1482 Results for "

Potassium Channel Inhibitor

" in MedChemExpress (MCE) Product Catalog:
Products (1482)

1482 Results for "Potassium Channel Inhibitor" in MCE Product Catalog:

Cat. No.: HY-13551C
CAS No.: 80277-14-1
Synonyms: m-AMSA isethionate; Acridinyl anisidide isethionate
Amsacrine isethionate (m-AMSA isethionate) is a Topoisomerase II inhibitor. Amsacrine isethionate intercalates into DNA. Amsacrine isethionate induces Ca 2+-mediated inactivation of ERK, and also downregulates AKT, promoting MCL1 downregulation mediated by GSK3β via reducing the phosphorylation level of GSK3β. Amsacrine isethionate induces Apoptosis by activating Caspase-9 and Caspase-3. Amsacrine isethionate blocks HERG potassium channels in the open/inactivated state. Amsacrine isethionate induces chromosomal aberrations and sister chromatid exchanges, and inhibits the synthesis of RNA and DNA. Amsacrine isethionate exhibits anti-leukemic activity. Amsacrine isethionate causes cardiac repolarization disorders, QT interval prolongation, ventricular arrhythmias, and increases the risk of sudden cardiac death. Amsacrine isethionate can be used in research related to acute myeloid leukemia, lymphoma and progressive malignancies .
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Cat. No.: HY-13551D
CAS No.: 80277-11-8
Synonyms: m-AMSA lactate; Acridinyl anisidide lactate
Amsacrine lactate (m-AMSA lactate) is a Topoisomerase II inhibitor. Amsacrine lactate intercalates into DNA. Amsacrine lactate induces Ca 2+-mediated inactivation of ERK, and also downregulates AKT, promoting MCL1 downregulation mediated by GSK3β via reducing the phosphorylation level of GSK3β. Amsacrine lactate induces Apoptosis by activating Caspase-9 and Caspase-3. Amsacrine lactate blocks HERG potassium channels in the open/inactivated state. Amsacrine lactate induces chromosomal aberrations and sister chromatid exchanges, and inhibits the synthesis of RNA and DNA. Amsacrine lactate exhibits anti-leukemic activity. Amsacrine lactate causes cardiac repolarization disorders, QT interval prolongation, ventricular arrhythmias, and increases the risk of sudden cardiac death. Amsacrine lactate can be used in research related to acute myeloid leukemia, lymphoma and progressive malignancies .
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Cat. No.: HY-187364
CAS No.: 3050594-88-9
Research Areas:  

Inflammation/Immunology

TRPV4 antagonist-7 is a potent and selective TRPV4 antagonist with an IC50 of 0.2 nM against human targets. TRPV4 antagonist-7 binds to the voltage-sensor-like domain cavity of TRPV4 and inhibits channel activity through the formation of salt bridges, hydrogen bonds, and edge-to-face π-stacking interactions. TRPV4 antagonist-7 induces phospholipid accumulation in HepG2 C3A cells in vitro with an IC50 of 3.8 μM, and exhibits moderate inhibitory effects on CYP2D6 with an IC50 of 5.1 μM. TRPV4 antagonist-7 dose-dependently inhibits GSK1016790A (HY-19608)-induced bronchoconstriction in rats and cough in guinea pigs. TRPV4 antagonist-7 can be used in studies related to respiratory system diseases .
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Cat. No.: HY-189470
Nav1.2-IN-4 is a blood-brain barrier-penetrant NaV1.2 inhibitor (IC50 = 31.21 μM). Nav1.2-IN-4 preferentially blocks the inactivated state of the neuronal voltage-gated sodium channel NaV1.2, inhibiting persistent and resurgent sodium currents associated with epileptogenesis. Nav1.2-IN-4 restores the GABA-glutamate balance by enhancing GABA and reducing glutamate. Nav1.2-IN-4 reduces oxidative stress in brain tissue by increasing GSH and decreasing MDA. Nav1.2-IN-4 protects mice against MES-induced tonic hindlimb extensor seizures and attenuates hippocampal neuronal degeneration in the PTZ kindling model. Nav1.2-IN-4 can be used for research on epilepsy .
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Cat. No.: HY-P2786A
CAS No.: 741738-57-8
Target:  

Potassium Channel

Research Areas:  

