuberculosis in mouse models and is effective against both drug-sensitive and drug-resistant strains. Mycobacterium tuberculosis-IN-9 can be used for the research of tuberculosis .

HY-183689

OAT-4828	Deubiquitinase	Cancer
OAT-4828 is an orally active ubiquitin-specific protease 7 (USP7) inhibitor with an IC₅₀ of 32 nM. OAT-4828 induces antileukemic activity in B-cell-derived non-Hodgkin's lymphoma models via inhibition of USP7. OAT-4828 is applicable to research related to chronic lymphocytic leukemia .

Cat. No.	Product Name

HY-L099

Targeted Diversity Library	2,300 compounds
MCE Targeted Diversity Library contains 2,300 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

2,300 compounds

MCE Targeted Diversity Library contains 2,300 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