Calcium Channel

Thapsigargin is a natural product, an inhibitor of sarcoplasmic endoplasmic reticulum Ca2+ ATPase (SERCA) and an endoplasmic reticulum stress inducer. Thapsigargin increases cytoplasmic calcium concentration by blocking the ability of cells to pump calcium into the sarcoplasmic and endoplasmic reticulum.

Ionomycin is an calcium ionophore and an antibiotic that binds calcium ions (Ca2+). It is produced by the bacterium Streptomyces conglobatus.It is used in research to raise the intracellular calcium level (Ca2+) and as a research tool to understand Ca2+ transport across biological membranes. Ionomycin promotes apoptosis and induces the activation of protein kinase C (PKC).

Jamaicin (AnCoA4), an isoflavone derived from the chickweed plant, is an inhibitor of the STIM1-Orai1 channel that blocks calcium influx, reduces its interaction with STIM1, and inhibits T-cell activation.

EMD57033 is a cardiac troponin C (cTnC) activator, a dominant Ca2+ sensitizer, which functions by binding to cardiac slow skeletal troponin C heterodimers to promote cardiac contraction.

Ziconotide Acetate (107452-89-1 free base) (Prialt) is an analgesic agent and has been used to treat neuropathic and non-neuropathic pain. Ziconotide Acetate (107452-89-1 free base) acts by binding to N-type calcium channels situated on the terminal part of primary afferent neurons of the nociceptive pathway therefore reducing synaptic transmission with potent antinociceptive effects.

Sulcardine sulfate (B-87823) is a multi-ion channel blocker with antiarrhythmic activity, inhibits Na+, K+ and Ca2+ channels, and inhibits hNav1.5 channels in a concentration-dependent and reversible manner.

Iganidipine（NKY 722） is a new water-soluble Ca2+ antagonist with antihypertensive activity for research and neurological related diseases.

Verapamil (CP-16533-1) is a calcium channel blocker and an orally active and effective inhibitor of P-gp. Verapamil inhibits CYP3A4 and can be used in studies about the treatment of high blood pressure, heart arrhythmias, and angina research.

Azumolene (EU4093 free base)

Ebselen (CCG-39161) is a organoselenium compound with anti-inflammatory, anti-oxidant and cytoprotective activity. Ebselen acts as a glutathione peroxidase mimetic and is thereby able to prevent cellular damage induced by reactive oxygen species (ROS). In addition, this agent inhibits the activity of a variety of enzymes including nitric oxide synthase (NOS), 5-lipoxygenase, cyclooxygenase, protein kinase C (PKC), NADPH oxidase and gastric H+ K+-ATPase. Furthermore, ebselen may be neuroprotective due to its ability to neutralize free radicals upon NMDA receptor activation thus, reducing lipoperoxidation mediated by glutamate-induced excitotoxicity.

AY 77 (Unk-Cha-Chg-NH2) is a potent and selective PAR2 agonist. AY 77 showed selectivity for Ca2+ and ERK1/2 signaling (ec50 value of Ca2+ release was 40 nM and ec50 value of ERK1/2 phosphorylation was 2 μM). AY 77 can promote migration of human breast cancer cells in vitro.

Halofuginone specifically inhibits collagen type I gene expression and matrix metalloproteinase 2 (MMP-2) gene expression, which may result in the suppression of angiogenesis, tumor stromal cell development, and tumor cell growth. Halofuginone Hydrobromide is the hydrobromide salt of halofuginone, a semisynthetic quinazolinone alkaloid anticoccidial derived from the plant Dichroa febrifuga, with antifibrotic and potential antineoplastic activities. These effects appear to be due to halofuginone-mediated inhibition of the collagen type I and MMP-2 promoters. Collagen type I and MMP-2 play important roles in fibroproliferative diseases.

DS16570511 is a novel, cell-permeable inhibitor targeting the mitochondrial calcium uniporter. It effectively blocks the increase in Ca2+ influx dependent on MCU or MICU1 [1].

Nepetin (6-Methoxyluteolin) has antioxidant activity, it is a potent inhibitor of histamine release and calcium influx via down-regulation of the FcεRI α chain.

