Catalog No.
Product Name
Application
Product Information
Citations
-
Calcium Channel Inhibitor
Lidoflazine is a potent inhibitor of calcium channels, specifically known for its high affinity blockade of the HERG potassium channel. This compound exhibits antianginal properties, making it relevant in studies related to cardiac function and arrhythmias. Notably, Lidoflazine is associated with a risk of QT interval prolongation and ventricular arrhythmia, which underscores its importance in pharmacological research aiming to understand cardiovascular safety profiles. -
Calcium Channel
PPZ2 is a diacylglycerol (DAG)-activated agonist of the TRPC3, TRPC6, and TRPC7 calcium channels. It promotes neuronal development and survival through its ability to elicit cation currents and calcium ion (Ca(2+)) influx in cultured central neurons in a dose-dependent manner. PPZ2 induces BDNF-like neurite outgrowth and provides neuroprotection, effects that are negated following TRPC channel knockdown or inhibition. Additionally, PPZ2 enhances the activation of the calcium-dependent transcription factor cAMP response element binding protein, highlighting the role of calcium signaling in its neurotrophic actions. -
Anti-Anrhythmic Agent
Aprindine hydrochloride is an Ib-class anti-arrhythmic agent primarily targeting sodium channels (INa) to reduce the excitability and conduction velocity of cardiac muscle cells. By significantly inhibiting delayed potassium currents, it prolongs the atrial effective refractory period (AERP) and mitigates the risk of atrial fibrillation. Additionally, Aprindine hydrochloride modulates intracellular calcium ion concentration through the inhibition of Na+/Ca2+ exchange current (INCX), further enhancing the stability of cardiac electrical activity. This compound is suitable for research focused on atrial fibrillation (AF) and ventricular arrhythmias. -
Calcium Channel Inhibitor
Pranidipine is a potent, long-acting 1,4-dihydropyridine calcium channel inhibitor, specifically designed to modulate calcium influx in vascular smooth muscle cells. Its primary biological activity involves the reduction of blood pressure, making it an effective antihypertensive agent. This compound is widely used in cardiovascular research to investigate mechanisms underlying hypertension and to evaluate therapeutic strategies for managing elevated blood pressure. -
Calcium Influx Inhibitor
Carboxyamidotriazole Orotate is an orotate salt of Carboxyamidotriazole, a potent inhibitor of calcium influx. It acts primarily as a cytostatic agent targeting nonvoltage-operated calcium channels and disrupting calcium-mediated signaling pathways. This compound demonstrates notable anti-tumor, anti-inflammatory, and antiangiogenic properties, making it valuable in cancer research and the study of inflammatory diseases. -
L-type calcium channel Blocker
(R)-Nimodipine is an L-type calcium channel blocker that effectively penetrates the blood-brain barrier, with an IC50 value of 5 nM. By inhibiting calcium channels on the hypothalamic-pituitary-adrenal axis, (R)-Nimodipine reduces corticosterone release, thereby mitigating memory impairment and behavioral abnormalities associated with immobilization stress. This compound is frequently utilized in research focused on aneurysmal subarachnoid hemorrhage, cerebral ischemia, epilepsy, age-related neurodegenerative diseases, and the effects of alcohol intoxication. -
Calcium Channel Blocker
Nemadipine-A is a selective inhibitor of the EGL-19 L-type calcium channel. This compound demonstrates the ability to sensitize TRAIL-resistant cancer cells to TRAIL-mediated apoptosis. It is primarily utilized in research focused on cancer therapy and calcium signaling pathways. -
Calcium Channel Blocker
Methyl homoveratrate functions as a voltage-sensitive calcium channel blocker. This compound serves as a metabolite of RWJ-26240 and can be detected in plasma, urine, and fecal extracts. Its role in calcium channel inhibition makes it a valuable tool for investigating calcium signaling pathways and related physiological processes in various research applications. -
Anti-arrhythmic Agent
Aprindine is an Ib-class antiarrhythmic agent that primarily targets sodium channels (INa) to reduce the excitability and conduction velocity of cardiac muscle cells. Its ability to significantly inhibit delayed potassium currents prolongs the atrial effective refractory period (AERP), thereby helping to prevent atrial fibrillation. Additionally, Aprindine modulates intracellular calcium levels by inhibiting the Na+/Ca2+ exchange current (INCX), further stabilizing cardiac electrical activity. This compound is useful for research into atrial fibrillation (AF) and ventricular arrhythmias. -
TRPV1 Antagonist
