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Calcium/Sodium Channel Blocker
Elpetrigine is a potent calcium and sodium channel blocker with significant anticonvulsant, antidepressant, antimania, and anxiolytic properties. This compound is primarily utilized in research focused on epilepsy and bipolar disorder, contributing to the understanding of neurological and mood disorders. Its mechanism of action makes it a valuable tool for exploring therapeutic avenues in these conditions. -
Calcium Channel Antagonist
Palonidipine hydrochloride is a calcium channel antagonist that selectively inhibits L-type calcium channels. It demonstrates potential therapeutic effects in the management of angina pectoris and hypertension. This compound is useful in research applications aimed at investigating cardiovascular diseases and calcium signaling pathways. -
Calcium Channel Blocker
(R)-Lercanidipine hydrochloride is an R-enantiomer of Lercanidipine, functioning primarily as a calcium channel blocker. This compound exhibits vasodilatory effects, making it useful in the research of hypertension and cardiovascular disorders. Its ability to inhibit calcium influx into vascular smooth muscle cells contributes to its therapeutic potential in managing blood pressure. -
Antiarrhythmic Agent
CPU-228 is a complex class III antiarrhythmic agent primarily targeting the rapid component of the delayed rectifier potassium channel (IKr) and L-type calcium channel (ICa,L). It exhibits concentration-dependent inhibition of ICa,L with an IC50 of 0.909 μM. Biological assays demonstrate that CPU-228 generates negative inotropic effects and induces a mild, non-frequency-dependent prolongation of the effective refractory period (ERP) in isolated left atrial tissues. Additionally, CPU-228 is effective in reducing the incidence of torsades de pointes in anesthetized rabbits and inhibits ischemia/reperfusion-induced arrhythmias in rats, making it a valuable tool for research on arrhythmias and cardiac electrophysiology. -
Calcium Channel Ligand
(Rac)-PD0299685 is a ligand targeting the calcium channel α2δ subunit, known for its role in modulating calcium ion influx. This compound has shown significant efficacy in reducing daily worst pain severity in interstitial cystitis patients during a phase IIa clinical trial. Additionally, (Rac)-PD0299685 serves as a potent voltage-dependent calcium channel inhibitor, making it a valuable tool for researching retina-related diseases and their underlying mechanisms. -
Calcium Channel Blocker
Tamolarizine is a calcium channel blocker that effectively crosses the blood-brain barrier to antagonize calcium's influence on neuronal activity. This compound is instrumental in studying neurological processes and provides valuable insights into calcium's role in various nervous system functions. Researchers may utilize Tamolarizine to investigate its impact on neuronal excitability and potential therapeutic applications in neurodegenerative conditions. -
Stable Isotope
1-Octanol-d2 is the deuterium-labeled version of 1-Octanol, a saturated fatty alcohol that serves as an inhibitor of T-type calcium channels (T-channels), exhibiting an IC50 of 4 μM for native T-currents. Its unique chemical properties make it a valuable tool for studying calcium channel modulation and its implications in various physiological processes. Additionally, 1-Octanol is noted for its potential as a biofuel with diesel-like characteristics, offering insights into alternative energy applications. -
N-type Calcium Channel Antagonist
PD 175069 is a selective antagonist of N-type calcium channels, exhibiting an IC50 of 0.32 μM. It demonstrates effective inhibition in an audiogenic seizure model with DBA/2 mice, highlighting its potential in the study of neurological conditions. PD 175069 is valuable for research into neuropathic pain and stroke, providing insights into calcium channel modulation in these disorders. -
Calcium Channel Inhibitor
Pincainide is a calcium channel inhibitor that specifically targets voltage-gated calcium channels in smooth muscle. It effectively reduces calcium influx, leading to the inhibition of norepinephrine- and high potassium-induced contractile responses. Pincainide is relevant in the study of cardiovascular diseases, providing insights into mechanisms related to smooth muscle function and regulation. -
Ca2+ Channel Blocker
(R)-Lercanidipine-d3 hydrochloride is a deuterium-labeled derivative of (R)-Lercanidipine, functioning primarily as a calcium channel blocker. This compound selectively inhibits L-type calcium channels, thereby reducing intracellular calcium influx. Its key biological activity makes it a valuable tool for research on cardiovascular disorders, hypertension, and related therapeutic areas. -
