Catalog No.
Product Name
Application
Product Information
Citations
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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. -
IP3 Receptor Modulator
Adenophostin A is a potent modulator of inositol 1,4,5-trisphosphate receptors (IP3) that functions as a calcium (Ca2+) releaser, exhibiting an IC50 of 1.3 nM and an EC50 of 1.4 nM in rat models. This compound effectively stimulates Ca2+ release from intracellular stores and microsomes, inhibits the binding of [3H]IP3 to plasma membrane receptors, and activates chloride channels. Notably, Adenophostin A is resistant to phosphorylation and dephosphorylation by metabolic enzymes, thereby sustaining its activity and enhancing cytoplasmic Ca2+ levels in vascular smooth muscle cells. This reagent is highly relevant for research on hemorrhagic shock and related physiological studies. -
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. -
Calcium Channel Antagonist
Flosatidil is an orally active calcium channel antagonist that effectively inhibits calcium influx through L-type calcium channels. Its primary biological activities include antianginal and antihypertensive effects, making it a valuable compound for cardiovascular research. Flosatidil is utilized in studies investigating the modulation of vascular tone and cardiac output, contributing to the understanding of hypertension and angina management. -
Calcium Channel Antagonist
Lomerizine is an antagonist of L- and T-type voltage-gated calcium channels, primarily inhibiting calcium influx into cells. This activity is associated with its potential to modulate vascular smooth muscle contraction and neurotransmitter release. Lomerizine is utilized in research to investigate cardiovascular diseases and neurological disorders related to calcium channel dysregulation. -
Anti-inflammatory Agent
LQFM020 is an orally active pyrazole derivative that functions as an anti-inflammatory agent. It effectively inhibits calcium channels while activating potassium and nitric oxide/cGMP pathways, leading to reduced vasoconstriction. LQFM020 exhibits significant anti-inflammatory and analgesic properties, making it a valuable reagent for research focused on inflammation and pain mechanisms. -
Ca2+‑ATPase Inhibitor
rel-(E)-6,7-Transdihydroxyligustilide is a potent inhibitor of Ca2+-ATPase, specifically in calmodulin-deficient human erythrocyte membranes. This compound, derived from the dried tuberous roots of Polygonum multiflorum, plays a significant role in the regulation of calcium homeostasis. It is particularly valuable in research related to hyperlipidemia and related metabolic disorders. -
Calcium Channel
Levamlodipine (gentisate) is a potent calcium channel blocker primarily employed for its antihypertensive and antianginal effects. This pharmacologically active amino ester exhibits significant biological activity by inhibiting calcium influx into cardiovascular cells, thereby reducing blood pressure and alleviating angina. Additionally, high enantiomeric purity can be assessed through fast capillary electrophoresis, yielding a resolution of 9.8, which underscores its utility in compound analysis and development within chemical research. -
Isotope-Labeled Compounds
Verapamil-d7 is a deuterium-labeled derivative of Verapamil, a calcium channel blocker and a potent inhibitor of the P-glycoprotein (P-gp) transporter. This isotope-labeled compound is utilized in pharmacokinetic studies and metabolic research, providing insights into drug interactions and transport mechanisms. Its applications extend to investigating conditions such as hypertension, cardiac arrhythmias, and angina, making it a valuable tool in cardiovascular research. -
Calcium Channel Antagonist
Araguspongin B is a potent calcium channel antagonist that specifically targets inositol 1,4,5-trisphosphate (IP3) receptors. It effectively inhibits the calcium-releasing activity induced by IP3, demonstrating an IC50 value of 0.6 μM in cerebral microsomes. This compound is recognized for its vasodilatory properties and is valuable for research exploring calcium signaling pathways and their implications in various physiological and pathological processes. -
Calcium-sensitizing Agent
BA 41899 is a selective calcium-sensitizing agent that enhances cardiac contractility without phosphodiesterase (PDE) III inhibition or other inotropic mechanisms. This compound is valuable for investigating mechanisms underlying cardiovascular diseases, particularly congestive heart failure (CHF). Its unique activity profile makes it a useful tool for researchers studying cardiac physiology and therapeutic interventions in heart disease. -
Calcium Channel Agonist
LND 796 is a calcium channel agonist with positive inotropic effects reminiscent of digitalis. It demonstrates a concentration-dependent increase in contractility in guinea pig papillary muscles, enhancing both contraction components and slow action potential amplitude, particularly in partially potassium-depolarized conditions. The mechanism of action involves increased calcium influx through calcium channels and inhibition of sodium-potassium ATPase. Due to its unique profile, LND 796 may have potential applications in the treatment of congestive heart failure. -
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. -
Ca2+ Antagonist
SR33805 oxalate is a potent calcium (Ca2+) channel antagonist, specifically blocking L-type calcium channels. It demonstrates effective inhibition with EC50 values of 4.1 nM in depolarized conditions and 33 nM under polarized conditions. This reagent is valuable for research into acute and chronic heart failure, aiding in the understanding of Ca2+ signaling in cardiac pathophysiology. -
Potassium/Calcium/Sodium Channel Blocker
