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Pathways Recommended: Membrane Transporter/Ion Channel
Results for "

Cation channels

" in MedChemExpress (MCE) Product Catalog:

41

Inhibitors & Agonists

1

Screening Libraries

9

Peptides

6

Natural
Products

3

Isotope-Labeled Compounds

1

Oligonucleotides

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-122605
    TRPM4-IN-1

    CBA

    		 TRP Channel Cardiovascular Disease Cancer
    TRPM4-IN-1 (CBA) is a potent and selective inhibitor of the cation channel TRPM4, with an IC50 of 1.5 μM. TRPM4-IN-1 can be used for the research of cardiac diseases and prostate cancer .
    TRPM4-IN-1
  • HY-131897
    1-Stearoyl-2-arachidonoyl-sn-glycerol
    1 Publications Verification

    		 PKC TRP Channel Endogenous Metabolite Neurological Disease
    1-Stearoyl-2-arachidonoyl-sn-glycerol is a diacylglycerol (DAG) containing polyunsaturated fatty acids. 1-Stearoyl-2-arachidonoyl-sn-glycerol can activate PKC. 1-Stearoyl-2-arachidonoyl-sn-glycerol also can augment nonselective cation channel (NSCC) activity .
    1-Stearoyl-2-arachidonoyl-sn-glycerol
  • HY-107535
    AS1269574

    		GPR119 TRP Channel Metabolic Disease
    AS1269574 is a potent, orally available GPR119 agonist, with an EC50 of 2.5 μM in HEK293 cells expressing human GPR119. AS1269574 activates TRPA1 cation channels to stimulate glucagon-like peptide-1 (GLP-1) secretion. AS1269574 specifically induces glucose-dependent insulin secretion from pancreatic β-cells only under high-glucose conditions. AS1269574 has the potential for the research of type 2 diabetes .
    AS1269574
  • HY-P0163
    Gramicidin
    4 Publications Verification

    		 Bacterial Antibiotic Infection
    Gramicidin is an antimicrobial peptide assembling as channels in membranes and increasing their permeability towards cations.
    Gramicidin
  • HY-N1378
    (E)-Cardamonin
    1 Publications Verification

    (E)-Cardamomin; (E)-Alpinetin chalcone

    		 TRP Channel Apoptosis Neurological Disease Cancer
    (E)-Cardamonin ((E)-Cardamomin) is a novel antagonist of hTRPA1 cation channel with an IC50 of 454 nM.
    (E)-Cardamonin
  • HY-B1793
    Tetraethylammonium chloride
    4 Publications Verification

    		 Potassium Channel Neurological Disease Cancer
    Tetraethylammonium chloride is a non-selective potassium channel blocker. Tetraethylammonium chloride is a good substrate for organic cation transporter (OCTN1). Tetraethylammonium chloride antitumor properties .
    Tetraethylammonium chloride
  • HY-B1221
    Flufenamic acid
    5+ Cited Publications

    		 COX AMPK Potassium Channel Chloride Channel Calcium Channel Parasite Inflammation/Immunology
    Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K + channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
    Flufenamic acid
  • HY-107756
    LOE 908 hydrochloride

    		Calcium Channel Neurological Disease
    LOE 908 hydrochloride is a non-selective cation channel (NSCC) inhibitor .
    LOE 908 hydrochloride
  • HY-134268
    8-Br-7-CH-ADPR

    8-Bromo-7-deazaadenosine-5'-O-diphosphoribose

    		 TRP Channel Cardiovascular Disease Neurological Disease Metabolic Disease
    8-Br-7-CH-ADPR (8-Bromo-7-deazaadenosine-5'-O-diphosphoribose) is a specific TRPM2 antagonist that inhibits TRPM2 activation by binding to the NUDT9 homology domain of the TRPM2 channel, thereby controlling the influx of cations through the cell membrane channel. 8-Br-7-CH-ADPR can be used to study the role of TRPM2 in pathological processes such as cell death, neurodegenerative diseases, myocardial infarction, and diabetes .
    8-Br-7-CH-ADPR
  • HY-137639
    Sp-8-Br-cGMPS

    		HCN Channel Neurological Disease
    Sp-8-Br-cGMPS is an analog of cGMP. Sp-8-Br-cGMPS is an agonist for cGMP-gated cation channels (CNG channels), with an EC50 of 106.5 μM. Sp-8-Br-cGMPS induces the currents, without the ability to stabilize the channel open state as a full agonist .
    Sp-8-Br-cGMPS
  • HY-N1378R
    (E)-Cardamonin (Standard)