Cavα2δ1/NET Inhibitor
Cavα2δ1&NET-IN-3 is a selective inhibitor targeting the α2δ subunit of voltage-gated calcium channels (VGCC) and the noradrenaline transporter (NET). This compound exhibits inhibitory constants (Kis) in the range of 100-500 nM for the human α2δ-1 subunit of the Cav2.2 calcium channel and for NET. Cavα2δ1&NET-IN-3 is utilized in research applications focused on pain modulation and neurotransmitter regulation, contributing to the understanding of various neurological disorders. -
Calcium Antagonist
Naltiazem hydrochloride is a thiazepinone calcium antagonist that primarily targets calcium channels. It is known for its ability to inhibit platelet aggregation both in vitro and in vivo, making it a valuable tool in cardiovascular research. This compound is often utilized to investigate mechanisms underlying platelet function and cardiovascular diseases. -
SERCA Blocker
JTV-519 is a calcium-dependent blocker of sarcoplasmic reticulum Ca2+-stimulated ATPase (SERCA) and serves as a partial agonist of ryanodine receptors in striated muscle. This compound exhibits antiarrhythmic and cardioprotective properties, making it valuable for research into cardiac function and arrhythmia prevention. JTV-519 is utilized in studies investigating the modulation of calcium signaling and its implications for cardiovascular health. -
IDHP Isomer
(R)-IDHP is an isomer of isovaleryl-DL-3-hydroxybutyric acid, functioning primarily by inhibiting Ca2+ release and modulating Ca2+ inward flow in both voltage-dependent and receptor-operated calcium channels in vascular smooth muscle cells. This compound exhibits vasorelaxant properties and is valuable in research focused on cardiovascular disease mechanisms and treatments. Its biological activity makes it a useful tool for investigating vascular dynamics and related pathophysiological conditions. -
α9α10 nAChR/CaV2.2 Antagonist
GeX-2 is a truncated analogue of αO-conotoxin that serves as an antagonist of the α9α10 nicotinic acetylcholine receptor (nAChR) and CaV2.2 channels. This compound demonstrates significant analgesic properties, effectively alleviating pain in rat models exhibiting chronic constriction injury. GeX-2 is valuable in research focusing on pain mechanisms and the modulation of excitatory neurotransmission through its interactions with nAChR and calcium channels. -
Calcium Channel inhibitor
Calcium Channel Antagonist 4 is a potent inhibitor of voltage-gated calcium channels, exhibiting an IC50 value within the range of 5-20 μM. This compound's ability to selectively block calcium influx makes it a valuable tool for studying calcium signaling pathways in various cellular processes. It is particularly useful in research applications related to neurology, cardiology, and muscle physiology. -
Calcium Channel Blocker
RWJ 22108 is a bronchoselective calcium channel blocker that inhibits calcium influx in smooth muscle cells, demonstrating an IC50 value of 5.7 nM in the calcium-dependent contraction of canine bronchiolar smooth muscle. This compound is primarily utilized in research applications focused on respiratory physiology and the study of bronchial hyper-reactivity. Its specificity for bronchial tissues makes it a valuable tool in exploring mechanisms of airway relaxation and potential therapeutic interventions for respiratory disorders. -
α-Obscurine Derivative
α-Obscurine derivative-1 is a derivative of α-Obscurine that specifically targets CaV3.1 ion channels, exhibiting an inhibitory effect with an IC50 of 0.19 μM. This compound is valuable for research into neurological disorders, providing insights into calcium channel modulation and its implications in neurological function. Its unique properties make it a useful tool for exploring the role of ion channels in various pathophysiological conditions. -
Calcium Antagonist
SL-870495 is a calcium antagonist that selectively targets L-type calcium channels. It exhibits significant potential in investigating cardiovascular diseases, particularly hypertension and angina pectoris, by regulating calcium influx in cardiac and vascular smooth muscle cells. This compound is valuable for research applications aimed at understanding calcium-mediated mechanisms in cardiovascular pathology. -
Calcium Channel Blocker
Diproteverine hydrochloride is a calcium channel blocker that primarily targets L-type calcium channels, inhibiting calcium influx into cells. This compound exhibits significant antianginal properties, making it useful in research related to cardiovascular diseases. Additionally, studies have indicated that Diproteverine hydrochloride may have implications in embryonic toxicity assessment, highlighting its relevance in developmental biology research. -