Neurological Disease

Phrixotoxin 2 is a Kv4 family potassium channel inhibitor, with Ki values in rats of 120 nM for Kv4.2, 110 nM for Kv4.3, and 230 nM for Kv4.1. Phrixotoxin 2 mediates voltage-dependent inhibition of Kv4.2 and Kv4.3 currents, and voltage-independent inhibition of Kv4.1 currents. Phrixotoxin 2 fails to inhibit A-type K + currents in visceral dorsal root ganglion neurons. Phrixotoxin 2 induces contraction of non-pregnant uterine smooth muscle and triggers orofacial cold hyperalgesia in rats. Phrixotoxin 2 can distinguish the contribution of Kv4 subunits to A-type K + currents in different subsets of sensory neurons. Phrixotoxin 2 can be used in research related to chronic pain and trigeminal neuropathic pain .
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Cat. No.: HY-101396R
CAS No.: 582323-16-8
ICA-069673 (Standard) is the analytical standard of ICA-069673 (HY-101396). This product is intended for research and analytical applications. ICA-069673 is a KCNQ2/Q3 potassium channel activator. ICA-069673 demonstrates greater selectivity for KV7.2/7.3 over KV7.3/KV7.5, with EC50s of 0.69 μM and 14.3 μM, respectively. ICA-069673 inhibits spontaneous phasic and nerve-evoked contractions in guinea pig detrusor smooth muscle (DSM). ICA-069673 also decreases the global intracellular Ca(2+) concentration in DSM cells .
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Cat. No.: HY-119649S
CAS No.: 2483830-60-8
Purity:  ≥98.0%
Synonyms: IKI220-15N18O
Flonicamid- 15N, 18O (IKI220- 15N, 18O) is the 18O , 15N-labeled Flonicamid (HY-119649). Flonicamid (IKI220) is an antifeedant Insecticide active against Hemiptera, Thysanoptera, and piercing-sucking pests including aphids of all species, developmental stages and morphs. Flonicamid inhibits the inward rectifier potassium channel NlKir1, blocking stylet penetration, salivation, sap feeding, honeydew secretion, and fluid secretion by isolated Malpighian tubules. Flonicamid reduces renal excretory function in female Culex pipiens pallens. Flonicamid rapidly disrupts insect feeding behavior without neurotoxic poisoning symptoms, induces irreversible starvation, and increases the mortality of nymph progeny of adult aphids exposed to this agent .
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Cat. No.: HY-12962A
CAS No.: 1784252-90-9
Target:  

iGluR

Research Areas:  

Neurological Disease

NMDA-IN-1 dihydrochloride is a selective NMDA NR2B antagonist with a Ki of 0.85 nM; NR2B Ca2+ influx IC50 is 9.7 nM. NMDA-IN-1 dihydrochloride inhibits Glu/Gly stimulated Ca2+ flux in Ltk- cells expressing the hNR1a/NR2B with a IC50 of 9.7 nM. NMDA-IN-1 dihydrochloride has no activities on NR2A, NR2C, NR2D, hERG-channel and α1-adrenergic receptor. NMDA-IN-1 dihydrochloride shows excellent activity in the mechanical hyperalgesia assay in rats. NMDA-IN-1 dihydrochloride can be used for the studies of stroke, parkinson, and neuropathic pain .
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Cat. No.: HY-142117
CAS No.: 149091-92-9
Research Areas:  

