Calcium Channel
Calcium channels generate intracellular Ca2+ signals by mediating Ca2+ entry during depolarization in excitable cells[1]. These signals support neurotransmitter release, hormone release, excitation-contraction coupling, pacemaker activity, gene transcription, and synaptic plasticity[1][2]. Mechanistically, adrenergic agonists increase cardiac Ca2+ influx through PKA phosphorylation of Rad, which releases inhibition of calcium channels and enhances contractility[3]. In disease research, CACNA1C/CaV1.2 links L-type calcium channel signaling to bipolar disorder, depression, schizophrenia, autism spectrum disorders, brain function, and rodent antidepressant-like behavioral actions of LTCC inhibitors[4]. Compared with related isoforms, CaVα1 splice variants show tissue-specific expression, distinct protein-domain composition, and different pharmacological sensitivities[5]. CaV2.2 e37a is enriched in nociceptors and couples N-type calcium channels to voltage-independent G protein inhibition by µ-opioid and GABA_B receptors[6]. For experimental applications, blockers, toxins, gene-knockout models, agonists, and inhibitors help dissect channel-specific functions and guide next-generation CaV channel modulators[1][5].
References:
- [1]. Striessnig J, et al. Exploring the function and pharmacotherapeutic potential of voltage-gated Ca2+ channels with gene knockout models. Channels (Austin). 2008 Jul-Aug;2(4):233-51. [Content Brief]
- [2]. Prakriya M. Calcium and cell function. J Physiol. 2020 May;598(9):1647-1648. doi: 10.1113/JP279541. PMID: 32350889; PMCID: PMC7885240. et al. Calcium and cell function. J Physiol. 2020 May;598(9):1647-1648. [Content Brief]
- [3]. Papa A, et al. Adrenergic Regulation of Calcium Channels in the Heart. Annu Rev Physiol. 2022 Feb 10;84:285-306. [Content Brief]
- [4]. Bhat S, et al. CACNA1C (Cav1.2) in the pathophysiology of psychiatric disease. Prog Neurobiol. 2012 Oct;99(1):1-14. [Content Brief]
- [5]. Lipscombe D, et al. Calcium Channel CaVα₁ Splice Isoforms - Tissue Specificity and Drug Action. Curr Mol Pharmacol. 2015;8(1):22-31. [Content Brief]
- [6]. Lipscombe D, et al. Alternative splicing matters: N-type calcium channels in nociceptors. Channels (Austin). 2007 Jul-Aug;1(4):225-7. [Content Brief]
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Calcium Channel Related Products (961)
Related Products (961)
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L-Ascorbic acid sodium salt (Standard)
0 ImagesSynonyms: Sodium ascorbate (Standard); Sodium L-ascorbate (Standard); Vitamin C sodium salt (Standard)L-Ascorbic acid (sodium salt) (Standard) is the analytical standard of L-Ascorbic acid (sodium salt). This product is intended for research and analytical applications. L-Ascorbic acid sodium salt (Sodium ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid sodium salt selectively inhibits Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid sodium salt is also a collagen deposition enhancer and an elastogenesis inhibitor.
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Nimodipine (Standard)
0 ImagesCat. No.: HY-B0265RCAS No.: 66085-59-4Synonyms: BAY-e 9736 (Standard)Nimodipine (Standard) is the analytical standard of Nimodipine. This product is intended for research and analytical applications. Nimodipine (BAY-e 9736) is an orally active, well-tolerated and light-sensitive dihydropyridine calcium antagonist. Nimodipine can be used for the research of cerebrovascular disorders.
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Verapamil-d3
0 ImagesCat. No.: HY-14275SCAS No.: 152561-91-6Synonyms: (±)-Verapamil-d3; CP-16533-1-d3Verapamil-d3 ((±)-Verapamil-d3) is deuterium labeled Verapamil. Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research.
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Inositol 1,3-bisphosphate sodium
0 ImagesCat. No.: HY-W788583CAS No.: 208584-52-5Inositol 1,3-bisphosphate sodium is one of the many inositol phosphate (InsP) isomers that could act as small, soluble second messengers in the transmission of cellular signals.
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Brovincamine
0 ImagesCat. No.: HY-106698CAS No.: 57475-17-9Brovincamine is an orally active slow Ca2+ channel blocker and vasodilator. Brovincamine reduces Ca2+ influx across the plasma membrane by blocking Ca2+ channels. Brovincamine inhibits catecholamine secretion, cholinergic function, autonomic parasympathetic nervous system activity, cerebrovascular resistance, and nerve stimulation-induced convulsive responses. Brovincamine induces cerebrovascular, coronary, and intracranial vasodilation, improves cerebral cortical microcirculation, enhances cerebral metabolic activity, and increases capillary clearance efficiency. Brovincamine can be used in research related to cerebral ischemic diseases, cardiac ischemic diseases, and normal-tension glaucoma.
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Manidipine (Standard)
0 ImagesManidipine (Standard) is the analytical standard of Manidipine. This product is intended for research and analytical applications. Manidipine is an orally active calcium channel antagonist. Manidipine regulates the expression of cytokines (IL-1β, IL-6). Manidipine has a hypotensive effect. Manidipine can be used in the study of cardiovascular diseases (such as hypertension, myocardial ischemia-reperfusion injury, ventricular hypertrophy), kidney diseases (such as glomerular diseases), and epilepsy.