Calcium Channel Ligand
PD-217014 is an α2δ ligand targeting calcium channels, demonstrating significant visceral analgesic activity. This compound effectively inhibits visceral hypersensitivity reactions, exhibiting a dose-dependent anti-allodynic effect. It serves as a valuable tool in research related to pain management and the mechanisms underlying visceral pain. -
Calcium Channel Blocker
Bencyclane fumarate is a potent vasodilating calcium channel blocker. It has demonstrated efficacy in attenuating mucosal damage in a rat model of intestinal ischemia-reperfusion injury. This compound serves as a valuable tool for research into peripheral arterial occlusive diseases and related vascular conditions. -
SERCA Inhibitor
CXL 017 is a selective inhibitor of the sarco/endoplasmic reticulum Ca2+-ATPase (SERCA), functioning by competing with ATP for binding and thereby inhibiting ATPase activity. This compound demonstrates notable cytotoxicity specifically against multidrug-resistant acute myeloid leukemia cells, such as HL60/MX2. CXL 017 is valuable in research related to multidrug-resistant acute myeloid leukemia and offers insights into potential therapeutic approaches for overcoming drug resistance in cancer. -
Calcium Channel Antagonist
AH-1058 is a potent calcium channel antagonist primarily targeting L-type Ca2+ channels. This compound exhibits significant antiarrhythmic activity by effectively delaying premature ventricular complexes and preventing ventricular fibrillation in experimental arrhythmia models. AH-1058 has shown efficacy in suppressing ventricular tachycardia and ventricular fibrillation in reperfusion-induced arrhythmia models, making it a valuable tool for research in cardiac arrhythmias and related therapeutic approaches. -
Calcium Antagonist
S-312 is a calcium antagonist characterized by a bicyclic dihydrothienopyridine structure. This compound effectively relaxes helical strips of isolated rabbit arteries that have been pre-contracted with high potassium depolarization. S-312 acts as a competitive inhibitor of calcium-induced contractions in depolarized basilar and femoral arteries, and it also prolongs AV nodal conduction time in Langendorff-perfused isolated rabbit hearts. Additionally, S-312 demonstrates vasculoselectivity, particularly targeting cerebral vessels, making it a valuable tool for cardiovascular research applications. -
Calcium Channel Inhibitor
A-1048400 is a selective calcium channel inhibitor that demonstrates potent activity against N-type and T-type calcium channels, with IC50 values of 1.4 μM and 1.2 μM, respectively. By inhibiting neurotransmitter release and reducing membrane hyperexcitability, A-1048400 exhibits significant analgesic properties. This compound is particularly valuable for investigating mechanisms and treatments related to neuropathic pain, such as that resulting from spinal nerve ligation and chronic constriction injury. -
Calcium Channel Antagonist
FPL 62129 is a calcium channel antagonist that exhibits significant vasodilatory effects. It is effective in reducing blood pressure and total peripheral resistance while enhancing cardiac contractility and cardiac output in anesthetized beagle models. This reagent is valuable for research applications focusing on cardiovascular physiology and the modulation of vascular tone. -
Calcium Antagonist
MCI-176 is a calcium antagonist that selectively inhibits calcium-induced constriction in coronary arteries. This compound demonstrates significant capacity to modulate vascular tone, making it valuable for studying cardiovascular function and related pathologies. MCI-176 is particularly useful in research focusing on the mechanisms of calcium signaling and potential therapeutic interventions for coronary artery diseases. -
Cav3.2 Inhibitor
Cav 3.2 inhibitor 3 is a selective inhibitor of the Cav3.2 T-type calcium channel, exhibiting an IC50 of 0.1534 μM. This compound demonstrates minimal binding affinity for D2 receptors, making it a valuable tool for studying the role of Cav3.2 channels in various physiological processes. Its use is particularly relevant in research areas focused on neuronal excitability and pain modulation. -
Antitumor Compound
S 16317 is an orally active dihydropyridine derivative that demonstrates low affinity for calcium channels (Ki: 0.55 μM). It effectively inhibits P-glycoprotein-mediated efflux of doxorubicin (ADR), thus potentially reversing multidrug resistance in tumor cells. This compound is particularly relevant for research in cancer biology and the development of novel therapeutic strategies against resistant tumors. -
