Membrane Transporters-Ion Channels

Items 1751-1800 of 2532

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

    Sadopine serves as an allosteric modulator of dihydropyridine-sensitive L-type calcium channels. The compound exhibits dual functionality, with (-)Sadopine acting as a positive allosteric modulator and (+)Sadopine functioning as a negative allosteric modulator. This modulation of calcium channel activity makes Sadopine relevant for research focused on cardiovascular physiology and the modulation of calcium signaling pathways.
  30. Calcium Channel Inhibitor

    Ro 18-3981 is a dihydropyridine compound that selectively inhibits calcium channels in cardiac tissues. It demonstrates enhanced inhibitory potency at depolarized membrane potentials, with an IC50 value of 2.3 nM at -20 mV and 100 nM at -50 mV. This compound is useful for studying the role of calcium signaling in cardiac physiology and related pathologies.
  31. Calcium Absorption Inducer

    PDDHV is a potent calcium absorption inducer that stimulates the vanillic acid receptor VR1, leading to increased influx of 45Ca2+. It effectively promotes 45Ca2+ uptake in rat dorsal root ganglion neurons with an EC50 of 70 nM and elicits calcium mobilization in VR1-transfected CHO cells with an EC50 of 125 nM. Additionally, PDDHV inhibits [3H]-resiniferatoxin binding to rat dorsal root ganglion membranes, showcasing its utility in calcium signaling research.
  32. Potassium/Calcium Channel Blocker

    SB-237376 free base is a potent inhibitor of potassium and calcium channels, primarily targeting the rapidly activating delayed rectifier potassium current I(Kr) with an IC50 of 0.42 μM. Additionally, at elevated concentrations, it effectively blocks the L-type calcium current I(Ca,L). In studies utilizing rabbit ventricular models, SB-237376 free base has been shown to induce early afterdepolarizations (EADs) at a concentration of 3 µM. This compound presents a lower proarrhythmic risk compared to other known I(Kr) inhibitors, making it valuable for investigations into arrhythmia-related conditions.
  33. Ca2+- ATPase Activator

    Rp-8-Br-cGMPS (Rp-8-bromo-Cyclic GMP sodium salt) is an effective activator of Ca2+-ATPase, promoting the reduction of cytosolic Ca2+ levels by enhancing the efflux of Ca2+ from cells. Additionally, it acts as an agonist of the rod cyclic nucleotide-gated (CNG) channel and functions as an inhibitor of protein kinase G (PKG). This compound is valuable for studies involving calcium signaling, cellular response mechanisms, and cardiovascular research.
  34. Stable Isotope

    Teludipine-d6 is a deuterium-labeled analog of Teludipine hydrochloride, a potent lipophilic calcium channel blocker. This stable isotope is utilized in pharmacokinetic studies and metabolic research to trace the metabolic pathways of Teludipine without altering its pharmacological properties. It is well-suited for investigations requiring precise quantification of drug concentrations in biological systems.
  35. Calcium Channel Blocker

    (S)-Azelnidipine is a selective calcium channel blocker that specifically targets L-type calcium channels. This compound exhibits significant biological activity by inhibiting calcium influx, which can lead to vasodilation and reduced cardiac workload. It is primarily utilized in research related to cardiovascular diseases, offering insights into hypertension and other related conditions.
  36. Calcium Channel Inhibitor

    R 56865 is a calcium channel inhibitor that offers cardiomyocyte protection against digitoxin (ouabain)-induced myocardial calcium overload. This compound demonstrates a significant protective effect against digitoxin-induced intoxication, as evidenced in studies utilizing guinea pig papillary muscle. R 56865 is primarily utilized in research related to cardiac function and the mechanisms of arrhythmias.
  37. Calcium Channel Blocker

    Tamolarizine hydrochloride is a calcium channel blocker that effectively crosses the blood-brain barrier to inhibit calcium influx in neurons. This compound is valuable for studying neuronal activity and modulating calcium-dependent processes in nervous system research. Its unique properties make it an important tool for investigating neurological disorders and calcium signaling pathways.
  38. Calcium Antagonist

    BMS-188107 is a calcium antagonist that demonstrates anti-ischemic effects. This compound enhances post-ischemic contractile function and decreases lactate dehydrogenase release, making it a valuable tool in cardiovascular research. It is suitable for studies investigating calcium modulation and its impact on heart function and ischemic injury.
  39. L-type Calcium Channel Blocker