    		TRP Channel Apoptosis Neurological Disease Cancer
    (E)-Cardamonin (Standard) is the analytical standard of (E)-Cardamonin. This product is intended for research and analytical applications. (E)-Cardamonin ((E)-Cardamomin) is a novel antagonist of hTRPA1 cation channel with an IC50 of 454 nM.
    (E)-Cardamonin (Standard)
  • HY-B1221R
    Flufenamic acid (Standard)

    		COX AMPK Potassium Channel Chloride Channel Calcium Channel Parasite Inflammation/Immunology
    Flufenamic acid (Standard) is the analytical standard of Flufenamic acid. This product is intended for research and analytical applications. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K + channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
    Flufenamic acid (Standard)
  • HY-B1221S1
    Flufenamic acid-13C6

    		Isotope-Labeled Compounds COX AMPK Potassium Channel Chloride Channel Calcium Channel Parasite Inflammation/Immunology
    Flufenamic acid- 13C6 is the 13C6 labeled Flufenamic acid. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
    Flufenamic acid-13C6
  • HY-B1221S
    Flufenamic acid-d4

    		Isotope-Labeled Compounds COX AMPK Potassium Channel Chloride Channel Calcium Channel Parasite Inflammation/Immunology
    Flufenamic acid-d4 is deuterium labeled Flufenamic acid. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
    Flufenamic acid-d4
  • HY-P2324
    Gramicidin A
    1 Publications Verification

    		 Bacterial HIF/HIF Prolyl-Hydroxylase Antibiotic Infection Cancer
    Gramicidin A is a peptide component of gramicidin, an antibiotic mixture originally isolated from B. brevis. Gramicidin A is a highly hydrophobic channel-forming ionophore that forms channels in model membranes that are permeable to monovalent cations. Gramicidin A induces degradation of hypoxia inducible factor 1 α (HIF-1α) .
    Gramicidin A
  • HY-P1410
    GsMTx4
    Maximum Cited Publications
    58 Publications Verification

    		 TRP Channel Piezo Channel Cardiovascular Disease Neurological Disease Inflammation/Immunology
    GsMTx4 is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology .
    GsMTx4
  • HY-116478
    L-3373

    		Potassium Channel Others
    L-3373 is a voltage-dependent potassium channel inhibitor with activity that reduces the effective refractory period and the dispersion of monophasic action potential duration, while significantly reducing susceptibility to ventricular fibrillation in a cat model of left ventricular hypertrophy.
    L-3373
  • HY-P2324A
    Gramicidin A TFA

    		Antibiotic Bacterial Infection
    Gramicidin A (TFA) is a peptide component of gramicidin, an antibiotic mixture originally isolated from B. brevis. Gramicidin A (TFA) is a highly hydrophobic channel-forming ionophore that forms channels in model membranes that are permeable to monovalent cations. Gramicidin A (TFA) induces degradation of hypoxia inducible factor 1 α (HIF-1α) .
    Gramicidin A TFA
  • HY-P1410A
    GsMTx4 TFA
    Maximum Cited Publications
    58 Publications Verification

    		 TRP Channel Piezo Channel Cardiovascular Disease Neurological Disease Inflammation/Immunology
    GsMTx4 TFA is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 TFA also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 TFA is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology .
    GsMTx4 TFA
  • HY-126763
    ATI22-107

    		Phosphodiesterase (PDE) Calcium Channel Others
    ATI22-107 is a dual-pharmacophore compound designed to simultaneously inhibit cardiac phosphodiesterase (PDE-III) and L-type calcium channels (LTCC), with activity that has specific effects on calcium cycling and contractility in cat ventricular myocytes and trabeculae.
    ATI22-107
  • HY-75161
    (-)-Menthol
    1 Publications Verification

    		 TRP Channel Endogenous Metabolite Cancer
    (-)-Menthol is a key component of peppermint oil that binds and activates transient receptor potential melastatin 8 (TRPM8), a Ca 2+-permeable nonselective cation channel, to increase [Ca 2+]i . Antitumor activity .
    (-)-Menthol
  • HY-P1077
    CALP1
    1 Publications Verification

    		 mGluR Phosphodiesterase (PDE) Apoptosis Calmodulin Inflammation/Immunology
    CALP1 is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca 2+-binding site. CALP1 blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 activates CaM-dependent phosphodiesterase activity .
    CALP1
  • HY-P1077A
    CALP1 TFA
    1 Publications Verification

    		 mGluR Phosphodiesterase (PDE) Apoptosis Calmodulin Inflammation/Immunology
    CALP1 TFA is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca 2+-binding site. CALP1 TFA blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 TFA blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 TFA activates CaM-dependent phosphodiesterase activity .
    CALP1 TFA
  • HY-100973A
    Adenosine 5′-diphosphoribose sodium
    4 Publications Verification

