Search Result
Results for "
Ca2 channel antagonist
" in MedChemExpress (MCE) Product Catalog:
4
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-14656S
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Calcium Channel
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Cardiovascular Disease
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Diltiazem-d3 (hydrochloride) is the deuterium labeled Diltiazem hydrochloride. Diltiazem hydrochloride is a Ca2+ influx inhibitor (slow channel blocker or calcium antagonist)[1][2].
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- HY-16952A
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(±)-Bepridil hydrochloride hydrate; Org 5730 hydrochloride hydrate
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Calcium Channel
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Cardiovascular Disease
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Bepridil hydrochloride hydrate ((±)-Bepridil hydrochloride hydrate) is a non-selective, long-acting Ca + channel antagonist and Na +, K + channel inhibitor, with antianginal and type I antiarrhythmic effects. Bepridil hydrochloride hydrate also acts as a cardiac Na +/Ca2 + exchange (NCX1) inhibitor. Bepridil hydrochloride hydrate can be used for the research of cardiovascular disorders .
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- HY-12962
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iGluR
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Neurological Disease
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NMDA-IN-1 is a potent and NR2B-selective NMDA antagonist with Ki of 0.85 nM; NR2B Ca2+ influx IC50 is 9.7 nM; no activities on NR2A, NR2C, NR2D, hERG-channel and α1-adrenergic receptor.
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- HY-14656
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- HY-14656S1
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- HY-B1193R
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Potassium Channel
Histamine Receptor
Na+/Ca2+ Exchanger
Caspase
Apoptosis
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Inflammation/Immunology
Endocrinology
Cancer
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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 .
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- HY-N0219R
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GABA Receptor
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Neurological Disease
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Bicuculline (Standard) is the analytical standard of Bicuculline. This product is intended for research and analytical applications. Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca2+ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice .
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- HY-A0082R
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mAChR
Sodium Channel
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Neurological Disease
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Diphenidol (hydrochloride) (Standard) is the analytical standard of Diphenidol (hydrochloride). This product is intended for research and analytical applications. Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na+, K+, and Ca2+) in neuronal cells. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea [4] .
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- HY-12882
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RC 61-91; NP-120
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Others
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Neurological Disease
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Ifenprodil (RC 61-91) is a noncompetitive NMDA receptor antagonist with anti-excitotoxic activity. Ifenprodil significantly improves long-term sensorimotor and spatial learning deficits in mice after acute subarachnoid hemorrhage. Ifenprodil reduces neuronal cell death in the basal cortex and CA1 region of the hippocampus induced by experimental subarachnoid hemorrhage. Ifenprodil attenuates Ca2+ overload in basal cortical cells and mitochondria, as well as brain edema in blood-brain barrier damage and early brain injury. Ifenprodil reduces the intracellular Ca2+ increase and apoptosis of primary cortical neurons under conditions of high glutamate concentrations. Ifenprodil also reduces the increase in endothelial permeability caused by high glutamate concentrations in human brain microvascular endothelial cells. Ifenprodil also inhibits GIRK channels and interacts with α1-adrenergic, 5-HT, and σ receptors .
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- HY-N0215S14
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(S)-2-Amino-3-phenylpropionic acid-15N,d8
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Isotope-Labeled Compounds
Calcium Channel
iGluR
Endogenous Metabolite
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Metabolic Disease
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L-Phenylalanine- 15N,d8 is the deuterium and 15N-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca2+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
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- HY-U00026
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- HY-U00212
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- HY-131942
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- HY-136909
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Calcium Channel
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Cardiovascular Disease
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SR33805 is a potent Ca 2+ channel antagonist, with EC50s of 4.1 nM and 33 nM in depolarized and polarized conditions, respectively. SR33805 blocks L-type but not T-type Ca 2+ channels. SR33805 can be used for the research of acute or chronic failing hearts .
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- HY-10388
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- HY-103313
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Calcium Channel
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Cardiovascular Disease
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SR33805 oxalate is a potent Ca 2+ channel antagonist, with EC50s of 4.1 nM and 33 nM in depolarized and polarized conditions, respectively. SR33805 oxalate blocks L-type but not T-type Ca 2+ channels. SR33805 oxalate can be used for the research of acute or chronic failing hearts .
