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 (955)
Related Products (955)
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Typhaneoside
0 ImagesTyphaneoside is an orally active activator of PI3K/Akt/mTOR and farnesoid X receptor. Typhaneoside promotes the activation of AMPK and Caspase-3, induces apoptosis, ferroptosis, autophagy, ROS accumulation, cell cycle arrest at the G2/M phase, and reduces cancer cell viability. Typhaneoside improves glucose and lipid metabolism, alleviates inflammatory responses, oxidative stress and hepatic lipid accumulation, and exerts hepatoprotective effects. Typhaneoside can be used in research related to heart failure after myocardial infarction, acute myeloid leukemia, non-alcoholic fatty liver disease and neurological disorders.
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L-Phenylalanine (Standard)
0 ImagesSynonyms: (S)-2-Amino-3-phenylpropionic acid (Standard)L-Phenylalanine (Standard) is the analytical standard of L-Phenylalanine. This product is intended for research and analytical applications. 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 Ca+ 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.
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KB130015
0 ImagesSynonyms: KB015KB130015 (KB015) is an orally active and potent ThRα and ThRβ (thyroid hormone receptor) inhibitor, with IC50 values of 4.5 and 5.1 μM, respectively. KB130015 markedly slows the kinetics of inactivation of Na+ channels. KB130015 activates hERG1 channels (EC50 = 12.2 μM) and large-conductance Ca2+-activated K+ (BKCa) channels formed by hSlo1 (α) subunits in HEK 293 cells. KB130015 has antiarrhythmic properties. KB130015 can be used for the study of cardiovascular disease.
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Acetylcholine-d9 chloride
0 ImagesSynonyms: ACh-d9 chlorideAcetylcholine-d9 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent and BBB-permeable cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs). Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro.
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Carboxyamidotriazole
0 ImagesSynonyms: L-651582; CAICarboxyamidotriazole (L-651582) is an orally active cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole inhibits NF-κB, MAPK activation and NO production. Carboxyamidotriazole has anti-angiogenic and anti-inflammatory activities. Carboxyamidotriazole has anticancer activity against liver cancer, lung cancer and leukemia.
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Manidipine
0 ImagesManidipine 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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REM127
0 ImagesREM127 is an orally active, blood-brain barrier-penetrant septin 6/7 molecular glue degrader. REM127 binds to SEPT6 with high affinity and promotes the assembly of SEPT2/6/7 cortical filaments, thereby normalizing cytoplasmic calcium levels, cerebrospinal fluid hyperphosphorylated tau protein levels, synaptic function and cognitive function. REM127 can be used in research related to Alzheimer's disease.
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Tetracaine hydrochloride
0 ImagesTetracaine hydrochloride (Amethocaine hydrochloride) is a calcium channel protein inhibitor and blocks voltage-sensitive release of Ca2+ from sarcoplasmic reticulum. Tetracaine hydrochloride is mainly used topically in ophthalmology and as an antipruritic.
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3,5,7,3′,4′-Pentamethoxyflavone
0 Images3,5,7,3’,4’-Pentamethoxyflavone is a Ca2+ channel inhibitor. 3,5,7,3’,4’-Pentamethoxyflavone can protect DNA from oxidative damage. 3,5,7,3’,4’-Pentamethoxyflavone can induce relaxation of the human corpus cavernosum through calcium mobilization-related mechanisms. 3,5,7,3’,4’-Pentamethoxyflavone can promote the expression of eNOS and cystathionine gamma lyase CSE proteins in middle-aged male rats and regulate vascular function. 3,5,7,3’,4’-Pentamethoxyflavone can be used in research related to diabetes and cardiovascular diseases.
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Fendiline
0 ImagesFendiline, a diphenylalkylamine type of antianginal agent, is an L-type calcium channel blocker (IC50 of 17 µM). Fendiline is also a selective K-Ras inhibitor, and has no effect on H-Ras and N-Ras. Fendiline inhibits K-Ras plasma membrane localization (IC50 of 9.64 μM), inhibits K-Ras signal output and blocks the proliferation of pancreatic, colon, lung, and endometrial cancer cell lines expressing oncogenic mutant K-Ras. Fendiline is a STING agonist and is able to inhibit the growth of multiple refractory cold tumors (MC38, CT26 and B16F10).