    ADP ribose sodium

    		 TRP Channel Autophagy Metabolic Disease Endocrinology Cancer
    Adenosine 5′-diphosphoribose sodium (ADP ribose sodium) is a nicotinamide adenine nucleotide (NAD +) metabolite. Adenosine 5′-diphosphoribose sodium is the most potent and primary intracellular Ca 2+-permeable cation TRPM2 channel activator. Adenosine 5′-diphosphoribose sodium also can enhance autophagy .
    Adenosine 5′-diphosphoribose sodium
  • HY-152182
    ML-SA5
    1 Publications Verification

    		 TRP Channel Cancer
    ML-SA5 is a potent TRPML1 cation channel agonist that activates the entire endosomal TRPML1 (ML1) current in DMD myocytes with an EC50 of 285 nM and is more potent than ML-SA1. ML-SA5 has anticancer activity and can inhibit tumour growth .
    ML-SA5
  • HY-75161R
    (-)-Menthol (Standard)

    		TRP Channel Endogenous Metabolite Cancer
    (-)-Menthol (Standard) is the analytical standard of (-)-Menthol. This product is intended for research and analytical applications. (-)-Menthol is a key component of peppermint oil that binds and activates transient receptor potential melastatin 8 (TRPM8), a Ca2+-permeable nonselective cation channel, to increase [Ca2+]i . Antitumor activity .
    (-)-Menthol (Standard)
  • HY-19960
    BCTC
    4 Publications Verification

    		 TRP Channel Insulin Receptor CGRP Receptor Neurological Disease Metabolic Disease Cancer
    BCTC is an orally active current inhibitor of vanilloid receptor type 1 (VR1). BCTC is a transient receptor potential cation channel subfamily M member 8 (TRPM8) and transient receptor potential vanilloid 1 (TRPV1) antagonist. BCTC is an insulin sensitizer and secretor. BCTC has anticancer and analgesic effects .
    BCTC
  • HY-19976
    RN-1747
    2 Publications Verification

    		 TRP Channel Cardiovascular Disease
    RN-1747 is a selective transient receptor potential cation channel subfamily V member 4 (TRPV4) agonist, with EC50 values are 0.77 μM, 4.0 μM and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4 respectively. RN-1747 also antagonizes TRPM8, with an IC50 of 4 μM .
    RN-1747
  • HY-108460
    A-784168

    		TRP Channel Neurological Disease
    A-784168 is a potent and orally active inhibitor of vanilloid receptor type 1 (TRPV1). Vanilloid receptor type 1 (TRPV1) is a ligand-gated nonselective cation channel that is considered to be an important integrator of various pain stimuli such as endogenous lipids, capsaicin, heat, and low pH. A-784168 has good CNS penetration .
    A-784168
  • HY-148129
    TRPC6-IN-3

    		TRP Channel Cardiovascular Disease
    TRPC6-IN-3 (compound 17) is a potent, orally active transient receptor potential C6 ion channel (TRPC6) inhibitor. TRPC6-IN-3 modulates not only intracellular calcium concentration, but also membrane potential by modulating the flux of cations including calcium and sodium ions. TRPC6-IN-3 can be used in research of respiratory system .
    TRPC6-IN-3
  • HY-149203A
    MQA-P TFA

    		Fluorescent Dye Others
    MQA-P is a multifunctional near-infrared (NIR) fluorescent probe that simultaneously detects ONOO -, viscosity, and polarity within mitochondria. MQA-P exhibits significant response to ONOO -, λem=645 nm; and NIR channel at λem>704 nm Medium is highly sensitive to viscosity/polarity. MQA-P possesses excited-state intramolecular charge transfer (ESICT) properties that are highly sensitive to polarity by designing the N,N-dimethylamino group as the electron donor and the quinoline cation unit as the electron acceptor. MQA-P is used for ferroptosis or cancer diagnosis in vitro and in vivo via dual-channel images .
    MQA-P TFA
  • HY-111527
    PPZ2

    		Calcium Channel Neurological Disease
    PPZ2 is a diacylglycerol (DAG)-activated TRPC3/TRPC6/TRPC7 channel activator with activity in promoting neuronal development and survival. PPZ2 activates recombinant TRPC3/TRPC6/TRPC7 channels in a dose-dependent manner without affecting other TRPC channels. PPZ2 elicits cation currents and calcium ion (Ca(2+)) influx in cultured central neurons. PPZ2 is able to induce BDNF-like neurite outgrowth and neuroprotection, an effect that disappears after TRPC3/TRPC6/TRPC7 knockdown or inhibition. PPZ2 also increases the activation of the calcium-dependent transcription factor cAMP response element binding protein. The effects of PPZ2 suggest that calcium signaling mediated by activation of DAG-activated TRPC channels plays an important role in its neurotrophic effects .
    PPZ2
  • HY-145150
    TRPC5-IN-1