Opc 8490 is a cardiotonic agent and a positive inotropic vasodilator that increases Ca current (ICa) in a dose-dependent and reversible manner and prolongs atrial action potential in a concentration-dependent manner.

CERM-11956 is a beprudil derivative and an anti-ischemic agent with Ca2+ cardioprotective effects and induces negative inotropic effects.

Felodipine (CGH-869) is a longlasting 1, 4-dihydropyridine calcium channel repressor.

Bryonolic acid (20-epi-Bryonolic acid), a triterpenoid extracted from Sandoricum indicum, possesses immunomodulatory, anti-inflammatory, antioxidant and anticancer activities and protects PC12 cells from NMDA-induced apoptosis by inhibiting Ca2+ in-flux and modulating gene expression in the Ca2+-CaMKII-CREB signalling pathway.

Isradipine (PN 200-110) is a dihydropyridine calcium channel blocker with antihypertensive and vasodilator activities. Isradipine blocks calcium entry through calcium ion channels in coronary and peripheral vascular smooth muscle, dilating coronary arteries and peripheral arterioles. This action increases oxygen delivery by enhancing blood flow and decreases oxygen requirements by reducing total peripheral resistance.

Yangambin is a selective antagonist of the cardiovascular effects of platelet activating factor (PAF); it has hypotensive effect, which is probably due to a peripheral vasodilatation that involves, at least, the inhibition the Ca2+ influx through voltage-gated Ca2+ channels. Yangambin also has central nervous system activity.

FPL-62129 is a calcium channel antagonist and a novel angiotensin-converting enzyme inhibitor with vasodilator activity for the study of cardiovascular disease.

McN5691 (RWJ26240) is a voltage-dependent calcium channel blocker with antihypertensive activity that can be used in the study of diseases caused by vascular smooth muscle abnormalities.

Monatepil maleate (AJ-2615 maleate) is an orally active Ca2+-channel and α1-adrenoceptor antagonist and non-competitive heparanoyl-coenzyme A:cholesterol acyltransferase (ACAT) inhibitor with antihypertensive activity.Monatepil maleate is used in studies of hyperlipidemia and atherosclerosis. Monatepil maleate is used to study hyperlipidemia and atherosclerosis.

TTA-A2 is a selective T-type calcium channel antagonist as a potent anticonvulsant that the Cav3.1 isoform plays a prominent role in mediating. TTA-A2 is equally potent against the Cav3.1 (a1G) and Cav3.2 (a1H) channels with IC50 values of 89 nM and 92 nM, respectively, at -80 and -100 mV holding potentials. TTA-A2 can be used for the research of a variety of human neurological diseases, including sleep disorders and epilepsy.

KT-362 fumarate is a novel compound that acts as an antagonist of calcium channels, potassium channels and sodium channels.KT-362 fumarate causes vasodilation by affecting intracellular calcium mobilization in atrial muscle cells.KT-362 fumarate has a relaxing effect on femoral and basilar artery strips in rabbits.

Nicardipine (Cardene), a calcium channel blockers belonging to the dihydropyridine class, is a drug used to treat angina and high blood pressure.

Bay K 8644 (SQ 28,873) is a potent, selective activator of L-type Ca2+ channel with IC50 of 17.3 nM.

Caldaret HCl is an intracellular Ca2+ modulator that regulates calcium homeostasis at the sarcoplasmic reticulum and cell membrane, and can be used to study acute myocardial infarction and heart failure.

Temiverine hydrochloride is a potential calcium channel antagonist with anticholinergic effects that inhibits some of the functions of atropine.

Tiapamil hydrochloride (Ro 11-1781 hydrochloride) is a calcium channel blocker with antihypertensive activity and may be used in the study of angina and cardiovascular disease.

Levosemotiadil（SA 3212） is a novel calcium antagonist and a very potent inhibitor of low-density lipoprotein oxidation.Levosemotiadil may be used to prevent lethal cardiac arrhythmias.

Sipatrigine (619C89) is an antiepileptic compound with neuroprotective activity through glutamate release, TREK ion channels, TRESK channels, sodium channels, and calcium channel inhibitors in the CNS, and can be used to study TRESK channels.

