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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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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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
SOCE inhibitor
SOCE inhibitor 1 is a store-operated calcium entry (SOCE) inhibitor with an IC50 of 4.4 μM. -
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). -
CRAC inhibitor
RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. -
Calcium channel antagonist
Felodipine is a 1,4-dihydropyridine antagonist and calcium channel protein inhibitor.
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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. -
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. -
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. -
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. -
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. -
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. -
SERCA Inhibitor
CAD204520 is a selective inhibitor of the Sarcoplasmic Reticulum Calcium ATPase (SERCA), demonstrating an IC50 value of 0.34 μM. This compound specifically targets mutated NOTCH1 proteins more effectively than wild-type, making it a valuable tool for studying T-cell acute lymphoblastic leukemia (T-ALL) and mantle cell lymphoma (MCL). CAD204520 is suitable for research aimed at understanding the molecular mechanisms and therapeutic strategies in these malignancies. -
Calcium Channel Inhibitor
Heteroclitin D is a lignan derived from Kadsura medicinal plants, functioning primarily as a calcium channel inhibitor. It exhibits significant biological activity by inhibiting L-type calcium channels, which are critical in various physiological processes. This compound is suitable for research applications focusing on calcium signaling, neuroprotection, and studies related to oxidative stress and lipid peroxidation. -
Calcium Channel Inhibitor
Yangambin is a furofuran lignan that functions as a calcium channel inhibitor, targeting voltage-gated Ca2+ channels. This compound effectively reduces intracellular calcium levels in vascular smooth muscle cells, promoting peripheral vasodilation. Additionally, Yangambin demonstrates antiallergic activity by inhibiting β-hexosaminidase release with an IC50 of 33.8 μM and exhibits anti-inflammatory properties with an IC50 of 37.4 μM, making it valuable for research in vascular biology and inflammation. -
Calcium Channel Inhibitor
PD0176078 is a selective N-type calcium channel inhibitor, primarily targeting voltage-gated calcium channels. It exhibits significant biological activity by effectively blocking calcium influx, which modulates neurotransmitter release and can influence pain signaling pathways. This compound is valuable for research applications focused on neuropharmacology and the investigation of pain mechanisms. -
Cav3.1/Cav3.2/Cav3.3 Inhibitor
ML218 hydrochloride is a selective inhibitor of T-type calcium channels, specifically Cav3.1, Cav3.2, and Cav3.3, exhibiting IC50 values of 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively. This compound effectively inhibits burst activity in subthalamic nucleus neurons and demonstrates minimal interference with L- or N-type calcium channels, KATP channels, or hERG potassium channels. Additionally, ML218 hydrochloride has the capability to penetrate the blood-brain barrier, making it a valuable tool for neurological research applications. -
Calcium Channel Inhibitor
Etripamil hydrochloride is a potent L-type calcium channel inhibitor primarily used in the research of paroxysmal supraventricular tachycardia (PSVT). By blocking calcium influx through slow calcium channels, it effectively slows down atrioventricular node conduction and extends the refractory period of the atrioventricular node. This compound is valuable for studying cardiac electrophysiology and the mechanisms underlying arrhythmias. -
CaVAb Inhibitor
UK-59811 hydrochloride is a Br-dihydropyridine derivative that functions as a potent inhibitor of the bacterial homotetrameric voltage-gated calcium channel, CaVAb, with an IC50 value of 194 nM. It serves as a valuable tool for studying calcium ion transport and its physiological implications in bacterial systems. Its specific action on CaVAb makes it suitable for research applications focused on calcium signaling and channel modulation. -
T-type Calcium Channel Inhibitor
IAA65 is a potent inhibitor of T-type calcium channels, exhibiting an IC50 value of 18.9 µM. This compound is primarily utilized in research related to epilepsy, aiding in the investigation of calcium channel modulation and its effects on neuronal excitability. IAA65 may facilitate the exploration of therapeutic strategies targeting T-type calcium channels for seizure management. -
T-type Calcium Channel Inhibitor
IAB15 is a potent inhibitor of T-type calcium channels, which play a crucial role in regulating neuronal excitability and neurotransmitter release. This compound demonstrates significant activity in modulating calcium ion influx, making it a valuable tool in epilepsy research. Its ability to selectively target these channels positions IAB15 as an important reagent for studying calcium signaling pathways and their implications in seizure disorders. -
Potassium/Sodium Channel Inhibitor
Huwentoxin I is a peptide toxin that specifically inhibits voltage-gated sodium channels and N-type calcium channels. This compound has demonstrated significant inhibitory effects on sodium channels in both rat hippocampus and cockroach dorsal unpaired median (DUM) neurons, with IC50 values of 66.1 nM and 4.80 nM, respectively. Huwentoxin I is valuable for studies focused on neuronal excitability and channelopathy-related research applications. -
Cav 3.2 Inhibitor
Cav 3.2 inhibitor 1 is a selective inhibitor of the Cav 3.2 T-type calcium channel, exhibiting minimal interaction with dopamine D2 receptors. This compound is valuable for studying mechanisms underlying somatic and visceral pain, making it a significant tool in pain research and potential therapeutic development. -
Cav 3.2 Inhibitor
Cav 3.2 Inhibitor 4 is a selective inhibitor targeting the Cav 3.2 T-type calcium channel, exhibiting an IC50 of 0.6 μM. This compound is primarily researched for its potential in investigating atrial fibrillation and related cardiac conditions. Its peripheral restriction enhances its utility in studying physiological processes influenced by Cav 3.2 activity in diverse experimental settings. -
Calcium Channel Inhibitor
Calcicludine is a potent inhibitor of high-voltage-activated calcium channels, with a particular affinity for L-type calcium channels. Derived from the venom of the green mamba, this protein toxin plays a critical role in studies investigating calcium signaling and neurotransmitter release. Its unique mechanism makes Calcicludine a valuable tool for researchers exploring neuronal excitability and muscle contraction pathways.
