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Results for "

open-channel block

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (5) Caspase (5) Drug Derivative (1) GABA Receptor (1) Histamine Receptor (3) iGluR (4) Isotope-Labeled Compounds (2) Na+/Ca2+ Exchanger (3) P-glycoprotein (2) PARP (2) Potassium Channel (8) Reference Standards (1)
By Research Areas:	Cancer (4) Cardiovascular Disease (3) Endocrinology (3) Infection (1) Inflammation/Immunology (3) Neurological Disease (9)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B1193

Terfenadine 4 Publications Verification (±)-Terfenadine; MDL-991	Potassium Channel Histamine Receptor Na+/Ca2+ Exchanger Caspase Apoptosis	Inflammation/Immunology Endocrinology Cancer
Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC₅₀ of 204 nM . Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca ²⁺ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9 .

HY-B1302

Quinidine hydrochloride monohydrate 20+ Cited Publications	P-glycoprotein PARP Caspase Apoptosis Potassium Channel	Cardiovascular Disease Neurological Disease
Quinidine hydrochloride monohydrate is an orally active antiarrhythmic agent. Quinidine hydrochloride monohydrate reduces the expression level of P-gp, inhibits P-gp-mediated efflux, increases the intracellular accumulation of P-gp substrates, induces PARP cleavage and Caspase-3 activation, and elevates the proportion of Apoptotic cells at the sub-G1 phase. Quinidine hydrochloride monohydrate exerts sustained block and open-channel block effects on I_K(f). Quinidine hydrochloride monohydrate alters the urinary metabolic ratio of Amphetamine, modulates the Pentylenetetrazol-induced seizure threshold, and regulates the anticonvulsant effect of Dextromethorphan. Quinidine hydrochloride monohydrate can be used in studies related to uterine sarcoma and seizures .

HY-B1482A

Mesoridazine TPS-23	Potassium Channel	Neurological Disease
Mesoridazine (TPS-23) , a metabolite of Thioridazine (HY-B0965A), acts as an orally active phenothiazine antipsychotic agent. Mesoridazine is a potent and rapid open-channel blocker of human ether-a-go-go related gene (hERG) channels and blocks hERG currents with an IC₅₀ of 550 nM (at 0 mV) in human embryonic kidney 293 cells .Mesoridazine can be used for the research of schizophrenia, as well as certain other psychiatric disorders .

HY-B1193R

Terfenadine (Standard) (±)-Terfenadine (Standard); MDL-991 (Standard)	Reference Standards Potassium Channel Histamine Receptor Na+/Ca2+ Exchanger Caspase Apoptosis	Inflammation/Immunology Endocrinology Cancer
Terfenadine (Standard) is the analytical standard of Terfenadine. This product is intended for research and analytical applications. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM . Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9 .

HY-100547

IEM-1754	iGluR	Neurological Disease
IEM-1754, a dicationic adamantane derivative, is a potent blocker of open channels of native ionotropic glutamate receptors including quisqualate-sensitive receptors in insect muscles, NMDAR in cultured rat cortical neurons, and AMPAR in freshly isolated hippocampal cells. IEM-1754 shows anticonvulsant potency in vivo .

HY-B1482

Mesoridazine benzenesulfonate TPS-23 benzenesulfonate	Potassium Channel	Neurological Disease
Mesoridazine (TPS-23) benzenesulfonate, a metabolite of Thioridazine (HY-B0965A), acts as an orally active phenothiazine antipsychotic agent. Mesoridazine benzenesulfonate is a potent and rapid open-channel blocker of human ether-a-go-go related gene (hERG) channels and blocks hERG currents with an IC₅₀ of 550 nM (at 0 mV) in human embryonic kidney 293 cells .Mesoridazine benzenesulfonate can be used for the research of schizophrenia, as well as certain other psychiatric disorders .

HY-N8472

Chrodrimanin B	GABA Receptor	Infection
Chrodrimanin B, a metabolite of a fungal, is a potent, non-open-channel-blocking antagonist on?B.?mori GABAR RDL with an IC₅₀?of 1.13 nM. Chrodrimanin B attenuates the peak current amplitude of the GABA response of RDL with an IC₅₀?of 1.66 nM.?Chrodrimanin B, a meroterpenoid, shows insecticidal activity .

HY-164264

Caged MK801	iGluR	Neurological Disease
Caged MK801 (cMK801) is a selective, non-competitive, irreversible NMDA receptor open-channel blocker. NVOC cages are neuro pharmocologically compatible .

HY-B1193S

Terfenadine-d3	Isotope-Labeled Compounds Na+/Ca2+ Exchanger Histamine Receptor Apoptosis Caspase Potassium Channel	Inflammation/Immunology Endocrinology Cancer
Terfenadine-d₃ ((±)-Terfenadine-d₃) is the deuterium labeled Terfenadine. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC₅₀ of 204 nM . Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9[2].

HY-B1482AS

Mesoridazine-d3	Isotope-Labeled Compounds Potassium Channel	Neurological Disease
Mesoridazine-d₃ is the deuterium labeled Mesoridazine (HY-B1482A). Mesoridazine (TPS-23) , a metabolite of Thioridazine (HY-B0965A), acts as an orally active phenothiazine antipsychotic agent. Mesoridazine is a potent and rapid open-channel blocker of human ether-a-go-go related gene (hERG) channels and blocks hERG currents with an IC₅₀ of 550 nM (at 0 mV) in human embryonic kidney 293 cells .Mesoridazine can be used for the research of schizophrenia, as well as certain other psychiatric disorders .

