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Catalog No.
Product Name
Application
Product Information
Citations
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Calcium Channel inhibitor
Nimodipine is a L-type Ca2+ channel blocker.- Shiqian Han, .et al. , iScience, 2023, Apr 8;26(5):106613 PMID: 37128603
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Ca2+ channel agonist/CDK2 inhibitor
Ca2+ channel agonist 1 is an agonist of N-type Ca2+ channel and an inhibitor of Cdk2, with EC50s of 14.23 μM and 3.34 μM, respectively, and is used as a potential treatment for motor nerve terminal dysfunction. -
Calcium channel proteins inhibitor
Dantrolene sodium is a inhibitor of calcium channel proteins, inhibiting the release of Ca2+ from the sarcoplasm. Dantrolene sodium is a skeletal muscle relaxant which acts by blocking muscle contraction beyond the neuromuscular junction. -
elastogenesis inhibitor
L-Ascorbic acid sodium salt (Sodium L-ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid sodium salt inhibits selectively 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. -
SOCE inhibitor
SOCE inhibitor 1 is a store-operated calcium entry (SOCE) inhibitor with an IC50 of 4.4 μM. -
CRAC inhibitor
CM-4620 is a calcium-release activated calcium-channel (CRAC) inhibitor, with IC50s of 119, 895 nM for Orai1/STIM1 and Orai2/STIM1 channels, respectively. -
elastogenesis inhibitor
L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor. -
Ca2+ release inhibitor
Dantrolene sodium is a muscle relaxant that acts by abolishing excitation-contraction coupling in muscle cells, probably by action on the ryanodine receptor. -
SERCA inhibitor
Cyclopiazonic acid is an inhibitor of SERCA (endoplasmic reticulum Ca2+-ATPase) which induces the release of intracellular stored Ca2+, without increasing IP3 levels. -
Calcium Channel inhibitor
Tetrandrine is a calcium channel blocker. It inhibits the degranulation of mast cells.Tetrandrine has anti-inflammatory and anti-fibrogenic actions, which make tetrandrine and related compounds potentially useful in the treatment of lung silicosis, liver cirrhosis, and rheumatoid arthritis. -
NF-κB Expression Reducer, ERK 1/2 Activator, Beta-Adrenergic Receptor Modulator, Calcium Channel Inhibitor
Eupatorin is a flavonoid that functions primarily as an NF-κB expression reducer and an ERK 1/2 activator, while also modulating beta-adrenergic receptors and inhibiting calcium channels. It demonstrates significant antiproliferative and vasodilatory effects, inducing apoptosis and causing G2/M phase cell cycle arrest, alongside reactive oxygen species (ROS) production. Eupatorin has been shown to impact inflammatory mediators and calcium signaling pathways, making it relevant for research in breast cancer, hypertension, and leukemia. Metabolized by CYP1A1 and other CYP1 enzymes, Eupatorin yields bioactive metabolites that maintain antiproliferative properties. -
glutamate release inhibitor
Sipatrigine, a neuroprotective agent, is a glutamate release inhibitor, voltage-dependent sodium channel and calcium channel inhibitor, penetrating the central nervous system. Has potential to treat focal cerebral ischemia and stroke. -
CRAC inhibitor
RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. -
Calcium Channel Inhibitor
Gabapentin enacarbil (XP-13512) is a prodrug for the anticonvulsant and analgesic drug gabapentin. -
calcium channel inhibitor
Bay-K-8644 (R)-(+)- is a calcium channel inhibitor. Bay-K-8644 (R)-(+)- inhibits Ba2+ currents (IBa) (IC50=975 nM). -
Calcium channel antagonist
Felodipine is a 1,4-dihydropyridine antagonist and calcium channel protein inhibitor.