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Dihydrocytochalasin B
0 ImagesDihydrocytochalasin B is an Actin disruptor. Dihydrocytochalasin B disrupts actin microfilament bundles, inhibits actin polymerization, and alters intracellular actin cytoskeletal structures. Dihydrocytochalasin B blocks the initiation of DNA synthesis. Dihydrocytochalasin B inhibits Calcium transport. Dihydrocytochalasin B inhibits cytokinesis and alters cell morphology. Dihydrocytochalasin B can be used in studies related to rickets.
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Ifenprodil
0 ImagesSynonyms: NP-120; RC-61-91Ifenprodil (NP-120), a cerebral vasodilator, is a noncompetitive NMDA receptor antagonist. Ifenprodil exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM). Ifenprodil is an α1 adrenergic receptor antagonist. Ifenprodil inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil has reliable inhibitory effects against A/H1N1 strains (EC50 of 6.6 µM). Ifenprodil has neuroprotective, anticonvulsant and antinociceptive effects. Ifenprodil can be used for the study of cerebrovascular diseases and peripheral arterial obliterative disease.
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Reldesemtiv
0 ImagesSynonyms: CK-2127107Reldesemtiv (CK-2127107) is a selective, orally active and next-generation fast skeletal muscle troponin activator (FSTA). Reldesemtiv selectively activates fast skeletal myofibrils with an EC50 of 3.4 μM. Reldesemtiv increases exercise performance in a heart failure model.
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MRS1845
0 ImagesMRS1845 is a selective store-operated calcium (SOC) channel inhibitor with an IC50 of 1.7 μM. MRS1845 is an ORAI1 inhibitor. MRS1845 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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Demethylsuberosin
0 ImagesSynonyms: 7-DemethylsuberosinDemethylsuberosin (7-Demethylsuberosin) is a coumarin compound found in Angelica gigas Nakai. Demethylsuberosin exerts antihypertensive effects by inhibiting the L-type CaV1.2 channel. Demethylsuberosin has antioxidant and anti-inflammatory activities. Demethylsuberosin also exhibits neuroprotective activities against glutamate-induced toxicity in primary cultured rat cortical cells.
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Calenduloside E
0 ImagesCalenduloside E is a pentacyclic triterpenoid saponin that can be extracted from the bark and roots of Aralia ovata, and has anti-inflammatory and anti-apoptotic activities. Calenduloside E alleviates atherosclerosis by regulating macrophage polarization, improves mitochondrial function by regulating the AMPK-SIRT3 pathway, and alleviates acute liver injury. In addition, Calenduloside E promotes the interaction between L-type calcium channels and Bcl-2 related apoptosis genes, inhibits calcium overload, and alleviates myocardial ischemia/reperfusion injury. Calenduloside E also improves non-alcoholic fatty liver disease by regulating heat shock-dependent pathways, and inhibits ROS mediated JAK1-STAT3 pathways to reduce cellular inflammatory responses.
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Carbamazepine (Standard)
0 ImagesSynonyms: CBZ (Standard); NSC 169864 (Standard)Carbamazepine (Standard) is the analytical standard of Carbamazepine. This product is intended for research and analytical applications. Carbamazepine is an orally active pressure-sensitive sodium ion channel blocker with an IC50 of 131 μM. Carbamazepine blocks voltage gated Na+, Ca2+, and K+ channels, and is also a HDAC inhibitor (IC50: 2 μM). Carbamazepine is an anticonvulsant and can be used for research of epilepsy and neuropathic pain.
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Nelutroctiv
0 ImagesSynonyms: CK-136Nelutroctiv (CK-136) is an orally active and selective cardiac troponin activator. Nelutroctiv activates cardiac sarcomeres by enhancing the sensitivity of troponin to calcium ions and promoting the interaction between actin and myosin. Nelutroctiv enhances cardiac contractility. Nelutroctiv can be used in the researches for cardiovascular diseases with impaired cardiac contractile function.