Calcium Channel Inhibitor
TTA-P1 is a potent inhibitor of human T-type calcium channels, exhibiting state-independent characteristics. This compound is crucial for studying various physiological processes such as neuronal burst firing, hormone secretion, and cell proliferation. TTA-P1 is particularly valuable for research related to absence epilepsy and other neurological disorders linked to calcium signaling. -
N-type Calcium Channel Antagonist
Huwentoxin XVI is a selective antagonist of N-type calcium channels, demonstrating a potent inhibitory effect with an IC50 of approximately 60 nM. Derived from the Chinese tarantula Ornithoctonus huwena, it serves as an analgesic and exhibits no activity against voltage-gated T-type calcium channels, potassium channels, or sodium channels. This specificity makes Huwentoxin XVI valuable in research aimed at understanding pain mechanisms and the role of calcium channels in various physiological processes. -
T-type Calcium Channel Antagonist
TTA-A8 is a potent T-type calcium channel antagonist, demonstrating an IC50 value of 31.3 nM in the FLIPR depolarization assay. This compound exhibits favorable pharmacokinetic properties, making it an ideal candidate for research applications focused on epilepsy and sleep disorders. Its short-acting profile allows for detailed studies into the physiological roles of T-type calcium channels in related conditions. -
Broad-Spectrum Antiepileptic Agent
JNJ-26990990 is a broad-spectrum antiepileptic agent that primarily targets voltage-gated sodium channels and N-type calcium channels. It exhibits significant anticonvulsant activity, making it suitable for the study of various seizure models. Although it shows minimal inhibition of human carbonic anhydrase-II with an IC50 of 110 μM, its primary applications lie in the investigation of epilepsy and related neurological disorders. -
Antihypertensive Agent
Vatanidipine hydrochloride is an orally active dihydropyridine (DHP) calcium channel blocker that primarily functions as an antihypertensive agent. It exhibits vasodilatory effects, resulting in reduced vascular resistance, and additionally inhibits the release of noradrenaline from sympathetic nerve endings. This dual action makes Vatanidipine hydrochloride valuable in research related to hypertension and cardiovascular health. -
Calcium Channel Inhibitor
Agelenin is a polypeptide composed of 35 amino acids, functioning primarily as a calcium channel inhibitor. Isolated from the Agelena opulenta spider, this compound exhibits structural similarity to insect-specific calcium channel inhibitors, making it a valuable tool for studying calcium signaling pathways. Research applications include investigations into neuromuscular transmission and calcium-dependent cellular processes. -
Sodium/Calcium Channel Blocker
KT 2-230 is a sodium and calcium channel blocker that exhibits significant anti-inflammatory properties. This compound is utilized in research applications focused on neuropathic pain and various inflammatory conditions. Its ability to modulate ion channel activity makes it a valuable tool for studying the underlying mechanisms of synaptic transmission and neuroprotection. -
L-/T-type Calcium Channel Inhibitor
HM12 is a covalent inhibitor targeting L-/T-type calcium channels, specifically Cav1.2 and Cav3.2, while demonstrating selectivity for N-type channels. This compound induces irreversible inhibition that remains effective post-washout, making it a valuable tool for investigating calcium channel dynamics. HM12 is applicable in research focused on various diseases, including hypertension, pain, and epilepsy, facilitating the exploration of calcium channel modulation in therapeutic contexts. -
Ca2+ Channel α2δ Ligand
PD-0299685 is a potent ligand for the Ca2+ channel α2δ subunit. This compound exhibits significant potential in the study of refractory genito-urinary pain conditions, including interstitial cystitis and bladder pain syndrome. Its ability to modulate calcium channel activity makes it a valuable tool in pain research and related therapeutic investigations. -
Calcium Antagonists
KT-362 free acid is an intracellular calcium antagonist that exhibits antiarrhythmic and vasodilatory properties. It antagonizes norepinephrine-induced vasoconstriction by reducing inositol phospholipid hydrolysis, leading to decreased intracellular calcium mobilization. This reagent is suitable for investigating the mechanisms of contraction and relaxation in vascular smooth muscle, particularly the roles of intracellular calcium dynamics and inositol phospholipid pathways in vascular contraction. -