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IL-1 Inhibitor
Diacerein is a potent IL-1 inhibitor that functions by reducing the production of IL-1 converting enzyme, thereby inhibiting the activation of IL-1β and its downstream signaling pathways. This compound exhibits significant anti-inflammatory and anti-rheumatic properties, making it useful for various research applications, including studies on osteoarthritis and the management of bronchospasm and airway inflammation in asthmatic models. Diacerein is recognized as a slow-acting drug for symptomatic relief of osteoarthritis, facilitating insights into long-term therapeutic strategies. -
SERCA2 Inhibitor
COX-2-IN-55 is a selective SERCA2 inhibitor that exhibits promising anticancer properties, with a unique profile derived from a Celecoxib analog. This compound enhances caspase-3 cleavage and elevates DR5 levels, leading to the activation of GRP78, which contributes to the repression of triple-negative breast cancer (TNBC) progression. Additionally, COX-2-IN-55 reduces angiogenic markers such as VEGF-α and IL-8, effectively inhibiting microvessel formation and supporting its potential utility in cancer research applications. -
PKA inhibitor
HA-1004 is a selective and multifunctional inhibitor of cyclic nucleotide-dependent protein kinases, including protein kinase A (PKA) and cyclic GMP-dependent protein kinase (PKG). It regulates key second messenger pathways involving cyclic AMP and cyclic GMP and has broad pharmacological effects. HA-1004 inhibits lipolysis and induces vascular smooth muscle relaxation, acting as a vasodilator. It also functions as a calcium antagonist, contributing to its ability to suppress contraction in rabbit aortic strips. In neurological models, HA-1004 has been shown to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models, suggesting potential relevance in addiction and neurochemical regulation. Its diverse actions make it a valuable tool for studying cardiovascular, metabolic, and neurobiological processes. -
Bone resorption inhibitor
Chicken calcitonin is a peptide hormone involved in the regulation of calcium metabolism. It inhibits bone resorption by suppressing the motility and activity of osteoclasts, as demonstrated in neonatal rat models. This hormone plays a key role in maintaining bone homeostasis and is of interest in bone-related research. -
Calcium Channel Inhibitor
Ethacrynic acid sodium is an effective calcium channel inhibitor that primarily targets L-type voltage-dependent and store-operated calcium channels. This compound exhibits diuretic properties and significantly modulates glutathione S-transferases (GSTs) while inhibiting the NF-kB signaling pathway. Ethacrynic acid sodium demonstrates anti-inflammatory activity, evidenced by its ability to reduce retinoid-induced ear edema in murine models, making it a valuable tool in research focused on inflammation and airway smooth muscle relaxation. -
Calcium Channel Inhibitor
Levamlodipine hydrobromide is a calcium channel inhibitor with notable antioxidant and vasodilatory properties. This compound has been shown to reduce serum malondialdehyde (MDA) levels while increasing superoxide dismutase (SOD) activity, thus improving oxidative stress responses. It is appropriate for research applications related to vascular dementia, hypertension, and cerebrovascular diseases. -
SERCA Inhibitor
2,5-Di-tert-butylhydroquinone is a potent inhibitor of Sarco/endoplasmic reticulum Ca2+ ATPase (SERCA), demonstrating an IC50 of 400 nM. This compound disrupts the gating function of Glu309, thereby preventing calcium ions from accessing their binding site. Additionally, 2,5-Di-tert-butylhydroquinone influences the activity of key enzymes such as 5-lipoxygenase and COX-2, with IC50 values of 1.8 μM and 14.1 μM, respectively. It is utilized in research focused on cellular calcium regulation and inflammatory processes. -
Calcium Channel Inhibitor
Ethosuximide is a calcium channel inhibitor primarily targeting T-type calcium channels, specifically blocking low voltage-activated currents. This compound is extensively used in research for its anti-epileptic properties as well as its potential therapeutic effects in various neurodegenerative disease models. Ethosuximide facilitates the study of calcium signaling pathways and their involvement in neuronal excitability and degeneration. -
T-channels Inhibitor
1-Octanol is a saturated fatty alcohol that selectively inhibits T-type calcium channels, demonstrating an IC50 of 4 μM for native T-currents. This compound serves as a valuable tool in pharmacological research aimed at understanding calcium signaling pathways. Additionally, its properties as a biofuel with diesel-like characteristics make it an interesting candidate for energy applications. -
Sodium-Calcium Exchanger Inhibitor
KB-R7943 is a selective inhibitor of the sodium-calcium exchanger, exhibiting an IC50 value of 5.1 µM. This compound is utilized as a valuable tool in studies involving cardiac and renal failure models, facilitating research into calcium homeostasis and its implications in heart and kidney function. -
Calcium Channel Inhibitor
McN5691 is a voltage-sensitive calcium channel inhibitor that selectively blocks calcium influx through L-type calcium channels. This action leads to reduced calcium-dependent cellular events, making it a valuable tool for investigating calcium signaling pathways. McN5691 is particularly useful in research focused on cardiovascular physiology and the modulation of muscle contraction mechanisms. -
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. -
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. -
SERCA Inhibitor
4,4'-Methylenebis(2,6-di-tert-butylphenol) is a selective inhibitor of sarco/endoplasmic reticulum calcium ATPase (SERCA), with an IC50 value of 17 μM. This compound plays a critical role in modulating calcium homeostasis and is valuable for research into cellular processes and disorders linked to calcium dysregulation. Its application extends to studying various diseases where altered calcium signaling is implicated. -
Calcium Channel Inhibitor
A-39355 is a calcium channel inhibitor that effectively reverses multidrug resistance in tumor cells. It enhances the cytotoxicity of antitumor compounds by increasing their accumulation within resistant cells and inhibiting their efflux. Unlike traditional calcium antagonists, A-39355 exhibits minimal hypotensive effects. This compound is particularly useful for research focused on overcoming treatment resistance in cancer therapy. -
