Calcium Channels

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  1. 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.
  2. 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.
  3. 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.
  4. 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.
  5. 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.
  6. 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.
  7. 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.
  8. 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.
  9. 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.
  10. 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.
  11. 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.
  12. 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.
  13. 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.
  14. 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.
  15. 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.
  16. 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.
  17. 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.
  18. 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.
  19. 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.
  20. 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.
  21. 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.
  22. 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.
  23. 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.
  24. 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.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. 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.
  33. Calcium Channel Antagonist

    PD-151307 is an N-type calcium channel antagonist that effectively inhibits calcium influx in neuroblastoma cells, demonstrated by an IC50 of 0.32 µM in IMR-32 human neuroblastoma cells. This compound is pertinent for research applications in cancer therapy, anticonvulsant studies, and models of neuropathic pain, making it a valuable tool for investigating calcium channel modulation in various neurological conditions.
  34. Multi-ion channel Blocker

    Sulcardine hydrochloride is a multi-ion channel blocker primarily targeting sodium (INa) and calcium (ICa) channels, exhibiting IC50 values of 26.9 µM and 69.2 µM, respectively. This compound effectively inhibits the hNav1.5 channel and demonstrates a mild inhibitory effect on hERG channels. Due to its pharmacological properties, Sulcardine hydrochloride is often utilized in research related to anti-arrhythmic effects and cardiac electrophysiology.
  35. cADPR Antagonist

    8-Br-7-CH-cADPR (7-Deaza-8-bromo-cADPR) functions as a potent cADPR antagonist. It exhibits partial inhibition of calcium elevation induced by sTIR dimerization, making it valuable in studies related to calcium signaling pathways. Furthermore, 8-Br-7-CH-cADPR has been shown to significantly reduce axon degeneration caused by Paclitaxel treatment, providing insights into neuroprotective mechanisms and potential therapeutic applications in neurodegenerative research.
  36. Calcium Channel Antagonist

    NP-252 is a calcium channel antagonist that exhibits significant inhibitory effects on calcium influx through voltage-gated calcium channels. It has an effective dose (ED20) of 2.55 mg/kg in spontaneously hypertensive rats, highlighting its potential utility in hypertension research. This compound may serve as a valuable tool for studying cardiovascular physiology and pharmacological interventions targeting calcium signaling pathways.
  37. Calcium Channel Antagonist

    Dopropidil hydrochloride is a calcium channel antagonist that modulates intracellular calcium levels. It demonstrates significant anti-ischemic effects and is utilized in research related to cardiovascular diseases, particularly in models of angina. This compound is valuable for investigating the mechanisms underlying calcium signaling and its implications in ischemic conditions.
  38. Calcium Channel Blocker

    SR33805 analog is an orally active calcium channel blocker that effectively inhibits the proliferation of smooth muscle cells. By blocking calcium channels, it reduces calcium uptake, thereby attenuating proliferation induced by serum, platelet-derived growth factor, and basic fibroblast growth factor. Notably, SR33805 analog has demonstrated a significant reduction in intimal thickening following endothelial injury in animal models. This compound holds promise for research into cardiovascular diseases, particularly early atherosclerosis.
  39. 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.
  40. Calcium Channel Antagonist

    (R)-Azelnidipine is a potent calcium channel antagonist that primarily targets vascular smooth muscle cells. With its high lipophilicity and affinity for vascular walls, it exhibits significant antihypertensive activity. This compound is valuable for research applications in cardiovascular disease, specifically in studies focused on hypertension and vascular function.
  41. Calcium Channel Agonist

    RS 30026 is a potent calcium channel agonist that exhibits significant biological activity with a pEC50 value of 7.45. This compound is utilized in research to investigate the modulation of calcium signaling pathways, offering insights into various physiological processes and potential therapeutic interventions. Its ability to activate calcium channels makes it a valuable tool for studying cardiovascular, neurobiological, and muscle function research.
  42. Ca2+ Inward Current Blocker

    Antiarrhythmic agent-2 is a nonspecific blocker of Ca2+ inward currents, inhibiting ionic currents in the membranes of sensory neurons. This compound is valuable for investigating cardiovascular diseases, particularly arrhythmias, by modulating calcium ion dynamics and contributing to the understanding of electrophysiological mechanisms. Its applications extend to various research areas focusing on cardiac function and arrhythmic conditions.
  43. T-Type Calcium-Channel Antagonist

    NSC156529 is a potent antagonist of T-type calcium channels, specifically inhibiting Cav3.1 and Cav3.2 while showing no effect on Cav3.3. This compound exhibits significant biological activity that may be relevant for research into neuropsychic disorders and conditions affecting the genital system. Its targeted mechanism of action makes it a valuable tool for investigating the roles of T-type calcium channels in various pathophysiological processes.
  44. Stable Isotope

    Ranolazine-d8 is a deuterated form of Ranolazine, which primarily targets the late phase of inward sodium current (INa) and potassium current (IKr) with IC50 values of 6 μM and 12 μM, respectively. This compound functions as an anti-anginal agent, alleviating symptoms without influencing heart rate or blood pressure. Additionally, Ranolazine acts as a partial fatty acid oxidation inhibitor, making it valuable for research related to cardiac ischemia and metabolic modulation in heart diseases.
  45. Stable Isotope

    Verapamil-d3 is a deuterium-labeled form of Verapamil, a calcium channel blocker that serves as a potent, orally active first-generation inhibitor of P-glycoprotein (P-gp) and CYP3A4. This stable isotope variant is utilized in pharmacokinetic studies and metabolic research, aiding in the investigation of cardiovascular diseases such as hypertension, arrhythmias, and angina. Verapamil-d3's unique properties make it an invaluable tool for studying drug interactions and bioavailability in various biological systems.
  46. Calcium Channel Activator

    CGP 28392 is a calcium channel activator that enhances the activity of calcium-dependent processes. It is particularly effective in reactivating oxygen evolution in calcium-deficient photosystem II (PS II) particles, making it valuable for studies focused on photosynthesis and cellular signaling pathways. This compound is useful in biochemical research aimed at elucidating calcium dynamics and its role in various biological systems.
  47. Calcium Channel Blocker

    (R)-Lercanidipine is a selective calcium channel blocker that targets L-type calcium channels. This compound is primarily utilized for its antihypertensive effects, promoting vasodilation and reducing peripheral vascular resistance. Its pharmacological profile supports research in cardiovascular disease and hypertension management.
  48. Calcium Channel Blocker

    PD 122860 is a calcium channel blocker that also exhibits the ability to stimulate sodium channels. It is primarily utilized in research focused on cardiovascular and cerebrovascular diseases. By modulating calcium and sodium ion flux, PD 122860 contributes to understanding the underlying mechanisms of these conditions.
  49. Stable Isotope

    1-Octanol-d2-1 is a deuterated form of 1-Octanol, serving as a stable isotope for various research applications. As a saturated fatty alcohol, 1-Octanol acts as an inhibitor of T-type calcium channels with an IC50 value of 4 μM for native T-currents, making it valuable for studies in neurobiology and pharmacology. Additionally, its characteristics as a biofuel with diesel-like properties position it for investigation in energy research and sustainable technologies.
  50. Stable Isotope

    Norverapamil-d6 hydrochloride is a stable isotope-labeled version of Norverapamil, an N-demethylated metabolite of Verapamil. This compound acts as a blocker of L-type calcium channels and inhibits P-glycoprotein (P-gp) function. It is primarily utilized in pharmacokinetic studies, drug metabolism research, and for tracing metabolic pathways in biological systems.

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