    Norverapamil, an N-demethylated metabolite of Verapamil, acts as an L-type calcium channel blocker and inhibits P-glycoprotein (P-gp) function. This compound is primarily utilized in research to study calcium ion dynamics and assess the role of P-gp in drug transport and resistance mechanisms. Its ability to modulate calcium influx makes it valuable for applications in cardiovascular and neuropharmacological investigations.
  40. Calcium Indicator

    Rhod-FF tripotassium is a cell-impermeant calcium indicator targeting intracellular calcium levels, with a dissociation constant (Kd) of 320 μM. This derivative of Rhod-2 exhibits fluorescent properties, emitting light upon calcium ion binding, with excitation at 552 nm and emission at 580 nm. It is widely used in research applications to explore calcium dynamics and signaling within cellular environments.
  41. Calcium Channel Antagonist

    Calcium Channel Antagonist 5 is a potent inhibitor of calcium channels, exhibiting a pIC50 of 5.50. This compound effectively modulates calcium influx in cells, making it valuable for studies in cardiovascular research and neuropharmacology. It is particularly useful in investigating the role of calcium channels in cellular excitability and signal transduction.
  42. RyR2 Stabilizer

    RyR2 stabilizer-1 is a potent stabilizer of the ryanodine receptor 2 (RyR2) and an activator of the sarco/endoplasmic reticulum Ca2+ ATPase 2a (SERCA2a), exhibiting EC50 values of 2.7 μM for RyR2 and 383 nM for SERCA2a. This compound effectively inhibits calcium leakage from the sarcoplasmic reticulum through RyR2 while enhancing the reuptake of calcium by SERCA2a. As a result, RyR2 stabilizer-1 shows promise in preventing cardiac arrhythmias by maintaining calcium homeostasis in cardiac cells.
  43. Calcium Channel Modulator

    Calcium channel-modulator-1 is an orally active agent that targets calcium channels, effectively inhibiting aortic contraction with an IC50 of 0.8 μM. This modulator is useful for investigating cardiovascular conditions and mechanisms associated with calcium signaling in vascular tissues.
  44. Calcium Channel

    β-Amino Acid Imagabalin Hydrochloride is a selective ligand for the α2δ subunit of voltage-dependent calcium channels. This compound modulates calcium influx, thereby regulating neurotransmitter release and exhibiting anticonvulsant properties. It is primarily utilized in research focused on pain management, anxiety disorders, and seizure activity.
  45. Calcium Channel Modulator

    Myomodulin is a neuropeptide that functions as a calcium channel modulator. It plays a critical role in neurotransmission and muscle contraction by regulating calcium ion flow in excitable tissues. Myomodulin is widely used in research to investigate neurophysiological processes and the modulation of synaptic activity in various model organisms, including molluscs and insects.
  46. Calcium Channel Antagonist

    AE0047 Hydrochloride is a calcium channel antagonist that effectively inhibits calcium influx through the cell membrane. This compound demonstrates potential in the study of hypertensive diseases, making it a valuable tool for investigating cardiovascular physiology and related pathologies. Its role in modulating calcium signaling pathways can aid in understanding the mechanisms underlying hypertension and related disorders.
  47. Mineralocorticoid Receptor Modulator

    Felodipine 3,5-Dimethyl Ester is a dihydropyridine derivative functioning primarily as a mineralocorticoid receptor modulator and a selective inhibitor of the voltage-dependent L-type calcium channel CaV1.2. This compound exhibits significant pharmacological activity by affecting calcium ion flux, which plays a crucial role in cardiovascular and renal physiology. Its applications extend to research in hypertension, heart failure, and other cardiovascular disorders related to calcium channel dysregulation.
  48. UT-B Inhibitor

    UT-B-IN-1 is a reversible, competitive inhibitor targeting the urea transporter-B (UT-B) with IC50 values of 10 nM for human and 25 nM for mouse UT-B. It demonstrates low toxicity and high selectivity for UT-B over UT-A isoforms. UT-B-IN-1 significantly increases urine output and reduces urine osmolality in murine models, making it a valuable tool for research into diuretic mechanisms and kidney function studies.
  49. UT-A Inhibitor

    PU-48 is a selective inhibitor of urea transporters A (UT-A), exhibiting an IC50 of 0.32 μM. This compound demonstrates significant diuretic activity in mouse models while showing minimal cytotoxicity. PU-48 presents a valuable tool for investigating renal physiology and has potential applications in the development of diuretic therapies.
  50. Non-steroidal Compound

    Butibufen is an orally active non-steroidal compound that primarily targets cyclooxygenase enzymes. It exhibits significant analgesic and antipyretic properties, making it a valuable tool for the study of pain and fever mechanisms. This compound is applicable in research focused on inflammation and related pathological conditions.

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