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Thapsigargicin
0 ImagesSynonyms: ThapsigargicineThapsigargicin (Thapsigargicine) is a activator of mast cells and leukocytes. Thapsigargicin induces histamine release from rat peritoneal mast cells and human basophil leukocytes. Thapsigargicin increases the cytoplasmic free calcium level in intact human blood platelets.
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CGP 28392
0 ImagesCat. No.: HY-118136CAS No.: 89289-93-0CGP 28392 is an activator for calcium channel, and reactivates the oxygen evolution in calcium-deficient photosystem II (PS II) particles.
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CERM11956
0 ImagesCat. No.: HY-108981CAS No.: 97631-49-7CERM11956 is a potent anti-ischaemic agent. CERM11956 is a derivative of bepridil(HY-16952).
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ML218 (Standard)
0 ImagesCat. No.: HY-103309RCAS No.: 1346233-68-8ML218 (Standard) is the analytical standard of ML218 (HY-103309). This product is intended for research and analytical applications. ML218 is a potent, selective and orally active T-type Ca2+ channels (Cav3.1, Cav3.2, Cav3.3) inhibitor with IC50s of 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively. ML218 inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 has no significant inhibition of L- or N-type calcium channels, KATP or hERG potassium channels. ML218 can penetrate the blood-brain barrier.
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Manidipine dihydrochloride (Standard)
0 ImagesSynonyms: CV-4093 (Standard)Manidipine (dihydrochloride) (Standard) is the analytical standard of Manidipine (dihydrochloride). This product is intended for research and analytical applications. Manidipine dihydrochloride is a third-generation, lipophilic, orally active and highly vasoselective calcium channel antagonist (IC50 = 2.6 nM in guinea-pig ventricular cells) and acts as an antihypertensive agent. Manidipine effectively reduces blood pressure as well as improving insulin sensitivity, renal protection, and antiatherosclerotic activity. Manidipine also exerts anti-inflammatory activity mediated by NF-κB and antiviral activity against many flavivirus and negative-strand RNA viruses through the inhibition of calcium channel. Manidipine is widely applied to research of cardiovascular, metabolic disease and infection.
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Levamlodipine besylate Hemipentahydrate
0 ImagesCat. No.: HY-14744DCAS No.: 884648-62-8Levamlodipine besylate Hemipentahydrate is an orally active L-type calcium channel blocker and MMP-9 modulator with high permeability and retention properties. Levamlodipine besylate Hemipentahydrate significantly enhances plaque stability and improves lipid profiles by reducing blood pressure, decreasing systolic blood pressure variability, and inhibiting MMP-9 expression in atherosclerotic plaques. Levamlodipine besylate Hemipentahydrate not only alleviates cardiac and aortic hypertrophy and prevents renal atrophy, but also produces synergistic effects in blood pressure reduction and organ protection when combined with bisoprolol (HY-129029). Levamlodipine besylate Hemipentahydrate exerts no significant inhibitory effect on abdominal aortic intimal hyperplasia. When excessively accumulated in the epidermis, Levamlodipine besylate Hemipentahydrate may induce changes in keratin structure, impair the skin barrier and trigger inflammation; long-term use further exacerbates skin irritation caused by local administration. Levamlodipine besylate Hemipentahydrate can be used in research related to hypertension and atherosclerosis.
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(R)-Lercanidipine
0 ImagesCat. No.: HY-B0612CCAS No.: 185197-70-0(R)-Lercanidipine is the R-enantiomer of Lercanidipine. (R)-lercanidipine is a calcium channel blocker.
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Cilnidipine-d4
0 ImagesCat. No.: HY-17404S1Synonyms: FRC-8653-d4
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Almorexant (Standard)
0 ImagesCat. No.: HY-10805RCAS No.: 871224-64-5Synonyms: ACT 078573 (Standard)Almorexant (Standard) is the analytical standard of Almorexant. This product is intended for research and analytical applications. Almorexant (ACT 078573) is an orally active, potent and competitive dual orexin receptor antagonist, with Kd values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant totally blocked the intracellular Ca2+ signal pathway. Almorexant stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis .
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D-myo-Inositol-1,4,5,6-tetraphosphate sodium
0 ImagesCat. No.: HY-W794363CAS No.: 157542-47-7D-myo-Inositol-1,4,5,6-tetraphosphate sodium is one of several different inositol oligophosphate isomers implicated in signal transduction.
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(-)-SA2572
0 ImagesCat. No.: HY-118968CAS No.: 112946-90-4(-)-SA2572 is an orally active Ca2+ inward channel inhibitor. (-)-SA2572 inhibits the slow Ca2+ inward channel and the fast Na+ inward channel. (-)-SA2572 inhibits depolarization-induced contraction of gastrointestinal smooth muscle and vascular smooth muscle, prolongs atrioventricular nodal conduction time, and inhibits His bundle-ventricular conduction time. (-)-SA2572 reduces systolic blood pressure in spontaneously hypertensive rats. (-)-SA2572 can be used in the research of hypertension.
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Dronedarone (Standard)
0 ImagesSynonyms: SR 33589 (Standard)Dronedarone (Standard) is the analytical standard of Dronedarone. This product is intended for research and analytical applications. Dronedarone (SR 33589), a derivative of amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone is a substrate for and a moderate inhibitor of CYP3A4.
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HA-1004 dihydrochloride
0 ImagesCat. No.: HY-123468ACAS No.: 92564-08-4HA-1004 dihydrochloride is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 dihydrochloride is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 dihydrochloride is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models.