Others

Adenophostin A is an IP3 receptor (inositol 1,4,5-trisphosphate receptors) modulator and Ca 2+ releaser, with an IC50 of 1.3 nM, an EC50 of 1.4 nM, and a Ki of 0.18 nM in rats, and an IC50 of 0.95 nM in humans. Adenophostin A activates IP3 receptors, stimulates Ca 2+ release from intracellular stores and microsomes, inhibits the binding of [ 3H]IP3 to plasma membrane receptors, and activates chloride channels. Adenophostin A resists phosphorylation and dephosphorylation by IP3 metabolic enzymes to maintain its activity, and increases cytoplasmic [Ca 2+] levels via calcium mobilization from the endoplasmic reticulum of vascular smooth muscle cells. Adenophostin A is applicable to research related to hemorrhagic shock .
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Cat. No.: HY-185057
CAS No.: 41656-56-8
Synonyms: S-Lactylglutathione; (R)-S-Lactoylglutathione
S-D-Lactoylglutathione (S-Lactylglutathione; (R)-S-Lactoylglutathione) is a multifunctional metabolic intermediate of the glyoxalase system. S-D-Lactoylglutathione activates K + efflux in bacteria by displacing inhibitory glutathione from KefGB channels, thereby acidifying the cytoplasm. In eukaryotic cells, S-D-Lactoylglutathione mediates S-glutathionylation as a substrate of glyoxalase 2. S-D-Lactoylglutathione serves as a sensitive metabolic biomarker for neodymium nitrate neurotoxicity; when used in combination with MSCs-exo, it upregulates glutathione levels, downregulates lactate dehydrogenase and Glo2 levels, and inhibits cellular inflammatory responses and pyroptosis. S-D-Lactoylglutathione can be used in research related to prostate cancer, breast cancer, non-small cell lung cancer, sepsis-associated encephalopathy, and neurotoxicity .
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Cat. No.: HY-B0653AS
Synonyms: (S)-(–)-Bupivacaie-d9hydrochloride
Levobupivacaine-d9 ((S)-(–)-Bupivacaie-d9) hydrochloride is deuterium labeled Levobupivacaine hydrochloride (HY-B0653A). Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local agent that can suppress or relieve pain. Levobupivacaine hydrochloride exerts agent that can suppress or relieve pain. and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine hydrochloride can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine hydrochloride is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine hydrochloride can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer .
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Cat. No.: HY-B1302R
CAS No.: 6151-40-2
Quinidine hydrochloride monohydrate (Standard) is the analytical standard of Quinidine hydrochloride monohydrate (HY-B1302). This product is intended for research and analytical applications. 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 IK(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 .
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Cat. No.: HY-B1751S1
Quinidine- 13C, d2 hydrochloride is the 13C, d2 labeled Quinidine hydrochloride (HY-W115674). 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 IK(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 .
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Cat. No.: HY-N1934R
CAS No.: 483-15-8
Dihydroberberine (Standard) is the analytical standard of Dihydroberberine. This product is intended for research and analytical applications. Dihydroberberine is a naturally occurring isoquinoline alkaloid with anti-inflammatory, anti-atherosclerotic, hypolipidemic and anti-tumor activities. Dihydroberberine inhibits the human ether-related gene (hERG) channel and significantly reduces the expression of heat shock protein 90 (Hsp90) and its interaction with hERG. Dihydroberberine also blocks the TLR4/MyD88/NF-κB signaling pathway to reduce pro-inflammatory cytokines and immunoglobulins, and has inhibitory effects on DSS (HY-116282C)-induced experimental colitis. Dihydroberberine also increases the sensitivity of lung cancer to sunitinib (HY-10255A), with synergistic efficacy .
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Cat. No.: HY-W008581
CAS No.: 1035-77-4
Synonyms: 3-O-Methyl estradiol; 17β-Estradiol 3-methyl ether; 3-Methoxyestradiol
Estradiol 3-methyl ether (EDME) is a highly selective TRPML1 ion channel antagonist and microtubule (microtubule) depolymerizing agent, with IC50 values of 0.22 μM and 3.8 μM against TRPML1 and TRPML2, respectively; it shows no activity against TRPML3. Estradiol 3-methyl ether induces the disruption of cytoplasmic microtubule networks in mammalian cells, with an EC50 of 9 μM. Independent of estrogen receptors, Estradiol 3-methyl ether blocks autophagy (autophagy), TFEB nuclear translocation, and inhibits the migration and invasion of triple-negative breast cancer cells by suppressing TRPML1. Estradiol 3-methyl ether is applicable for relevant research on triple-negative breast cancer .
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Cat. No.: HY-N0168AR
CAS No.: 69097-99-0
(Rac)-Hesperetin (Standard) is the analytical standard of (Rac)-Hesperetin. This product is intended for research and analytical applications. (Rac)-Hesperetin is the racemate of Hesperetin (HY-N0168), an orally active multi-target inhibitor. (Rac)-Hesperetin exhibits significant anti-tumor and anti-inflammatory activities by blocking the TGF-β1-mediated Fyn/RhoA signaling axis and the TLR4-MyD88-NF-κB inflammatory pathway. (Rac)-Hesperetin inhibits the formation of actin stress fibers and the migration and invasion of cancer cells, and is suitable for triple-negative breast cancer research. In inflammation models, (Rac)-Hesperetin effectively alleviates lung injury by reducing the release of pro-inflammatory mediators and regulating the activity of oxidative stress enzymes, and is suitable for acute lung injury research. (Rac)-Hesperetin also interferes with the entry and early replication processes of channel catfish virus, inhibits viral gene expression and progeny virus production, thereby protecting cells from virus-induced cytopathic effects .
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Cat. No.: HY-N0168AS
CAS No.: 1346605-26-2
(Rac)-Hesperetin-d3 is the deuterium labeled (Rac)-Hesperetin. (Rac)-Hesperetin is the racemate of Hesperetin (HY-N0168), an orally active multi-target inhibitor. (Rac)-Hesperetin exhibits significant anti-tumor and anti-inflammatory activities by blocking the TGF-β1-mediated Fyn/RhoA signaling axis and the TLR4-MyD88-NF-κB inflammatory pathway. (Rac)-Hesperetin inhibits the formation of actin stress fibers and the migration and invasion of cancer cells, and is suitable for triple-negative breast cancer research. In inflammation models, (Rac)-Hesperetin effectively alleviates lung injury by reducing the release of pro-inflammatory mediators and regulating the activity of oxidative stress enzymes, and is suitable for acute lung injury research. (Rac)-Hesperetin also interferes with the entry and early replication processes of channel catfish virus, inhibits viral gene expression and progeny virus production, thereby protecting cells from virus-induced cytopathic effects .
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Cat. No.: HY-N4267
CAS No.: 13060-14-5
Yangambin is a PAF receptor antagonist and UGT1A1/UGT1A3 inhibitor, with an IC50 of 29.7 μM and a Ki of 17.1 μM against human UGT1A1, and an IC50 of 56.5 μM and a Ki of 66.8 μM against human UGT1A3. Yangambin blocks PAF-mediated responses, inhibits LTB4-mediated neutrophil infiltration, and suppresses inflammatory events and anaphylactic contraction. Yangambin acts as a central nervous system inhibitor to reduce spontaneous activity, and also exhibits analgesic, anticonvulsant, antileishmanial, vasodilatory and hypotensive effects. Yangambin blocks voltage-gated Ca 2+ channels, reduces the production of NO, TNF-α, IL-6 and PGE2 in cells, increases the production of IL-10, and exerts a protective effect against cardiovascular injury. Yangambin can be used in research related to allergies, cutaneous leishmaniasis, central nervous system diseases and cardiovascular diseases .
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Cat. No.: HY-120078
CAS No.: 1845753-81-2
Target:  