A-425619 is a selective antagonist of the transient receptor potential type V1 (TRPV1), exhibiting oral bioactivity. It effectively inhibits capsaicin- and N-arachidonoyl-dopamine (NADA)-induced calcium influx in both dorsal root ganglia and trigeminal ganglia. A-425619 demonstrates efficacy in alleviating pathophysiological pain linked to inflammation and tissue injury in preclinical models. This compound is valuable for researching pain mechanisms associated with inflammatory conditions. -
Calcium Channel Antagonist
Praeruptorin C serves as a calcium channel antagonist, exhibiting a pD2′ value of 5.7. Derived from Peucedanum praeruptorum, this bioactive compound plays a significant role in modulating calcium influx across cellular membranes. Research applications include studies on cardiovascular function and smooth muscle contraction, making it a valuable tool for investigating calcium-related physiological processes. -
Ligand for the α2δ Subunit of Voltage-gated Calcium Channels
Crisugabalin is a selective ligand targeting the α2δ subunit of voltage-gated calcium channels, exhibiting an IC50 of 3.96 nM in rat models. This compound effectively inhibits the binding of [3H]gabapentin to the α2δ subunit, leading to reduced calcium influx and decreased neuronal excitability, ultimately impairing nociceptive transmission. Crisugabalin has demonstrated efficacy in alleviating mechanical allodynia and various pain models, including neuropathic and inflammatory pain. Its applications are relevant in research contexts involving chronic pain syndromes such as diabetic neuropathy, fibromyalgia, and postherpetic neuralgia. -
Calcium Channel Antagonist
(+)-Niguldipine hydrochloride is a calcium channel antagonist that effectively induces vasodilation by inhibiting calcium influx through cell membranes. This compound demonstrates significant biological activity by antagonizing U-46619-induced coronary vasoconstriction in guinea pig Langendorff heart preparations, with a pID50 value of 11.37. Additionally, it binds to calcium channels in guinea pig skeletal muscle membranes with a Ki of 9.75 and exhibits blood pressure-lowering effects in spontaneously hypertensive rats, with a pED30 of 7.1. (+)-Niguldipine hydrochloride is utilized in research related to cardiovascular diseases, including hypertension, angina pectoris, and arrhythmias. -
Calcium Channel Antagonist
Clopimozide is a calcium channel antagonist that inhibits [3H]nitrendipine binding with an IC50 value of 17 nM. This orally active antipsychotic agent is utilized in research to investigate both negative and positive symptoms of schizophrenia, contributing to a deeper understanding of the neurobiological mechanisms underlying this disorder. Its selective action on calcium channels allows for targeted studies in pharmacology and therapeutics related to schizophrenia. -
Calcium Channel Antagonist
BTT-266 is a calcium channel antagonist that functions by inhibiting the interaction between CaVα1-AID and CaVβ3, exhibiting a Ki value of 1.4 μM. It effectively modulates the activation of voltage-dependent CaV2.2 channels. BTT-266 demonstrates analgesic properties in models of neuropathic pain, making it a valuable tool for research into pain modulation and potential therapeutic applications. -
Calcium Channel
2-Chloro-ATP sodium is an analog of ATP that acts as an antagonist of the purinergic P2Y1 receptor, inhibiting intracellular calcium mobilization induced by ADP in Jurkat cells with a Ki of 2.3 μM. Additionally, it serves as an agonist for the purinergic P2X receptor, generating inward currents in HEK293 cells with varying affinities (EC50 of 0.5 and 2.5 μM). This compound also induces concentration-dependent relaxation of precontracted guinea pig cecal strips. Furthermore, 2-Chloro-ATP sodium is utilized to investigate substrate specificity among cyclic nucleotide-dependent protein kinases, including protein kinase A (PKA) and PKG. -
Calcium Channel Inhibitor
Nothofagin is a dihydrochalcone that acts as a calcium channel inhibitor. By blocking calcium influx, it downregulates NF-κB translocation, providing a mechanism to modulate inflammatory responses. This compound exhibits antioxidant properties and has potential applications in research related to septic responses and vascular inflammation. -
Calcium Channel Blocker
MONIRO-1 is a selective inhibitor of T-type and N-type calcium channels, demonstrating IC50 values of 34 µM, 3.3 µM, 1.7 µM, and 7.2 µM against hCav2.2, hCav3.1, hCav3.2, and hCav3.3, respectively, while exhibiting minimal activity against L-type calcium channels. Its ability to modulate calcium influx makes MONIRO-1 a valuable tool for research into pain pathways and epilepsy mechanisms. This compound is instrumental for studies focused on the pharmacological modulation of calcium channels in neuronal excitability. -
