Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
Furin Inhibitor
BOS-318 is a highly selective and cell-permeable inhibitor of furin, exhibiting an IC50 value of 1.9 nM. This compound demonstrates the ability to protect epithelial sodium channels (ENaC) from activation by neutrophil elastase. BOS-318 is a valuable tool for research focused on cystic fibrosis and related pulmonary conditions. -
Endogenous Metabolite
D-myo-Inositol-1,4,5,6-tetraphosphate (D-Ins(1,4,5,6)P4) functions primarily as an endogenous metabolite involved in cellular signaling pathways. This compound exhibits a strong inhibitory effect on calcium-activated chloride channels, effectively operating at concentrations of 8-10 μM. It is commonly utilized in research applications focused on signal transduction and ion channel regulation. -
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. -
Endogenous Metabolite
Stearoyl serotonin is a hybrid compound designed to target the endogenous metabolite systems and is structurally derived from arachidonoyl serotonin. This compound is investigated for its ability to function as a dual antagonist of fatty acid amide hydrolase (FAAH) and the TRPV1 channel, which are critical pathways in the modulation of pain. Preliminary studies suggest that modifications to the arachidonoyl structure, such as the introduction of an 18-carbon stearoyl moiety, may influence TRPV1 channel activity; replacement with saturated fatty acids has demonstrated significant inhibition of capsaicin-induced activation. This positions stearoyl serotonin as a potential candidate for research into pain mechanisms and therapeutic applications. -
Endogenous Metabolite
SU200 is a TRPV1 agonist that modulates intracellular calcium ion concentrations. It induces distinct calcium ion response patterns, displaying notable reactivity and peak efficacy. The effects of SU200 exhibit varying degrees of response delay and variability across different cell types. This compound offers potential avenues for pharmacological development and further research into calcium signaling pathways. -
Endogenous Metabolite
UCCF-029 free base is a potent activator of the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel. This compound showcases enhanced activity due to the benzannulation of the flavone A-ring at the 7,8-position, serving as a critical structural reference for the development of more effective flavonoid analogues. UCCF-029 demonstrates superior potency compared to apigenin in activating wild-type CFTR and possesses potential for activating the mutant G551D-CFTR, though its efficacy in this regard is not as pronounced as that of apigenin. This reagent is valuable for research into cystic fibrosis and related therapeutic strategies. -
Endogenous Metabolite
ISQ-1 hydrochloride is an isoquinolinone compound that functions as an inhibitor of the IKur potassium channel. It demonstrates potential to influence cardiac electrophysiology by modulating arrhythmic activity in atrial tissues. This reagent is primarily utilized in research focused on cardiac rhythm disorders and electrophysiological studies of heart functions. -
Antiarrhythmic Agent
Droxicainide hydrochloride is an antiarrhythmic agent primarily targeting sodium channels. It is effective in the management of ventricular arrhythmias and is utilized in research to investigate cardiac electrophysiology. The compound is valuable for studying interactions in cardiac tissues and assessing the effects of sodium channel modulation on heart rhythm disorders. -
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. -
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. -
Natural Products
Thevetin A is a cardiac glycoside derived from the plant Cascabela thevetioides. It exhibits potent biological activity by inhibiting Na+/K+ ATPase, leading to increased intracellular calcium levels and enhanced contractility of cardiac muscle. This compound is primarily utilized in cardiovascular research to study its effects on cardiac function and potential therapeutic applications in heart disease. -
Endogenous Metabolite
N-Oleoyl Taurine is an endogenous metabolite that acts as an amino-acyl endocannabinoid. It is known to activate transient receptor potential (TRP) channels, specifically TRPV1 and TRPV4, implicating its role in calcium signaling. This compound has been isolated from rat brain and presents potential applications in research studying the physiological effects of TRP channel modulation and its involvement in neurological functions. -
Stable Isotope
Safinamide-d4-1 is a deuterium-labeled derivative of Safinamide, a selective and reversible inhibitor of monoamine oxidase B (MAO-B) with an IC50 of 0.098 μM, demonstrating significantly lower inhibition of MAO-A (IC50=580 μM). In addition to its MAO-B inhibitory activity, Safinamide also interacts with sodium channels and modulates glutamate release, exhibiting a greater affinity at depolarized potentials (IC50=8 μM) compared to resting potentials (IC50=262 μM). This reagent is valuable for research applications related to neurobiology, particularly in the investigation of Parkinson's disease and ischemic stroke mechanisms.