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- HY-19062
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- HY-14656R
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CRD-401 (Standard)
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Calcium Channel
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Cardiovascular Disease
Cancer
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Diltiazem (hydrochloride) (Standard) is the analytical standard of Diltiazem (hydrochloride). This product is intended for research and analytical applications. Diltiazem hydrochloride is a Ca 2+ influx inhibitor (slow channel blocker or calcium antagonist).
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- HY-19409
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Calcium Channel
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Neurological Disease
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AJG049 is a novel antagonist of the Ca 2+ channel with an IC50 value of 79 nM. AJG049 can be used to reduce the contraction of intestinal smooth muscle .
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- HY-106818A
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AJ-2615
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Acyltransferase
Calcium Channel
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Cardiovascular Disease
Metabolic Disease
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Monatepil maleate (AJ-2615) is a potent and orally active Ca 2+-channel antagonist and a noncompetitive ACAT inhibitor. Monatepil maleate decreases blood pressure and improves plasma lipid metabolism. Monatepil maleate has the potential for the research of hyperlipidemia .
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- HY-10388A
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Calcium Channel
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Others
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TTA-Q6(isomer) is an isomer of TTA-Q6. TTA-Q6 is a selective T-type Ca 2+ channel antagonist.
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- HY-U00212R
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Calcium Channel
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Cardiovascular Disease
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Aranidipine (Standard) is the analytical standard of Aranidipine. This product is intended for research and analytical applications. Aranidipine (MPC1304) is a Ca 2+ channel antagonist with potent and long-lasting antihypertensive effects.
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- HY-121604
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Calcium Channel
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Others
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(Rac)-MEM 1003 is the racemate of MEM 1003. MEM 1003, a dihydropyridine compound, is a potent L-type Ca 2+ channel antagonist and has the potential for Alzheimer’s disease research .
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- HY-100783
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l-Bicuculline methobromide
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GABA Receptor
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Neurological Disease
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(-)-Bicuculline methobromide (l-Bicuculline methobromide) is a potent GABAA receptor antagonist. (-)-Bicuculline methobromide blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-activated K + channels in various types of neurons .
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- HY-100783A
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l-Bicuculline methochloride
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GABA Receptor
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Neurological Disease
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(-)-Bicuculline methochloride (l-Bicuculline methochloride) is a potent GABAA receptor antagonist. (-)-Bicuculline methochloride blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-activated K + channels in various types of neurons .
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- HY-167203
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Calcium Channel
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Cardiovascular Disease
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AJG049 free base is a calcium channel (Ca 2+ channel) antagonist. AJG049 free base regulates vascular relaxation, reduces cardiac load, and improves cardiac perfusion by binding to the binding site of L-type calcium channels, specifically Diltiazem (HY-B0632). AJG049 free base can be used in cardiovascular disease research .
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- HY-133596
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Potassium Channel
GABA Receptor
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Neurological Disease
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12,14-Dichlorodehydroabietic acid, a chlorinated resin acid, is a potent Ca 2+-activated K + (BK) channel opener. 12,14-Dichlorodehydroabietic acid blocks GABA-dependent chloride entry in mammalian brain and operates as a non-competitive GABAA antagonist. 12,14-Dichlorodehydroabietic acid increases cytosolic free Ca 2+ and stimulates transmitter release .
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- HY-B0358A
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Calcium Channel
Sodium Channel
Dopamine Receptor
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Neurological Disease
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Flunarizine dihydrochloride is a potent dual Na +/Ca 2+ channel (T-type) blocker. Flunarizine dihydrochloride is a D2 dopamine receptor antagonist. Flunarizine dihydrochloride shows anticonvulsive and antimigraine activity, and peripheral vasodilator effects .
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- HY-B0358
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- HY-15084B
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Dizocilpine
Maximum Cited Publications
27 Publications Verification
MK-801
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iGluR
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Neurological Disease
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Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca 2+ flux .
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- HY-100783B
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(+)-Bicuculline methobromide; d-Bicuculline methobromide
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GABA Receptor
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Neurological Disease
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Bicuculline methobromide is a selective GABAA Receptor antagonist with an IC50 value of 3 μM. Bicuculline methobromide induces clonic tonic convulsions in mammals and can also be used to block Ca 2+ activated potassium channels. Bicuculline methobromide can be used in studies of epilepsy and other related psychiatric disorders .