Nav Channel Blocker
ProTx-I is a potent blocker of voltage-gated Na+ channels, specifically inhibiting NaV1.2, NaV1.6, and NaV1.7 with IC50 values of 104 nM, 21 nM, and 95 nM, respectively. Additionally, ProTx-I exhibits significant activity as a CaV3.1 channel blocker, demonstrating IC50 values of 0.2 μM for hCaV3.1 and 31.8 μM for hCaV3.2. It also inhibits KV 2.1 channels (IC50: 411 nM) and TRPA1 (IC50: 389 nM). This multi-targeting profile makes ProTx-I valuable for research in neurobiology and pain signaling pathways. -
SERCA Inhibitor
CAD204520 dihydrochloride is a selective SERCA inhibitor with an IC50 of 0.34 μM. This compound specifically targets mutated NOTCH1 proteins, demonstrating significant relevance in the study of T-cell acute lymphoblastic leukemia (T-ALL) and mantle cell lymphoma (MCL). It is a valuable tool for research investigating the therapeutic potential and mechanisms of these cancers. -
Ca2+- ATPase Activator
Rp-8-Br-cGMPS sodium is a potent activator of Ca2+-ATPase, facilitating the reduction of cytosolic Ca2+ levels. This compound acts as an agonist of the rod cyclic nucleotide-gated (CNG) channel while also inhibiting protein kinase G (PKG). Its key biological activities make it valuable for research applications involving calcium signaling and cellular calcium homeostasis. -
SERCA Inhibitor
CAD204520 is a selective inhibitor of the Sarcoplasmic Reticulum Calcium ATPase (SERCA), demonstrating an IC50 value of 0.34 μM. This compound specifically targets mutated NOTCH1 proteins more effectively than wild-type, making it a valuable tool for studying T-cell acute lymphoblastic leukemia (T-ALL) and mantle cell lymphoma (MCL). CAD204520 is suitable for research aimed at understanding the molecular mechanisms and therapeutic strategies in these malignancies. -
Calcium Channel
Ned-K is a nicotinic acid adenine dinucleotide phosphate (NAADP) antagonist that targets calcium channels. It has been shown to effectively attenuate simulated ischemia and reperfusion (sIR)-induced calcium oscillations in cardiomyocytes. This compound serves as a valuable tool for research in cardiac physiology and the mechanistic study of calcium signaling pathways. -
Calcium Channel Inhibitor
Heteroclitin D is a lignan derived from Kadsura medicinal plants, functioning primarily as a calcium channel inhibitor. It exhibits significant biological activity by inhibiting L-type calcium channels, which are critical in various physiological processes. This compound is suitable for research applications focusing on calcium signaling, neuroprotection, and studies related to oxidative stress and lipid peroxidation. -
Calcium Channel Modulator
BBT is a calcium channel modulator that enhances glucose-stimulated insulin secretion (GSIS) while exhibiting anti-hyperglycemic activity. In models of type 2 diabetes, BBT protects pancreatic β-cells from cytokine- or streptozotocin-induced cell death. Its mechanism of action involves the cAMP/PKA signaling pathway and the long-lasting activation of L-type voltage-dependent calcium channels and CaMK2 pathways, making it a valuable tool for diabetic research and therapeutic studies. -
Calcium Channel Inhibitor
Yangambin is a furofuran lignan that functions as a calcium channel inhibitor, targeting voltage-gated Ca2+ channels. This compound effectively reduces intracellular calcium levels in vascular smooth muscle cells, promoting peripheral vasodilation. Additionally, Yangambin demonstrates antiallergic activity by inhibiting β-hexosaminidase release with an IC50 of 33.8 μM and exhibits anti-inflammatory properties with an IC50 of 37.4 μM, making it valuable for research in vascular biology and inflammation. -
Calcium Channel Antagonist
Anipamil is a calcium channel antagonist that primarily inhibits L-type calcium channels. This compound exhibits significant vasodilatory effects, making it valuable in the management of cardiovascular conditions. It has applications in both clinical and preclinical research settings centered around cardiovascular disease and related pharmacological studies. -
Calcium Channel Antagonist
Devapamil is a calcium channel antagonist that selectively inhibits L-type calcium channels. Its primary mechanism involves blocking calcium influx into cardiac and smooth muscle cells, which results in reduced contractility and vascular resistance. Devapamil exhibits significant antiarrhythmic activity and is utilized in research related to cardiovascular diseases, hypertension, and calcium signaling pathways. -
Calcium Channel Blocker
Cronidipine is a calcium channel blocker that primarily targets L-type calcium channels. It exhibits potent vasodilatory effects, making it valuable in cardiovascular disease research, particularly in the study of hypertension and related disorders. This compound aids in elucidating the mechanisms of calcium signaling and its implications in vascular function. -
