Calcium Channels

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  1. CRAC inhibitor

    RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM.
  2. VK-II-36 is a carvedilol analog that suppresses sarcoplasmic reticulum (SR) Ca(2+) release but does not block the β-receptor.
  3. MCU modulator

    MCU-i4 is a novel negative modulator of the MCU, binding MICU1 and impairing muscle cell growth.
  4. calcium channel antagonist

    SM-6586 is a calcium channel antagonist and inhibitor of Na+/H+ and Na+/Ca2+ exchange transport, potentially for the treatment of cerebrovasular diseases and hypertension.
  5. dihydropyridine Ca2+ antagonist

    CV-159 is a unique dihydropyridine Ca2+ antagonist with an anti-calmodulin (CaM) action, and has antiinflammatory activities.
  6. Calcium Channel Inhibitor

    Gabapentin enacarbil (XP-13512) is a prodrug for the anticonvulsant and analgesic drug gabapentin.
  7. non-voltage dependent calcium channel blocker

    Carboxyamidotriazole (L 651582) is a blocker of non-voltage dependent calcium channel.
  8. calcium channel inhibitor

    Bay-K-8644 (R)-(+)- is a calcium channel inhibitor. Bay-K-8644 (R)-(+)- inhibits Ba2+ currents (IBa) (IC50=975 nM).
  9. L-type Ca2+ channel agonist

    (S)-(-)-Bay-K-8644 is an agonist of L-type Ca2+ channel. (S)-(-)-Bay-K-8644 activates Ba2+ currents (IBa) (EC50=32 nM).
  10. calcium-sensing receptor (CaR) antagonist

    SB-423562 is a short-acting calcium-sensing receptor (CaR) antagonist.
  11. phenylalkylamine calcium antagonist

    Gallopamil (Methoxyverapamil), a methoxy derivative of Verapamil, is a phenylalkylamine calcium antagonist.
  12. T-type Ca2+ channel antagonist

    TTA-Q6 is a selective T-type Ca2+ channel antagonist, used in the neurological disease.
  13. Ionomycin calcium (SQ23377 calcium) is a potent, selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus.
  14. Calcium channel blocker

    Levamlodipine besylate ((S)-Amlodipine besylate) is a powerful dihydropyridine calcium channel blocker, possessing vasodilation properties and used in the treatment of hypertension and angina.
  15. dual T-type and L-type calcium channel blocker

    Efonidipine Hcl (NZ-105) is a dual T-type and L-type calcium channel blocker (CCB).
  16. Calcium channel blocker

    Verapamil is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor.

  17. Calcium channel antagonist

    Felodipine is a 1,4-dihydropyridine antagonist and calcium channel protein inhibitor.

  18. vasodilator drug

    Pentamethonium bromide is a vasodilator drug.
  19. 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.
  20. T-type calcium channel Blocker

    KTt-45 is a selective T-type calcium channel blocker that exhibits significant anticancer activity. This compound induces apoptosis in the HeLa cervical cancer cell line, making it a valuable tool for studying the mechanisms of cancer cell death. Its ability to modulate calcium signaling has implications for research in cancer therapeutics and cellular physiology.
  21. 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.
  22. Calcium Channel Blocker

    14-Deoxyandrographolide is a diterpene known for its calcium channel blocking activity, functioning as a uterine smooth muscle relaxant. It enhances nitric oxide (NO) release in endothelial cells, contributing to vasodilation. Additionally, 14-Deoxyandrographolide modulates liver cell sensitivity to TNF-α mediated apoptosis by promoting the release of TNFRSF1A, making it a valuable compound for research into vascular health and liver cell biology.
  23. 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.
  24. 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.
  25. Calcium Channel Blocker

    Dotarizine is a selective calcium channel blocker that functions by inhibiting Ca2+ influx. This compound demonstrates significant antimigraine activity through its modulation of calcium signaling pathways. Additionally, Dotarizine reduces the release of lactate dehydrogenase and exhibits the capacity to block 5-HT receptors, making it a valuable tool for research in neural signaling and migraine pathophysiology.
  26. Calcium Channel Blocker

    Levemopamil hydrochloride is a calcium channel blocker that effectively penetrates the blood-brain barrier and acts as a 5-HT2 antagonist. This compound exhibits key biological activity in modulating calcium influx, making it valuable for research related to temporary occlusion and various neurological diseases. It serves as a useful tool for studying the effects of calcium channel modulation on neuronal function and pathophysiology.
  27. Calcium Channel Blocker

    Levemopamil is a calcium channel blocker known for its ability to antagonize 5-HT2 receptors. It demonstrates renoprotective properties, particularly in the context of ischemic acute kidney injury. This compound is suitable for research involving ischemic acute renal failure and related nephroprotective studies.
  28. Calcium Antagonist