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- HY-N4267
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Calcium Channel
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Infection
Cardiovascular Disease
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Yangambin, a furofuran lignan, is already isolated from plants such as member of the Annonaceae family, including species of the genus Rollinia: R. pickeli, R. exalbidaand R. mucosa, as well from the Magnolia biondii. Yangambin, a selective PAF receptor antagonist, inhibits Ca 2+ influx through voltage-gated Ca 2+ channels, leading to the reduction in [Ca 2+]i in vascular smooth muscle cells and consequent peripheral vasodilation . Yangambin exhibits the antiallergic activity against β-hexosaminidase release with an IC50 of 33.8 μM and for anti-inflammatory activity with an IC50 of 37.4 μM .
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- HY-16935
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JNJ-39439335
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TRP Channel
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Neurological Disease
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Mavatrep (JNJ-39439335) is an orally active, selective and potent TRPV1 antagonist with high affinity for hTRPV1 channels (Ki=6.5 nM). Mavatrep antagonizes capsaicin-induced Ca 2+ influx with an IC50 value of 4.6 nM. Mavatrep can be used in some studies of neuropathic pain .
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- HY-B0358AR
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Calcium Channel
Sodium Channel
Dopamine Receptor
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Neurological Disease
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Flunarizine (dihydrochloride) (Standard) is the analytical standard of Flunarizine (dihydrochloride). This product is intended for research and analytical applications. Flunarizine dihydrochloride is a potent dual Na +/Ca 2+ channel (T-type) blocker. Flunarizine dihydrochloride is a D2 dopamine receptor antagonist. Flunarizine dihydrochloride shows anticonvulsive and antimigraine activity, and peripheral vasodilator effects .
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- HY-B0358R
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Calcium Channel
Sodium Channel
Dopamine Receptor
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Neurological Disease
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Flunarizine (Standard) is the analytical standard of Flunarizine. This product is intended for research and analytical applications. Flunarizine is a potent dual Na +/Ca 2+ channel (T-type) blocker. Flunarizine is a D2 dopamine receptor antagonist. Flunarizine shows anticonvulsive and antimigraine activity, and peripheral vasodilator effects .
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- HY-106904
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Calcium Channel
5-HT Receptor
Dopamine Receptor
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Cardiovascular Disease
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Nexopamil is a calcium antagonist of Ca 2+ channel, 5HT2, 5HT1A, 5HT1C and dopamine D2 receptors. Nexopamil exhibits vasodilatory, cardioprotective, and platelet aggregation inhibiting effects. Nexopamil can be used for researches of stable or unstable angina and possibly of peripheral arterial occlusive disease .
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- HY-B1193
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- HY-N0219
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(+)-Bicuculline; d-Bicuculline
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GABA Receptor
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Neurological Disease
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Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca 2+ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice .
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- HY-137790
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(+)-Bicuculline methochloride; d-Bicuculline methochloride
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GABA Receptor
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Neurological Disease
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Bicuculline ((+)-Bicuculline; d-Bicuculline) methochloride is a selective GABAA receptor antagonist with an IC50 value of 3 μM. Bicuculline methochloride induces clonic tonic convulsions in mammals and can also be used to block Ca 2+ activated potassium channels. Bicuculline methochloride can be used in studies of epilepsy and other related psychiatric disorders .
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- HY-B0358AS
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- HY-A0082
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Difenidol hydrochloride
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mAChR
Sodium Channel
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Neurological Disease
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Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na +, K +, and Ca 2+) in neuronal cells. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea .
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- HY-A0270
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mAChR
Sodium Channel
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Neurological Disease
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Diphenidol is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol is also a potent non-specific blocker of voltage-gated ion channels (Na +, K +, and Ca 2+) in neuronal cells. Diphenidol can be used in the study of antivertigo and antinausea .
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- HY-10341
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HA-1077 Hydrochloride; AT-877 Hydrochloride
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ROCK
Calcium Channel
Autophagy
PKA
PKC
HIV
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Cancer
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Fasudil (HA-1077; AT877) Hydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil Hydrochloride is also a potent Ca 2+ channel antagonist and vasodilator .
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- HY-10341A
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HA-1077; AT877
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ROCK
Calcium Channel
Autophagy
PKA
PKC
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Cancer
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Fasudil (HA-1077; AT877) is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil is also a potent Ca 2+ channel antagonist and vasodilator .
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- HY-10341C
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HA-1077 dihydrochloride; AT-877 dihydrochloride
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Calcium Channel
ROCK
PKA
PKC
Autophagy
HIV
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Cancer
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Fasudil (HA-1077; AT877) dihydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil dihydrochloride is also a potent Ca 2+ channel antagonist and vasodilator .