    		TRP Channel Metabolic Disease
    TRPC5-IN-1 (Compound 6j) is a selective TRPC5 inhibitor with 50.5 % Inhibition for TRPC5 at 3 μM. TRPC5-IN-1 can be used for the research of chronic kidney disease (CKD) .
    TRPC5-IN-1
  • HY-131897S
    1-Stearoyl-2-Arachidonoyl-d8-sn-Glycerol

    		Isotope-Labeled Compounds PKC TRP Channel Endogenous Metabolite Neurological Disease
    1-Stearoyl-2-Arachidonoyl-d8-sn-Glycerol is the deuterium labeled 1-Stearoyl-2-arachidonoyl-sn-glycerol. 1-Stearoyl-2-arachidonoyl-sn-glycerol is a diacylglycerol (DAG) containing polyunsaturated fatty acids. 1-Stearoyl-2-arachidonoyl-sn-glycerol can activate PKC. 1-Stearoyl-2-arachidonoyl-sn-glycerol also can augment nonselective cation channel (NSCC) activity[1][2].
    1-Stearoyl-2-Arachidonoyl-d8-sn-Glycerol
  • HY-19408
    Pyr10
    3 Publications Verification

    		 TRP Channel Others
    Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. Pyr10 inhibits Ca 2+ influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC50 of 0.72 μM (IC50 of 13.08 μM for store operated Ca 2+ entry in BRL-2H3 cells). Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels .
    Pyr10
  • HY-P2141
    TRV-120027
    3 Publications Verification

    		 Angiotensin Receptor Arrestin Cardiovascular Disease
    TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ?-arrestins while blocking G-protein signaling . TRV120027?induces?acute?catecholamine?secretion?through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the?acute decompensated heart failure (ADHF) treatment .
    TRV-120027
  • HY-P2141A
    TRV-120027 TFA
    3 Publications Verification

    		 Angiotensin Receptor Arrestin Cardiovascular Disease
    TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ?-arrestins while blocking G-protein signaling . TRV120027?TFA induces?acute?catecholamine?secretion?through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 TFA inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 TFA has the potential for the?acute decompensated heart failure (ADHF) treatment .
    TRV-120027 TFA
  • HY-139192
    Brophenexin
    1 Publications Verification

    NMDAR/TRPM4-IN-2

    		 iGluR TRP Channel ERK Neurological Disease
    Brophenexin (compound 8) is a potent NMDAR/TRPM4 interaction interface inhibitor. Brophenexin shows neuroprotective activity. Brophenexin prevents NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC50 of 2.1 μM. Brophenexin protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss .
    Brophenexin
  • HY-139192A
    Brophenexin free base
    1 Publications Verification

    NMDAR/TRPM4-IN-2 free base

    		 iGluR TRP Channel ERK Neurological Disease
    Brophenexin free base (compound 8) is a potent NMDAR/TRPM4 interaction interface inhibitor. Brophenexin free base shows neuroprotective activity. Brophenexin free base prevents NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC50 of 2.1 μM. Brophenexin free base protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss .
    Brophenexin free base
  • HY-101840
    EIPA
    50+ Cited Publications

    L593754; MH 12-43; Ethylisopropylamiloride

    		 TRP Channel Prostaglandin Receptor Autophagy COX Na+/H+ Exchanger (NHE) Inflammation/Immunology Cancer
    EIPA (L593754) is an orally active TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA also enhances autophagy by inhibiting Na +/H +-exchanger 3 (NHE3). EIPA inhibits macropinocytosis as well. EIPA can be used in the research of inflammation and cancers, such as gastric cancer, colon carcinoma, pancreatic carcinoma .
    EIPA
  • HY-101840A
    EIPA hydrochloride
    50+ Cited Publications

    L593754 hydrochloride; MH 12-43 hydrochloride; Ethylisopropylamiloride hydrochloride

    		 TRP Channel Autophagy COX Prostaglandin Receptor Na+/H+ Exchanger (NHE) Inflammation/Immunology Cancer
    EIPA (L593754) hydrochloride is an orally active TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA hydrochloride also enhances autophagy by inhibiting Na +/H +-exchanger 3 (NHE3). EIPA hydrochloride inhibits macropinocytosis as well. EIPA hydrochloride can be used in the research of inflammation and cancers, such as gastric cancer, colon carcinoma, pancreatic carcinoma .
    EIPA hydrochloride

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