NIP-142 is a benzopyran derivative that functions as a potassium, calcium, and sodium channel blocker. It selectively inhibits potassium channels abundant in atrial muscle, leading to an increase in the effective refractory period (ERP) and action potential duration (APD) in the atrium, while sparing ventricular repolarization. Additionally, NIP-142 dampens L-type and T-type calcium channels and sodium channels, enhancing its anti-arrhythmic properties. This compound is particularly useful in the study of atrial fibrillation and related arrhythmias. -
Calcium Cage
DMNPE-4 AM-caged-calcium functions as a highly selective calcium cage, exhibiting a dissociation constant (Kd) for Ca2+ of 48 nM and 19 nM at pH 7.2 and pH 7.4, respectively. Upon photolysis, the compound releases Ca2+ with significantly enhanced availability, achieving a Kd of approximately 2 nM. This photolabile calcium chelator is instrumental for studies involving calcium signaling and dynamics in cellular research applications. -
Calcium Antagonist
Emopamil is a calcium channel antagonist that is effective in mitigating ischemia-induced neuronal cell damage. By inhibiting calcium influx, it helps in protecting neuronal cells from necrosis and apoptosis under ischemic conditions. This compound holds potential for research applications focused on neuroprotection and the study of calcium-mediated pathways in various neurological disorders. -
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 Blocker
Sornidipine is a potent calcium channel blocker that primarily targets L-type calcium channels to inhibit calcium ion influx into cells. This mechanism results in decreased vascular smooth muscle contraction, promoting vasodilation and effectively lowering blood pressure. Sornidipine is valuable for research applications focusing on the cardiovascular system, particularly in studies related to hypertension and associated cardiovascular disorders. Additionally, it has been noted for its ability to reduce neurogenic inflammation, further expanding its relevance in cardiovascular research. -
Stable Isotope
Ethosuximide-d5 is a stable isotopically labeled form of Ethosuximide, an established anti-epileptic agent. This compound acts primarily as a blocker of low voltage activated T-type calcium channels, contributing to its therapeutic effects. Ethosuximide-d5 is valuable for research applications involving neurodegenerative disease models and mechanisms of epilepsy, enabling precise metabolic studies and tracking within biological systems. -
Hypoglycemic Agent
AZ-DF 265 is a hypoglycemic agent that promotes insulin secretion through the inhibition of ATP-sensitive potassium channels and the activation of voltage-dependent calcium channels. This results in the influx of calcium ions, which is crucial for insulin release. AZ-DF 265 is applicable in diabetes research, providing insights into glucose metabolism and insulin regulation mechanisms. -
Nav1.2 Inhibitor
Nav1.2-IN-2 is a potent inhibitor of the voltage-gated sodium channel Nav1.2, demonstrating an IC₅₀ of 0.18 μM for channel inactivation. It effectively reduces both the amplitude and frequency of spontaneous synchronous calcium oscillations with IC₅₀ values of 0.38 μM and 0.88 μM, respectively. Additionally, Nav1.2-IN-2 inhibits calcium influx triggered by Veratridine with an IC₅₀ of 1.89 μM. This reagent is relevant for research into neurological disorders such as epilepsy. -
Stable Isotope
Diltiazem-(acetoxy-d3) hydrochloride is a deuterium-labeled derivative of Diltiazem hydrochloride, a calcium channel antagonist. As a stable isotope compound, it serves as a valuable tool for pharmacokinetic studies and metabolic research, allowing for precise tracking of Diltiazem's biological fate. This reagent can facilitate investigations into calcium signaling pathways and cardiovascular pharmacology. -
T-type Ca2+ Channel Antagonist
U 92032 is a T-type Ca2+ channel antagonist that effectively inhibits sodium channels. This compound has been shown to disrupt thalamic oscillations, providing valuable insights into the mechanisms underlying neurological disorders. U 92032 is applicable in research focused on various neurological diseases, making it a significant tool for studying calcium signaling and excitability in the central nervous system. -
Calcium Channel Antagonist
(-)-Niguldipine hydrochloride is a calcium channel antagonist that inhibits calcium influx across cell membranes, leading to vasodilation. Its biological activity includes the inhibition of U-46619-induced coronary artery contraction in guinea pig Langendorff hearts, demonstrating a pID50 of 9.93, as well as high affinity for calcium channel binding sites in guinea pig skeletal muscle membranes with a Ki of 8.10. Additionally, (-)-Niguldipine hydrochloride effectively lowers blood pressure in spontaneously hypertensive rats (pED30 of 5.55) and has potential applications in treating cardiovascular conditions such as hypertension, angina pectoris, and arrhythmias. -
Calcium Channel Blockers
Oxodipine is a dihydropyridine-based calcium channel blocker that primarily targets L-type and T-type calcium channels. It effectively inhibits KCl-induced aortic contractions in rabbit models and demonstrates a reduction in cardiac contractility in rat ventricular preparations. In cultured rat neonatal ventricular myocytes, Oxodipine decreases L-type calcium currents with an IC50 of 0.24 μM and T-type currents with an IC50 of 0.41 μM. Additionally, it is noted to cause gastrointestinal effects in mice and gingival hyperplasia in canine studies, making it relevant for cardiovascular and gastrointestinal research. -
Vasodilating Agent
HUP30 is a potent vasodilating agent that primarily stimulates soluble guanylyl cyclase. Its mechanism of action includes the activation of potassium channels and inhibition of extracellular calcium influx. This compound is valuable for research applications focused on vascular biology, cardiovascular diseases, and the modulation of blood pressure.
