Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
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. -
UT-A1/UT-B Urea Transporter Inhibitor
UTA1inh-D1 is a selective inhibitor of the UT-A1 and UT-B urea transporters, exhibiting IC50 values of 3.8 μM and 15 μM, respectively. This compound shows potential in the study of refractory edema conditions, including congestive heart failure and cirrhosis. Its unique mechanism of action makes it a valuable tool for exploring urea transport modulation in various pathological contexts. -
UT-A1/UT-B Inhibitor
UTA1inh-A1 is a selective inhibitor of urea transporters UT-A1 and UT-B, demonstrating IC50 values of 3.3 μM and 16 μM, respectively. This compound is primarily utilized in research focused on urea transport and its implications in diuretic therapy. UTA1inh-A1 aids in elucidating the physiological roles of urea transporters and their potential as therapeutic targets for urea-related conditions. -
UT-A Inhibitor
UTA1inh-C1 is a selective inhibitor of the urea transporter UT-A, demonstrating an IC50 of 4.2 μM. This compound effectively modulates urea transport, making it a valuable tool for studying renal physiology and urea homeostasis. Its application in research can help elucidate the role of UT-A in various physiological processes and the impact of urea transport dysregulation in pathological conditions. -
VDAC1 Inhibitor
VBIT-4 is a selective inhibitor of voltage-dependent anion channel 1 (VDAC1) oligomerization, exhibiting a binding affinity of 17 μM. This compound is recognized for its potential to inhibit apoptosis, making it suitable for therapeutic investigations in apoptosis-related conditions, including neurodegenerative and cardiovascular diseases. Researchers may utilize VBIT-4 to explore its effects on cell survival and disease progression in relevant biological models. -
VDAC1 Inhibitor
VBIT-12 is a potent inhibitor of Voltage-Dependent Anion Channel 1 (VDAC1) that functions by directly binding to the channel and preventing its oligomerization. This interaction effectively inhibits the pro-apoptotic actions mediated by VDAC1. VBIT-12 is valuable in studies aimed at elucidating the role of VDAC1 in apoptosis and mitochondrial function, making it a key reagent for research in cell death pathways and mitochondrial-related diseases. -
HK2 Inhibitor
HK2-IN-4 is a selective inhibitor of hexokinase 2 (HK2) with an IC50 value of 0.79 μM and a Kd value of 0.41 μM. It disrupts the interaction between HK2 and voltage-dependent anion channel 1 (VDAC1), leading to reduced lactate and ATP levels in cancer cells. Additionally, HK2-IN-4 promotes the activation of apoptosis pathways, evidenced by an increased p-AMPK/AMPK ratio and elevated Bax levels, alongside decreased Bcl2 levels. This compound is applicable in research focusing on colorectal cancer and non-small cell lung cancer, particularly in models with high HK2 expression. -
VDAC1 Inhibitor
AKOS-22 is a selective inhibitor of the mitochondrial protein VDAC1 (voltage-dependent anion channel 1), exhibiting an affinity with a Kd of 15.4 μM. This compound prevents VDAC1 oligomerization and inhibits apoptosis, thereby offering protection against mitochondrial dysfunction. AKOS-22 serves as a valuable tool in research focused on mitochondrial biology and related pathways in disease. -
VDAC1 Inducer
SW016789 is a potent inducer targeting the voltage-dependent anion channel 1 (VDAC1). It effectively promotes insulin hypersecretion and enhances Ca2+ influx in pancreatic β-cells, leading to a transient endoplasmic reticulum (ER) stress response without inducing cell death. This compound exhibits reversible and non-apoptotic properties, making it a valuable tool for exploring β-cell dysfunction associated with type 2 diabetes mellitus (T2DM). -
VDAC1 Inhibitor
VBIT-3 is a selective inhibitor of voltage-dependent anion channel 1 (VDAC1) oligomerization, exhibiting a binding affinity (Kd) of 31.3 μM. It functions as an apoptosis inhibitor, providing potential therapeutic applications in managing apoptosis-related disorders, including neurodegenerative and cardiovascular diseases. This reagent is valuable for research focused on understanding the biochemical pathways of apoptosis and exploring treatment strategies for related conditions. -
Antineoplastic Agent
Tuvatexib is an antineoplastic agent that inhibits cancer cell proliferation by targeting specific pathways involved in tumor growth. It exhibits significant cytotoxic activity against various cancer cell lines, making it a valuable tool for cancer research. Applications include the study of cancer cell metabolism and the evaluation of combination therapies in preclinical models. -
Antitumor Agent
Tyroservatide is a low-molecular-weight polypeptide recognized for its antitumor properties. It has demonstrated efficacy against hepatocellular carcinoma and lung cancer cells, making it a valuable tool for cancer research. Tyroservatide is utilized in studies aimed at elucidating its mechanisms of action and potential therapeutic applications in oncology. -
P-gp Inhibitor
P-gp Inhibitor 25 is a potent inhibitor of P-glycoprotein (P-gp), which plays a critical role in drug transport and multidrug resistance. This compound enhances the oral bioavailability of paclitaxel, making it valuable in cancer therapy research. Its application in studies focused on overcoming P-gp-mediated drug resistance positions P-gp Inhibitor 25 as a significant tool in the development of effective anticancer treatments.