Calcium Channel Blocker
RS-5773 is a calcium channel blocker that acts as a congener of diltiazem. This compound exhibits antianginal properties and is distinguished by its minimal impact on hypotension and atrioventricular conduction, making it suitable for cardiovascular research. RS-5773 can be utilized in studies focused on calcium dynamics in cardiac function and related therapeutic applications. -
Ca2+-Channel Antagonist
Monatepil maleate is a potent orally active calcium channel antagonist that functions as a noncompetitive ACAT inhibitor. It has demonstrated the ability to decrease blood pressure and enhance plasma lipid metabolism. This compound shows promise for research applications related to hyperlipidemia and cardiovascular health. -
Calcium Antagonist
Semotiadil is a benzothiazine compound that functions as a calcium antagonist. It demonstrates significant antiplatelet activity, making it valuable for research into cardiovascular diseases and thrombotic disorders. Semotiadil can be used to explore mechanisms related to calcium signaling and its role in platelet function and aggregation. -
Calcium Channel Blocker
Nicardipine-d3 hydrochloride is a deuterium-labeled analog of Nicardipine hydrochloride, a potent calcium channel blocker. It effectively inhibits cardiac calcium channels, exhibiting an IC50 of 1 μM. This compound is utilized in research related to cardiovascular diseases, particularly for studying conditions such as chronic stable angina and hypertension management. -
Calcium Channel Inhibitor
ω-Hexatoxin-Hv1a is a selective inhibitor of L-type voltage-dependent calcium channels. This neurotoxin reduces intracellular calcium ion concentration, thereby mitigating apoptosis, necroptosis, and oxidative stress, while enhancing cellular recovery and energy levels. Its ability to induce paralysis and mortality in insects through the disruption of central nervous system neurotransmission underscores its potency, although it has limited oral toxicity. Consequently, ω-Hexatoxin-Hv1a is a valuable tool for research into ischemia-reperfusion injury, atopic dermatitis, and ischemic damage in cardiomyocytes and neurons. -
Calcium Channel Antagonist
UK 52831 is a long-acting dihydropyridine calcium channel antagonist that selectively inhibits calcium influx through L-type calcium channels. This compound exhibits significant cardiovascular activity, making it valuable for research into conditions such as hypertension and myocardial ischemia. Additionally, UK 52831 has potential applications in anti-inflammatory studies, providing insights into the role of calcium signaling in inflammatory processes. -
Calcium/Sodium Channel Blocker
LY393615 (NCC1048) is a selective blocker of neuronal calcium (Ca2+) and sodium (Na+) channels, demonstrating IC50 values of 1.9 μM and 5.2 μM for the α1A and α1B calcium channel subunits, respectively. This compound exhibits excellent brain penetration and displays neuroprotective effects in cerebral ischemia models, making it a valuable tool for research in neurological diseases. Its dual-channel blocking mechanism contributes to its potential applications in understanding neuronal excitability and neuroprotection. -
Calcium Channel Blocker
Leualacin is a calcium channel blocker derived from the fungus Hapsidospora irregularis. This compound demonstrates significant inhibition of calcium influx through voltage-gated calcium channels, leading to potential therapeutic effects in conditions characterized by excitability and muscle contraction disorders. It is applicable in research exploring cardiovascular function and neurophysiology, providing insights into calcium signaling pathways. -
Calcium Channel
Semotiadil recemate fumarate is a vasoselective Ca2+ channel antagonist that inhibits calcium influx in vascular smooth muscle cells. It primarily targets L-type calcium channels, leading to vasodilation and reduced vascular resistance. This compound is significant in research related to cardiovascular diseases and may offer therapeutic insights into hypertension and related conditions. -
T-Type Calcium Channel Inhibitor
T-Type Calcium Channel Inhibitor 2 is a selective inhibitor of T-type calcium channels, specifically targeting Cav3.1 (α1G), Cav3.2 (α1H), and Cav3.3 (α1I), with IC50 values of 31.0, 83.1, and 69.3 µM, respectively. This compound exhibits significant cytotoxic activity against A549 and HCT-116 cancer cell lines, with IC50 values of 5.0 and 6.4 µM. It serves as a useful tool in the investigation of calcium channel involvement in various physiological processes and potential therapeutic targets in cancer research.