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- HY-10341B
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HA-1077 hydrochloride semihydrate; AT877 hydrochloride semihydrate
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ROCK
Calcium Channel
Autophagy
HIV
PKA
PKC
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Cancer
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Fasudil (HA-1077; AT877) hydrochloride semihydrate is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil hydrochloride semihydrate is also a potent Ca 2+ channel antagonist and vasodilator .
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- HY-126010
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Piezo Channel
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Others
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Dooku1 is a reversibly Yoda1 antagonist with IC50 value of 1.3 μM and 1.5 μM for 2 μM Yoda1-induced Ca 2+ entry HEK 293 cells and HUVECs, respectively. Dooku1 can disrupt Yoda1-induced Piezo1 channel activity and inhibit Yoda1-induced relaxation of aorta. Dooku1 can be used for vascular physiology and disease research .
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- HY-10341D
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HA-1077 mesylate; AT-877 mesylate
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ROCK
Calcium Channel
Autophagy
PKA
PKC
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Cancer
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Fasudil (HA-1077; AT877) mesylate is a nonspecific and orally active RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil mesylate is also a potent Ca 2+ channel antagonist and vasodilator .
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- HY-10341R
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ROCK
Calcium Channel
Autophagy
PKA
PKC
HIV
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Cancer
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Fasudil (Hydrochloride) (Standard) is the analytical standard of Fasudil (Hydrochloride). This product is intended for research and analytical applications. Fasudil (HA-1077; AT877) Hydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil Hydrochloride is also a potent Ca 2+ channel antagonist and vasodilator .
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- HY-B0561
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SC9420
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Mineralocorticoid Receptor
Androgen Receptor
Autophagy
Calcium Channel
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Cardiovascular Disease
Metabolic Disease
Endocrinology
Cancer
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Spironolactone is an aldosterone antagonist that acts on the aldosterone mineralocorticoid receptor (IC50=24 nM) and androgen receptor (IC50=77 nM), promotes podocyte autophagy and regulates pain. Spironolactone improves hypertension-related vascular hypertrophy and remodeling by reducing angiotensin II (AngⅡ)-induced inflammation, reduces aldosterone-induced vascular and soft tissue calcification through PIT1-dependent signaling, and alleviates vascular dysfunction in type Ⅱ diabetic mice by reducing oxidative stress and restoring NO/GC signaling; at low concentrations, it and its metabolites can interfere with aldosterone biosynthesis in the adrenal cortex and inhibit voltage-dependent Ca 2+ channels to exert antihypertensive effects .
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HY-L117
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160 compounds
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Calcium channel blockers (CCBs), also called calcium antagonists are compounds that slow the movement of calcium (Ca2+) through calcium channels into the cells of the heart and blood vessel walls. Calcium causes the heart and arteries to squeeze more strongly. By blocking calcium, calcium channel blockers allow blood vessels to relax and open. So calcium channel blockers are usually used to lower blood pressure, relieve chest pain (angina) and control an irregular heartbeat.
MCE supplies a unique collection of 160 calcium channel blockers and antagonists, all of which have the identified inhibitory effect on calcium channel. MCE Calcium Channel Blocker Library is a useful tool for discovery of antihypertensive drugs and cardiovascular disease research.
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-14656S
-
|
Diltiazem-d3 (hydrochloride) is the deuterium labeled Diltiazem hydrochloride. Diltiazem hydrochloride is a Ca2+ influx inhibitor (slow channel blocker or calcium antagonist)[1][2].
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- HY-14656S1
-
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Diltiazem-(acetoxy-d3) (hydrochloride) is the deuterium labeled Diltiazem hydrochloride. Diltiazem hydrochloride is a Ca2+ influx inhibitor (slow channel blocker or calcium antagonist)[1][2].
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- HY-N0215S14
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L-Phenylalanine- 15N,d8 is the deuterium and 15N-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca2+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
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- HY-B0358AS
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Flunarizine-d8 dihydrochloride is deuterated labeled Flunarizine dihydrochloride (HY-B0358A). Flunarizine dihydrochloride is a potent dual Na +/Ca 2+ channel (T-type) blocker. Flunarizine dihydrochloride is a D2 dopamine receptor antagonist. Flunarizine dihydrochloride shows anticonvulsive and antimigraine activity, and peripheral vasodilator effects .
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