Calcium Channels

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  1. 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.
  2. 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.
  3. 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.
  4. 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.
  5. 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.
  6. 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.
  7. 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.
  8. 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.
  9. 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.
  10. 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.
  11. 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.
  12. 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.
  13. 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.
  14. 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.
  15. 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.
  16. 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.
  17. 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.
  18. 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.
  19. 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.
  20. 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.
  21. 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.
  22. 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.
  23. SERCA Blocker

    JTV-519 fumarate is a Ca2+-dependent blocker of the sarcoplasmic reticulum Ca2+-stimulated ATPase (SERCA), functioning as a partial agonist for ryanodine receptors in striated muscle. This compound exhibits cardioprotective properties and demonstrates significant antiarrhythmic activity, making it valuable for research on cardiac function and arrhythmias. Its unique mechanism highlights its potential in studying calcium handling and related cardiac pathologies.
  24. Calcium Channel Antagonist

    S-312-d is a calcium channel antagonist that exhibits protective effects against ischemic acute renal failure. Administered intravenously at doses of 0.01-0.1 mg/kg body weight prior to ischemia, S-312-d demonstrates a dose-dependent reduction in ischemia-induced renal injury, enhances survival rates in ischemic models, and mitigates renal cortical edema as well as elevated renal tissue calcium levels. This compound is valuable for research into renal protection mechanisms and the pathophysiology of acute kidney injury.
  25. Calcium Channel Antagonist

    RS-93522 is a calcium channel antagonist that demonstrates significant pharmacological activity through the inhibition of calcium influx. This compound is readily absorbed and exhibits high bioavailability when administered via the nasal route. RS-93522 is primarily utilized in research focused on investigating calcium signaling pathways and their implications in various physiological and pathological conditions.
  26. Calcium Channel Blocker

    Amlodipine hydrochloride is a calcium channel blocker that primarily targets L-type calcium channels to produce vasodilation and reduce blood pressure. This compound is effective in managing hypertension and angina pectoris and has demonstrated synergistic antimicrobial activity, particularly against carbene peptide-resistant Acinetobacter baumannii in vitro. Amlodipine hydrochloride's ability to enhance the efficacy of certain antibiotics makes it a valuable tool in combating antibiotic resistance, potentially minimizing drug dosage and associated toxicities.
  27. 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.
  28. Vasodilatory Calcium Antagonist

    DHP-218 is a vasodilatory calcium antagonist that primarily targets calcium channels to induce vasodilation. This compound exhibits significant and prolonged antihypertensive effects, making it a valuable tool for studies focused on hypertension and vascular biology. Its ability to effectively lower blood pressure positions DHP-218 as a useful reagent for researchers investigating cardiovascular pathologies.
  29. Calcium Channel Blocker

    Falipamil is a calcium channel blocker that serves as a bradycardic agent. Its mechanism involves a reduction in the diastolic depolarization rate, leading to a prolongation of action potential duration. Falipamil is utilized in research focused on cardiovascular physiology and the modulation of heart rate.
  30. Cav1.2 Blocker

    Calciseptine is a natural polypeptide toxin derived from the venom of the black mamba snake (Dendroaspis p. polylepis). It serves as a selective blocker of the L-type Cav1.2 calcium channel, showcasing an IC50 value of 92 nM, while sparing other calcium channels such as Cav3.1 and Cav2.2, as well as sodium and potassium channels. Calciseptine induces negative inotropic and relaxant effects in murine models without impacting heart rate or sinoatrial node action potentials. This compound is valuable for investigations into cardiovascular diseases.
  31. Cav 3.1 Blocker

    Cav 3.1 Blocker 1 is a selective inhibitor targeting the Cav 3.1 T-type calcium channel with an IC50 of 160 nM. This compound exhibits weak inhibition of Cav 3.2 at an IC50 of 5000 nM, while it shows no significant inhibition of Cav 3.3 and Cav 1.2 (>10000 nM). Cav 3.1 Blocker 1 is valuable for research focused on calcium signaling pathways and their implications in various physiological and pathological processes.
  32. Stable Isotope