Physalin F is a natural blocker of CaV2.3 (R-type) and CaV2.2 (N-type) voltage-gated calcium channels.It is a secosteroid with potent anti-inflammatory and immunomodulatory activities. Physalin F induces apoptosis of PBMC, decreasing the spontaneous proliferation and cytokine production caused by Human T-lymphotropic virus type 1 (HTLV-1) infection

Acetylcholine Chloride is the chloride salt form of acetylcholine, a synthetic, quaternary amino alcohol with cholinergic properties. Acetylcholine chloride (Pilofrin) mimics the parasympathomimetic effect of the endogenous compound acetylcholine. Administered as an ophthalmic solution, this drug stimulates the cholinoceptors in the sphincter muscle of the iris, causing the pupil to constrict.

Zegocractin (CM-4620) is an inhibitor of calcium-release activated calcium (CRAC) channels.

Tanshinone IIA sulfonate sodium (Tanshinone IIA sodium sulfonate) is a water-soluble derivative of tanshinone IIA extracted from Savia miltiorrhiza; a potent negative allosteric modulator of the human purinergic receptor P2X7. Tanshinone IIA sulfonate sodium (12.5 μM) inhibits hypoxia-induced PKG and PPAR-γ downregulation in PASMCs and distal pulmonary arteries of rats.

Ginsenoside Ro (Chikusetsusaponin V) can reduce TXA2 production, weakly reduce COX-1 and TXAS activities, and has antiplatelet effects as a Ca2+ antagonist with an IC50 of 155 μM.

CDN1163 is a small molecule activator of sarco/endoplasmic reticulum Ca2+-ATPase (SERCA).

GSK1016790A (GSK101) (GSK101) is a novel, potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34 nM in choroid plexus epithelial cells.

Ruthenium Red (Ammoniated ruthenium oxychloride) is a polycationic dye widely used for electron microscopy (EM) of cells, tissues and vegetative bacteria. Ruthenium red strongly reacts with phospholipids and fatty acids and binds to acidic mucopolysaccharides. Ruthenium red is a L-type calcium current (ICa) blocker, blocks Ca2+ uptake and release, and voltage-sensitive Ca2+ channels

2-Aminoethyl diphenylborinate (2-APB) is a chemical compound that inhibits IP3 receptors and TRP channels, though it activates TRPV1, TRPV2, and TRPV3 at higher concentrations.

SKF-96365 hydrochloride (SKF96365) , a SOCE inhibitor, exhibits potent anti-neoplastic activity by inducing cell-cycle arrest and apoptosis in colorectal Y cells. SKF-96365 hydrochloride can induce cytoprotective autophagy to delay apoptosis by preventing the release of cytochrome c (cyt c) from the mitochondria into the cytoplasm. Mechanistically, SKF-96365 hydrochloride treatment inhibited the calcium calmodulin-dependent protein kinase IIγ (CaMKIIγ) AKT signaling cascade in vitro and in vivo. Overexpression of CaMKIIγ or AKT abolished the effects of SKF-96365 on Y cells, suggesting a critical role of the CaMKIIγ AKT signaling pathway in SFK-96365-induced biological effects. SKF-96365 hydrochloride inhibited hERG current in a concentration-dependent manner.

Halofuginone (RU-19110), the competitive inhibitor of prolyl-tRNA synthetase(Ki=18.3 nM), could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng ml in the mammal.

Fluspirilene (R 6218) is a non-competitive L-type calcium channel antagonist (IC50: 0.03 μM).Fluspirilene is a long-acting antipsychotic compound used in the treatment of schizophrenia.

Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.

Fasudil hydrochloride (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively.

Ethacrynic acid (Edecrin) is a nonsulfonamide loop diuretic that inhibits the activity of the Na+ K+ 2Cl- cotransporter NKCC2 in the thick ascending limb of the loop of Henle. It also inhibits glutathione S-transferase and Wnt signalling, producing cytotoxicity in chronic lymphocytic leukaemia cells and other tumour cells.

SB-237376 HCl (SB-237376 hydrochloride) is a calcium and potassium channel antagonist used in the treatment of cardiac arrhythmias.