Phospholipase

Research Areas:  

Cardiovascular Disease

AZD2716 is an orally active secretory phospholipase A2 (sPLA2) inhibitor. AZD2716 inhibits human GIIA sPLA2 (IC50=10 nM), human GV sPLA2 (IC50=40 nM), human GX sPLA2 (IC50=400 nM), snake venom sPLA2 (IC50=2 pM), and snake (Bothrops jararacussu) Lys49-PLA2-like toxin (Kd=110 μM). AZD2716 inhibits sPLA2 isoforms IIa, V, X, snake venom sPLA2s, and snake venom Lys49-PLA2-like toxin myotoxic activity via hydrophobic channel binding. AZD2716 suppresses GIIA sPLA2 production, neutralizes snake venom-induced myotoxicity, and improves survival in envenomed mice. AZD2716 can be used for the research of coronary artery disease, atherosclerosis, and snakebite envenoming .
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Cat. No.: HY-N0168AS1
CAS No.: 2750534-85-9
(Rac)-Hesperetin- 13C,d3 is the 13C- and deuterium labeled (Rac)-Hesperetin. (Rac)-Hesperetin is the racemate of Hesperetin (HY-N0168), an orally active multi-target inhibitor. (Rac)-Hesperetin exhibits significant anti-tumor and anti-inflammatory activities by blocking the TGF-β1-mediated Fyn/RhoA signaling axis and the TLR4-MyD88-NF-κB inflammatory pathway. (Rac)-Hesperetin inhibits the formation of actin stress fibers and the migration and invasion of cancer cells, and is suitable for triple-negative breast cancer research. In inflammation models, (Rac)-Hesperetin effectively alleviates lung injury by reducing the release of pro-inflammatory mediators and regulating the activity of oxidative stress enzymes, and is suitable for acute lung injury research. (Rac)-Hesperetin also interferes with the entry and early replication processes of channel catfish virus, inhibits viral gene expression and progeny virus production, thereby protecting cells from virus-induced cytopathic effects .
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