HY-107697

N20C hydrochloride	iGluR	Neurological Disease
N20C hydrochloride is a selective and noncompetitive open NMDA receptor open channel blocker, with micromolar affinity, fast on-off blockade kinetics, and strong voltage dependence. Neuroprotective activity .

HY-W115674

Quinidine hydrochloride	P-glycoprotein PARP Caspase Apoptosis Potassium Channel	Cardiovascular Disease Neurological Disease Cancer
Quinidine hydrochloride is an orally active antiarrhythmic agent. Quinidine hydrochloride reduces the expression level of P-gp, inhibits P-gp-mediated efflux, increases the intracellular accumulation of P-gp substrates, induces PARP cleavage and Caspase-3 activation, and elevates the proportion of Apoptotic cells at the sub-G1 phase. Quinidine hydrochloride exerts sustained block and open-channel block effects on I_K(f). Quinidine hydrochloride alters the urinary metabolic ratio of Amphetamine, modulates the Pentylenetetrazol-induced seizure threshold, and regulates the anticonvulsant effect of Dextromethorphan. Quinidine hydrochloride can be used in studies related to uterine sarcoma and seizures .

HY-180370

Nitromemantine NitroSynapsin; YQW-036; NMI-6979	iGluR Drug Derivative	Cardiovascular Disease Neurological Disease
Nitromemantine (NitroSynapsin) is a nitrate derivative of Memantine (HY-B0591) and is a dual-functional NMDAR antagonist. Nitromemantine exhibits significant efficacy in rodent models of cerebral infarction through a dual mechanism of blocking channels and regulating receptors via NO/redox regulation. Nitromemantine can target ischemic neurons under hypoxic conditions and enhance its activity. Nitromemantine inhibits the current induced by NMDA, with its IC₅₀ being 2.4 μM. Nitromemantine can be used for the study of cerebral ischemic stroke .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-B1302

Quinidine hydrochloride monohydrate 20+ Cited Publications	Cardiovascular Disease Structural Classification Natural Products Classification of Application Fields Rubiaceae Cinchona calisaya Wedd. Plants Disease Research Fields Source Classification	P-glycoprotein PARP Caspase Apoptosis Potassium Channel
Quinidine hydrochloride monohydrate is an orally active antiarrhythmic agent. Quinidine hydrochloride monohydrate reduces the expression level of P-gp, inhibits P-gp-mediated efflux, increases the intracellular accumulation of P-gp substrates, induces PARP cleavage and Caspase-3 activation, and elevates the proportion of Apoptotic cells at the sub-G1 phase. Quinidine hydrochloride monohydrate exerts sustained block and open-channel block effects on I_K(f). Quinidine hydrochloride monohydrate alters the urinary metabolic ratio of Amphetamine, modulates the Pentylenetetrazol-induced seizure threshold, and regulates the anticonvulsant effect of Dextromethorphan. Quinidine hydrochloride monohydrate can be used in studies related to uterine sarcoma and seizures .

HY-N8472

Chrodrimanin B	Infection Microorganisms Classification of Application Fields Ketones, Aldehydes, Acids Disease Research Fields Source Classification	GABA Receptor
Chrodrimanin B, a metabolite of a fungal, is a potent, non-open-channel-blocking antagonist on?B.?mori GABAR RDL with an IC₅₀?of 1.13 nM. Chrodrimanin B attenuates the peak current amplitude of the GABA response of RDL with an IC₅₀?of 1.66 nM.?Chrodrimanin B, a meroterpenoid, shows insecticidal activity .

Cat. No.	Product Name	Chemical Structure

HY-B1193S

Terfenadine-d3
Terfenadine-d₃ ((±)-Terfenadine-d₃) is the deuterium labeled Terfenadine. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC₅₀ of 204 nM . Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9[2].

Terfenadine-d3

Terfenadine-d₃ ((±)-Terfenadine-d₃) is the deuterium labeled Terfenadine. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC₅₀ of 204 nM . Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9[2].

HY-B1482AS

Mesoridazine-d3
Mesoridazine-d₃ is the deuterium labeled Mesoridazine (HY-B1482A). Mesoridazine (TPS-23) , a metabolite of Thioridazine (HY-B0965A), acts as an orally active phenothiazine antipsychotic agent. Mesoridazine is a potent and rapid open-channel blocker of human ether-a-go-go related gene (hERG) channels and blocks hERG currents with an IC₅₀ of 550 nM (at 0 mV) in human embryonic kidney 293 cells .Mesoridazine can be used for the research of schizophrenia, as well as certain other psychiatric disorders .

Mesoridazine-d3

Mesoridazine-d₃ is the deuterium labeled Mesoridazine (HY-B1482A). Mesoridazine (TPS-23) , a metabolite of Thioridazine (HY-B0965A), acts as an orally active phenothiazine antipsychotic agent. Mesoridazine is a potent and rapid open-channel blocker of human ether-a-go-go related gene (hERG) channels and blocks hERG currents with an IC₅₀ of 550 nM (at 0 mV) in human embryonic kidney 293 cells .Mesoridazine can be used for the research of schizophrenia, as well as certain other psychiatric disorders .

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