    Nexopamil is a calcium antagonist that targets Ca2+ channels, as well as 5-HT2, 5-HT1A, 5-HT1C, and dopamine D2 receptors. This compound demonstrates significant vasodilatory and cardioprotective properties, along with the ability to inhibit platelet aggregation. Nexopamil is useful for research focused on conditions such as stable and unstable angina, as well as potentially in studies of peripheral arterial occlusive disease.
  29. Calcium Channel Blocker

    Nitrendipine is a dihydropyridine calcium channel blocker primarily acting on L-type calcium channels. It exhibits significant antihypertensive properties and has been shown to induce apoptosis in various cellular contexts, including neuroblastoma. Additionally, Nitrendipine alleviates withdrawal symptoms associated with alcohol and morphine and reduces right ventricular hypertrophy and pulmonary vascular alterations induced by intermittent hypoxia. Its diverse biological activities make it valuable in research related to cardiovascular health and cancer biology.
  30. Calcium Channel Blocker

    Lercanidipine hydrochloride is a third-generation dihydropyridine calcium channel blocker with a primary mechanism of selectively inhibiting vascular calcium channels. Its potent antihypertensive effects are complemented by reno- and neuro-protective properties, making it valuable for research into cardiovascular and neurological conditions. Additionally, Lercanidipine exhibits anti-oxidant, anti-inflammatory, and anti-apoptotic activities, further supporting its utility in various biomedical applications.
  31. L-type Calcium Channel Blocker

    Fendiline is an L-type calcium channel blocker that exhibits an IC50 of 17 µM. In addition to its role in cardiovascular modulation, Fendiline acts as a selective inhibitor of K-Ras, with an IC50 of 9.64 μM, effectively preventing K-Ras plasma membrane localization and blocking downstream signaling. This compound has demonstrated potential in inhibiting the proliferation of various cancer cell lines such as pancreatic, colon, lung, and endometrial cancers that express oncogenic mutant K-Ras. Furthermore, Fendiline serves as a STING agonist, showing promise in inhibiting the growth of refractory cold tumors, including MC38, CT26, and B16F10.
  32. Calcium Channel Agonist

    (2R,3R)-Butane-2,3-diol functions as a reversible agonist of lanthanum-sensitive calcium channels in bacteria, specifically Escherichia coli, with an EC50 of approximately 25 mM. This compound interacts with calcium channel proteins, promoting channel opening and facilitating extracellular calcium influx, which leads to intracellular calcium transients. Such activity plays a crucial role in regulating bacterial physiological processes, including growth, metabolism, and signal transduction. Additionally, (2R,3R)-Butane-2,3-diol is valuable for investigating bacterial-host cell signaling dynamics and studying conditions like lactose intolerance and other related gastrointestinal disorders.
  33. Antiarrhythmic Agent

    HNS-32 is an antiarrhythmic agent that demonstrates vasodilatory effects, providing protective benefits against ischemic and reperfusion arrhythmias in canine hearts. This compound exhibits significant negative chronotropic effects on mammalian ventricular myocardium, highlighting its potential for applications in acute coronary syndrome research. HNS-32 serves as a valuable tool for exploring the mechanisms and treatment options for cardiac arrhythmias.
  34. Calcium Entry-Blocking

    YM-430 is a calcium entry-blocking and beta-adrenoceptor-blocking agent. It effectively inhibits Amifampridine-induced rhythmic contractions with an IC50 value of 59.2 nM and blocks arginine vasopressin-induced ST-segment depression with an IC50 of 36.6 mg/kg. This compound is valuable for research into angina pectoris and related cardiovascular conditions.
  35. Calcium Antagonist

    F-0401 is a calcium antagonist that exerts its effects through antagonism of the platelet-activating factor receptor (PAFR). This compound demonstrates significant potential in neurological research, particularly in studies related to stroke and related pathologies. Its ability to modulate calcium signaling pathways makes F-0401 a valuable tool for investigating therapeutic strategies in the context of neuroprotection and cerebrovascular disorders.
  36. Calcium Influx/NO Modulator

    Palmitoylglycine (N-palmitoyl glycine) is an endogenous lipid that functions as a modulator of calcium influx and nitric oxide production in sensory neurons. This compound is associated with an increased risk of Brugada syndrome (BrS) and interacts with various BrS-related proteins, displaying moderate binding affinities for DCC, CR1, CTSB, NAAA, DEFB1, EPHA1, IGF1/IGFBP3/ALS, and LTA. Palmitoylglycine is valuable in research investigating its roles in neuronal signaling and cardiovascular conditions linked to BrS.
  37. 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.
  38. Calcium Channel Blockers

    Levamlodipine hydrochloride is a dihydropyridine calcium channel blocker that primarily targets L-type calcium channels on vascular smooth muscle cells. By inhibiting calcium ion influx, it promotes vasodilation, effectively lowering blood pressure and alleviating angina. Additionally, its binding affinity to human serum albumin (HSA) enhances research into drug transport and release mechanisms within the body. This compound is beneficial for studies focused on cardiovascular therapies and mechanisms of action related to hypertension and coronary artery disease.
  39. 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.
  40. Calcium Channel Blocker