L-type Calcium Channel Inhibitor
Diltiazem malate is a potent inhibitor of L-type calcium channels, effectively modulating calcium influx in cardiac and vascular smooth muscle. It exhibits significant antihypertensive and antiarrhythmic properties, making it valuable for the investigation of cardiovascular conditions. Diltiazem malate is commonly used in research related to cardiac arrhythmia, hypertension, and angina pectoris. -
P-glycoprotein Inhibitor
Niguldipine monohydrochloride is a selective P-glycoprotein inhibitor known for its action as a calcium channel blocker. It demonstrates significant anticancer properties by inhibiting Cav 3.2, with an IC50 of 0.9 μM. This compound is primarily utilized in tumor research to explore its effects on drug resistance and the transport of therapeutic agents across cellular membranes. -
Calcium Channel Inhibitor
Piprofurol is a potent calcium channel inhibitor that effectively reduces calcium-induced contractions in isolated potassium depolarized rat aorta preparations in a concentration-dependent manner. This compound demonstrates the ability to relax K+-induced contractions in both dog coronary arteries and rabbit basilar arteries. Additionally, Piprofurol exhibits a negative inotropic effect on guinea-pig papillary muscle, with an EC50 value of 5 μM, highlighting its potential utility in cardiovascular research and related studies. -
Calcium Channel Inhibitor
(-)-Praeruptorin A is a natural product derived from the roots of Peucedanum praeruptorum Dunn, functioning as a calcium channel inhibitor. This compound induces relaxation of ileum and tracheal smooth muscles by activating the NO/cGMP signaling pathway. Its significant therapeutic potential in hypertension is primarily attributed to its capacity to block Ca2+-influx, making it a valuable reagent for research in cardiovascular pharmacology. -
Calcium Channel Inhibitor
Ro 18-3981 is a dihydropyridine compound that selectively inhibits calcium channels in cardiac tissues. It demonstrates enhanced inhibitory potency at depolarized membrane potentials, with an IC50 value of 2.3 nM at -20 mV and 100 nM at -50 mV. This compound is useful for studying the role of calcium signaling in cardiac physiology and related pathologies. -
Calcium Channel Inhibitor
R 56865 is a calcium channel inhibitor that offers cardiomyocyte protection against digitoxin (ouabain)-induced myocardial calcium overload. This compound demonstrates a significant protective effect against digitoxin-induced intoxication, as evidenced in studies utilizing guinea pig papillary muscle. R 56865 is primarily utilized in research related to cardiac function and the mechanisms of arrhythmias. -
L-type Calcium Chanel Inhibitor
Diltiazem is an orally active L-type calcium channel blocker that exerts antihypertensive and antiarrhythmic effects. It is utilized in research related to cardiac arrhythmias, hypertension, and angina pectoris, making it valuable for studies focused on cardiovascular health. Its mechanism of action contributes to the modulation of calcium influx, which is critical in various cardiac and vascular functions. -
NMDA Receptor Inhibitor
Bupivacaine is an NMDA receptor inhibitor that modulates neuronal excitability by blocking sodium, L-calcium, and potassium channels. It exhibits potent inhibition of SCN5A channels, with an IC50 of 69.5 μM. This compound is primarily utilized in research focused on chronic pain mechanisms and therapeutic interventions. -
Calcium Channel Inhibitor
Tetracaine hydrochloride is a calcium channel inhibitor that effectively blocks the voltage-sensitive release of Ca2+ from the sarcoplasmic reticulum. This compound exhibits significant biological activity and is primarily utilized in topical applications within ophthalmology, as well as serving as an antipruritic agent. Its mechanism of action makes it valuable for research in pain relief and modulation of calcium signaling pathways. -
Calcium Channel Inhibitor
Lidoflazine is a potent inhibitor of calcium channels, specifically known for its high affinity blockade of the HERG potassium channel. This compound exhibits antianginal properties, making it relevant in studies related to cardiac function and arrhythmias. Notably, Lidoflazine is associated with a risk of QT interval prolongation and ventricular arrhythmia, which underscores its importance in pharmacological research aiming to understand cardiovascular safety profiles. -
Calcium Channel Inhibitor
Pranidipine is a potent, long-acting 1,4-dihydropyridine calcium channel inhibitor, specifically designed to modulate calcium influx in vascular smooth muscle cells. Its primary biological activity involves the reduction of blood pressure, making it an effective antihypertensive agent. This compound is widely used in cardiovascular research to investigate mechanisms underlying hypertension and to evaluate therapeutic strategies for managing elevated blood pressure. -
Calcium Influx Inhibitor
Carboxyamidotriazole Orotate is an orotate salt of Carboxyamidotriazole, a potent inhibitor of calcium influx. It acts primarily as a cytostatic agent targeting nonvoltage-operated calcium channels and disrupting calcium-mediated signaling pathways. This compound demonstrates notable anti-tumor, anti-inflammatory, and antiangiogenic properties, making it valuable in cancer research and the study of inflammatory diseases. -
Calcium Channel Inhibitor
Nothofagin is a dihydrochalcone that acts as a calcium channel inhibitor. By blocking calcium influx, it downregulates NF-κB translocation, providing a mechanism to modulate inflammatory responses. This compound exhibits antioxidant properties and has potential applications in research related to septic responses and vascular inflammation. -
SERCA Inhibitor
CAD204520 dihydrochloride is a selective SERCA inhibitor with an IC50 of 0.34 μM. This compound specifically targets mutated NOTCH1 proteins, demonstrating significant relevance in the study of T-cell acute lymphoblastic leukemia (T-ALL) and mantle cell lymphoma (MCL). It is a valuable tool for research investigating the therapeutic potential and mechanisms of these cancers.