Calcium Channel Antagonist
YS-201 is a dihydropyridine-type calcium channel antagonist that selectively inhibits L-type calcium channels. This compound exhibits significant biological activity in reducing calcium influx, which makes it a valuable candidate for the treatment of cardiovascular conditions such as angina pectoris and hypertension. Its role in calcium signaling research also supports investigations into related pathophysiological processes. -
Calcium Channel Inhibitor
PD0176078 is a selective N-type calcium channel inhibitor, primarily targeting voltage-gated calcium channels. It exhibits significant biological activity by effectively blocking calcium influx, which modulates neurotransmitter release and can influence pain signaling pathways. This compound is valuable for research applications focused on neuropharmacology and the investigation of pain mechanisms. -
Calcium Channel Blocker
Nemadipine B is a calcium channel blocker and an antagonist of EGL-19. It has been shown to induce Egl, Vab, and Gro phenotypes in Caenorhabditis elegans, making it a valuable tool for studying calcium signaling pathways and their effects on neuronal function. Its applications extend to various areas of research, including neurobiology and developmental biology, facilitating insights into calcium channel modulation in living organisms. -
Calcium Channel Antagonist
Calcium Channel Antagonist 2 (Compound 154) is a selective antagonist of calcium channels, exhibiting an IC50 range of 5-20 μM. This compound is instrumental in the exploration of calcium channel-mediated pathologies, including pain and diabetes. It serves as a valuable tool for understanding the role of calcium influx in various biological processes and the development of potential therapeutic strategies. -
N-type Calcium Channels Antagonist
Ziconotide is a potent and selective antagonist of N-type calcium channels. By blocking these channels, Ziconotide effectively reduces synaptic transmission and is utilized in chronic pain research. This peptide is an important tool for studying pain mechanisms and the physiological roles of calcium channel modulation in neuronal signaling. -
Calcium Channel Blocker
Amlodipine mesylate is a potent dihydropyridine calcium channel blocker that inhibits voltage-dependent L-type calcium channels, leading to decreased calcium influx. This mechanism results in vasodilation and reduced cardiac workload, making it an important agent in the study of hypertension and ischemic heart disease. Amlodipine mesylate is also being explored for its potential applications in cancer research due to its effects on vascular dynamics. -
Cav3.1/Cav3.2/Cav3.3 Inhibitor
ML218 hydrochloride is a selective inhibitor of T-type calcium channels, specifically Cav3.1, Cav3.2, and Cav3.3, exhibiting IC50 values of 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively. This compound effectively inhibits burst activity in subthalamic nucleus neurons and demonstrates minimal interference with L- or N-type calcium channels, KATP channels, or hERG potassium channels. Additionally, ML218 hydrochloride has the capability to penetrate the blood-brain barrier, making it a valuable tool for neurological research applications. -
Calcium Channel Antagonist
Mibefradil dihydrochloride hydrate is a potent calcium channel antagonist primarily targeting low-voltage-activated (T) calcium channels. This compound exhibits a higher affinity for T-type channels compared to high-voltage-activated (L) channels, making it an effective antihypertensive agent. Mibefradil dihydrochloride hydrate is utilized in research to investigate calcium signaling pathways and their implications in cardiovascular health. -
Stable Isotope
Ranolazine-d3 is a deuterated form of Ranolazine, an anti-anginal agent that primarily inhibits the late phase of inward sodium current (INa) with an IC50 value of 6 μM and IKr with an IC50 value of 12 μM, leading to its therapeutic effects without altering heart rate or blood pressure. Additionally, Ranolazine acts as a partial fatty acid oxidation (FAO) inhibitor. This compound serves as a valuable tool in cardiovascular research, particularly in studying sodium channel activity and metabolic modulation in heart physiology. -
Stable Isotope
(R)-Amlodipine-d4 is a stable isotope-labeled form of (R)-Amlodipine, primarily targeting calcium channels. This deuterated compound is utilized in pharmacokinetic studies and metabolic research to track drug metabolism and distribution in various biological systems. Its use aids in the understanding of the pharmacological effects and biological activity of (R)-Amlodipine in cardiovascular research. -
Calcium Channel Inhibitor