    Levamlodipine besylate hemipentahydrate is a calcium channel blocker that exhibits significant antioxidant and vasodilatory effects. This compound has been shown to lower serum malondialdehyde (MDA) levels while enhancing superoxide dismutase (SOD) activity, thereby mitigating oxidative stress. Levamlodipine besylate hemipentahydrate is suitable for research applications focused on vascular dementia, hypertension, and cerebrovascular diseases.
  41. Endogenous Metabolite

    N-Stearoyl Taurine is an endogenous metabolite that exhibits activity as a fatty acyl amide. It demonstrates the ability to activate members of the transient receptor potential (TRP) family of calcium channels, linking it to various physiological processes. This compound is primarily used in research applications related to lipidomics and neurobiology, particularly in studies investigating the role of amino-acyl endocannabinoids in the central nervous system. Its discovery in rat brain lipid profiles underscores its significance in the exploration of neuronal signaling pathways.
  42. Endogenous Metabolite

    N-Lignoceroyl Taurine is an endogenous metabolite and taurine conjugate of lignoceric acid, identified through lipidomic analysis of bovine brain. This compound exhibits distinct biological activity as a substrate for fatty acid amide hydrolase (FAAH), with levels significantly elevated in FAAH knockout mice, indicating a potential role in lipid metabolism. Additionally, N-Lignoceroyl Taurine has been shown to activate transient receptor potential (TRP) calcium channels, including TRPV1 and TRPV4, highlighting its relevance in neurobiology and cellular signaling research.
  43. Biochemical Reagent

    D-myo-Inositol-4,5-diphosphate sodium is a critical biochemical reagent that functions as a second messenger in cellular signaling pathways. It primarily targets calcium channels, facilitating the release of intracellular calcium when it binds to its receptor on the endoplasmic reticulum. This compound is valuable for research applications investigating signal transduction, calcium homeostasis, and cellular responses in various biological systems.
  44. Stable Isotope

    rac Felodipine-(Methoxy-d3) is a deuterium-labeled analog of rac Felodipine, a potent calcium channel blocker that primarily targets L-type calcium channels. This stable isotope variant is useful for pharmacokinetic studies, metabolic tracing, and isotopic labeling in drug development research. Its deuterium labeling enhances the analytical sensitivity and specificity in mass spectrometry applications, facilitating the investigation of drug absorption, distribution, metabolism, and excretion (ADME) profiles.
  45. Isotope-Labeled Compounds

    Cilnidipine-d3 is a deuterium-labeled derivative of Cilnidipine, primarily acting as a calcium channel blocker. This isotope-labeled compound is valuable for research applications involving pharmacokinetic studies and metabolic profiling. Its use enhances the understanding of Cilnidipine's pharmacological effects and its interactions within biological systems.
  46. Stable Isotope

    Cinnarizine-d8 dihydrochloride is a deuterium-labeled form of the calcium channel blocker Cinnarizine. This stable isotope compound allows for precise tracking and analysis in pharmacokinetic studies. It is primarily utilized in research applications involving metabolic studies and the investigation of drug interactions, enhancing the understanding of pharmacological mechanisms.
  47. Calcium Channel Blocker

    Verapamil-d6 hydrochloride is a deuterated derivative of Verapamil, a selective calcium channel blocker. It exhibits potent inhibition of P-glycoprotein (P-gp) and CYP3A4, making it valuable in cardiovascular research, particularly for conditions such as hypertension, arrhythmias, and angina. This isotopically labeled compound aids in pharmacokinetic studies and offers insights into drug metabolism and transport mechanisms.
  48. Stable Isotope

    N-Desalkylflurazepam-d4 is a deuterated analog of N-Desalkylflurazepam, a long-acting metabolite of benzodiazepine compounds, including Flurazepam. This stable isotope is primarily used for research applications involving metabolic studies and pharmacokinetics of benzodiazepines. N-Desalkylflurazepam exhibits inhibitory effects on L-type voltage-gated calcium channels, with reported IC50 values of 55 μM for Cav1.2 and 37 μM for Cav1.3, making it a valuable tool for investigating calcium channel modulation in various biological contexts.
  49. Stable Isotope

    Nifedipine dehydro nitroso-d6 is a deuterium-labeled derivative of Nifedipine dehydro nitroso, primarily utilized as a stable isotope. This compound plays a crucial role in the study of pharmacokinetics and metabolic pathways of calcium channel blockers. Its isotopic labeling facilitates advanced analytical techniques such as mass spectrometry in chemical research applications.
  50. Stable Isotope

    Desacetyl Diltiazem-d3 is a deuterium-labeled derivative of Desacetyl Diltiazem, designed to serve as a stable isotope standard in analytical applications. This compound can be employed in pharmacokinetic studies and metabolic labeling to trace drug interactions and bioavailability. Its precise labeling enhances accuracy in mass spectrometry and other analytical techniques, making it an invaluable tool for researchers investigating calcium channel blocking activities and cardiovascular-related pharmacology.

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