    Levamlodipine-d4 is the deuterium-labeled form of Levamlodipine, a selective dihydropyridine calcium channel blocker. This compound exhibits significant vasodilatory activity and is commonly utilized in the management of hypertension and angina. As a stable isotope, Levamlodipine-d4 is a valuable tool for pharmacokinetic studies and related research applications.
  33. Calcium Antagonist

    SIM-6080 is a calcium antagonist that effectively inhibits the proliferation of rat aortic myocytes. This compound has been shown to reduce aortic atherosclerosis in rabbit models, making it a valuable tool for research in cardiovascular biology and atherogenesis. Its ability to modulate calcium signaling pathways further positions it as a significant reagent for studying vascular smooth muscle cell behavior and related conditions.
  34. Calcium Antagonist

    Ronipamil is a calcium ion antagonist that modulates calcium influx in cells. It is known to enhance the specific binding and internalization of human 125I-labeled low-density lipoprotein (LDL) in human skin fibroblasts and the human hepatoma cell line Hep G2. This compound is valuable in research applications related to cellular cholesterol metabolism and cardiovascular studies.
  35. Calcium Channel Agonist

    Bay Y5959 is a potent calcium channel agonist that interacts with the DHP receptor in a voltage-dependent manner, enhancing both the mean open and closed times of calcium channels. This compound demonstrates significant biological activity, making it valuable in the study of cardiovascular conditions such as congestive heart failure and arrhythmias. Bay Y5959 may serve as an essential tool for researchers investigating calcium channel dynamics and their implications in cardiac health.
  36. Stable Isotope

    Menthol-d2 is a deuterated derivative of menthol, serving as a stable isotope. It acts as an analgesic and modulates the TRPM8 ion channel, which is responsible for sensing cold temperatures. By regulating TRPM8, Menthol-d2 exerts analgesic and anti-irritation effects. Additionally, it stimulates cold receptors, inducing a cooling sensation through the inhibition of Ca++ currents in neuronal cell membranes, making it valuable for research in pain relief and sensory modulation.
  37. Calcium Antagonist

    Flordipine is a calcium antagonist that effectively modulates calcium ion influx in the cardiovascular system. Its primary biological activity includes the reduction of vascular resistance, contributing to antihypertensive effects. Flordipine is widely used in research applications aimed at studying blood pressure regulation and vascular function.
  38. Vasodilator

    Riodipine is a selective vasodilator that primarily targets vascular smooth muscle. It is effective in promoting blood vessel relaxation, leading to reduced vascular resistance and lower blood pressure. This compound is widely utilized in research focused on antihypertensive therapies and cardiovascular disease models, providing insights into the mechanisms of vascular regulation and potential therapeutic interventions.
  39. Ca2+ Channel Blocker

    (2R,3R)-Diltiazem hydrochloride is a selective L-type Ca2+ channel blocker primarily used in cardiovascular research. It exhibits antihypertensive and antiarrhythmic properties, making it valuable for studying conditions such as cardiac arrhythmia, hypertension, and angina pectoris. This compound provides a critical tool for investigating calcium signaling pathways and their role in heart function.
  40. Calcium Antagonist

    Fostedil, a calcium antagonist, primarily targets voltage-gated calcium channels, inhibiting calcium influx. This compound demonstrates significant potential in research related to cardiovascular conditions, including angina pectoris and other heart diseases. Its pharmacological properties make it a valuable tool for studying the mechanisms underlying calcium dysregulation in cardiac function.
  41. Stable Isotope

    Amlodipine-1,1,2,2-d4 maleate is a deuterium-labeled derivative of Amlodipine, a dihydropyridine calcium channel blocker. Its primary mechanism involves the inhibition of voltage-dependent L-type calcium channels, which reduces calcium influx. This reagent is valuable for studies related to hypertension and cancer research, offering insights into calcium signaling pathways and their implications in various pathological conditions.
  42. Calcium Channel/Sodium Channel Antagonist