Etripamil hydrochloride is a potent L-type calcium channel inhibitor primarily used in the research of paroxysmal supraventricular tachycardia (PSVT). By blocking calcium influx through slow calcium channels, it effectively slows down atrioventricular node conduction and extends the refractory period of the atrioventricular node. This compound is valuable for studying cardiac electrophysiology and the mechanisms underlying arrhythmias. -
Stable Isotope
Lercanidipine-13C,d3 hydrochloride is a stable isotope-labeled form of Lercanidipine hydrochloride, a third-generation dihydropyridine calcium channel blocker (DHP-CCB). It exhibits prolonged antihypertensive effects and offers renoprotective benefits. This compound is valuable for pharmacokinetic studies and mechanistic research involving calcium signaling and cardiovascular physiology. -
CaVAb Inhibitor
UK-59811 hydrochloride is a Br-dihydropyridine derivative that functions as a potent inhibitor of the bacterial homotetrameric voltage-gated calcium channel, CaVAb, with an IC50 value of 194 nM. It serves as a valuable tool for studying calcium ion transport and its physiological implications in bacterial systems. Its specific action on CaVAb makes it suitable for research applications focused on calcium signaling and channel modulation. -
T-type Calcium Channel Inhibitor
IAA65 is a potent inhibitor of T-type calcium channels, exhibiting an IC50 value of 18.9 µM. This compound is primarily utilized in research related to epilepsy, aiding in the investigation of calcium channel modulation and its effects on neuronal excitability. IAA65 may facilitate the exploration of therapeutic strategies targeting T-type calcium channels for seizure management. -
Calcium Antagonist
UK 55444 is a calcium antagonist that primarily targets L-type calcium channels. It exhibits coronary vasodilator activity, making it relevant for research focused on cardiovascular physiology. UK 55444 is utilized in studies investigating the modulation of vascular tone and the role of calcium in myocardial function. -
Calcium Channel Blocker
Niludipine is an orally active calcium channel blocker primarily used for vasodilation and antihypertensive therapy. It has been shown to improve early fatal ventricular arrhythmias induced by acute myocardial ischemia in animal models. In addition, Niludipine effectively reduces left ventricular systolic and diastolic loads during pacing-induced angina pectoris. This compound is valuable for research into cardiovascular diseases, including coronary heart disease and myocardial ischemia. -
Calcium Channel
SB-237376 is a selective inhibitor of calcium channels, specifically targeting the L-type calcium current (I(Ca,L)) at elevated concentrations. Additionally, it effectively blocks the rapidly activating delayed rectifier potassium current (I(Kr)) with an IC50 value of 0.42 μM. This compound is valuable in studies focused on cellular signaling, cardiomyocyte function, and other physiological processes involving calcium channel modulation. -
Calcium Channel Antagonist
PD-217014-methyl ester is a calcium channel antagonist that acts as an αδ ligand, exhibiting significant visceral analgesic properties. This compound shows potential in inhibiting visceral hypersensitivity, and its anti-hyperalgesic effects are dose-dependent. It may be useful for research applications focused on pain management and the modulation of sensory signaling pathways. -
T-type Calcium Channel Inhibitor
IAB15 is a potent inhibitor of T-type calcium channels, which play a crucial role in regulating neuronal excitability and neurotransmitter release. This compound demonstrates significant activity in modulating calcium ion influx, making it a valuable tool in epilepsy research. Its ability to selectively target these channels positions IAB15 as an important reagent for studying calcium signaling pathways and their implications in seizure disorders. -
Calcium Channel
BBR 2160 is a dihydropyridine calcium channel antagonist that primarily targets voltage-gated calcium channels. This compound exhibits significant cardiac electrophysiological effects, including the reduction of myocardial contractility and prolongation of action potential duration. BBR 2160 is suitable for research applications focused on cardiac function and calcium signaling in cardiovascular studies. -
Potassium/Sodium Channel Inhibitor
Huwentoxin I is a peptide toxin that specifically inhibits voltage-gated sodium channels and N-type calcium channels. This compound has demonstrated significant inhibitory effects on sodium channels in both rat hippocampus and cockroach dorsal unpaired median (DUM) neurons, with IC50 values of 66.1 nM and 4.80 nM, respectively. Huwentoxin I is valuable for studies focused on neuronal excitability and channelopathy-related research applications.