    EO-122 is a potent antagonist targeting calcium and sodium channels. It exhibits significant inhibitory activity, making it a valuable tool for studying mechanisms related to arrhythmias. This compound aids in the exploration of cardiac and neuronal excitability, facilitating research into related therapeutic strategies.
  43. Stable Isotope

    Diltiazem-d5 hydrochloride is a deuterated isotopic form of Diltiazem, a calcium channel blocker that inhibits L-type calcium channels. Its primary mechanism involves modulation of calcium ion influx, leading to reduced myocardial contractility and vasodilation. This stable isotope is valuable for pharmacokinetic studies, metabolic pathway analysis, and isotopic labeling techniques in chemical research and drug development.
  44. Stable Isotope

    Farnesyl pyrophosphate-d6 is a deuterium-labeled stable isotope derivative of farnesyl pyrophosphate, an important metabolic intermediate in the mevalonate pathway. It acts as an agonist for TRP channel TRPM2, facilitating calcium influx and promoting cell death. Farnesyl pyrophosphate plays a crucial role in cholesterol and ubiquinone synthesis, as well as in protein farnesylation and geranylgeranyl pyrophosphate synthesis. This reagent is utilized in research exploring cerebral ischemia, neurodegenerative diseases, pancreatic cancer, inflammation, and autoimmune disorders.
  45. Insecticide

    Kadethrin is a synthetic pyrethroid that functions as an effective insecticide. It modulates the binding of [3H] full-histamine toxin ([3H]H12-HTX) to nicotinic acetylcholine receptor/channel binding sites and inhibits calcium ion (Ca2+) flux through these receptor ion channels. This compound is valuable for research applications in understanding insect neurophysiology and developing pest control strategies.
  46. Stable Isotope

    Diltiazem-d4 is a deuterated form of Diltiazem, which acts as a selective L-type calcium channel blocker. It exhibits significant antihypertensive and antiarrhythmic properties, making it useful in the study of cardiac arrhythmias, hypertension, and angina pectoris. This stable isotope is ideal for research applications requiring isotopic tracing and elucidation of pharmacokinetic pathways involved in calcium channel modulation.
  47. Calcium/Sodium Channel Blocker

    LY393615 free base is an effective blocker of neuronal calcium (Ca²⁺) and sodium (Na⁺) channels, exhibiting IC50 values of 1.9 μM and 5.2 μM for the α1A and α1B calcium channel subunits, respectively. This compound demonstrates substantial brain penetration and offers neuroprotective properties in cerebral ischemia models. It serves as a valuable tool in neurological disease research, providing insight into the pathophysiology of various neurodegenerative conditions.
  48. Calcium Channel Antagonist

    AJG049 free base is a potent calcium channel antagonist that selectively targets L-type calcium channels. By inhibiting calcium influx, AJG049 facilitates vascular relaxation, decreases cardiac workload, and enhances cardiac perfusion. This compound is valuable for research into cardiovascular diseases, providing insights into calcium channel modulation and its effects on cardiac function.
  49. Calcium Channel Control

    Amlodipine metabolite is an active metabolite derived from the calcium channel blocker Amlodipine. It exerts its biological activity by modulating calcium ion influx through L-type calcium channels, thus influencing vascular smooth muscle contraction. This compound is primarily utilized in cardiovascular research to study mechanisms of hypertension and investigate calcium channel regulation.
  50. Calcium Channel Blocker

    Diproteverine is a calcium channel blocker that exerts its effects by selectively inhibiting calcium influx through voltage-gated calcium channels. This compound demonstrates antianginal properties, making it relevant for research into cardiovascular health and related disorders. Additionally, studies indicate potential embryotoxicity, highlighting the importance of further investigation into its safety profile for developmental biology applications.

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