Catalog No.
Product Name
Application
Product Information
Citations
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BCRP/ABCG2 Inhibitor
3,7,2',4'-Tetramethoxy-5-hydroxyflavone is a potent inhibitor of the breast cancer resistance protein (BCRP/ABCG2), exhibiting an IC50 value of 5.98 μM. This compound is significant for research into multidrug resistance mechanisms in breast cancer, providing insights into potential therapeutic strategies to overcome treatment resistance. Its ability to modulate BCRP activity makes it a valuable tool in cancer pharmacology studies. -
BCRP Inhibitor
BCRP-IN-1 is a potent inhibitor of breast cancer resistance protein (BCRP), exhibiting IC50 values of 2.92 μM in the Hoechst 33342 assay and 2.46 μM in the Pheophorbide A assay. This compound is valuable for research applications targeting multidrug resistance in cancer cells, facilitating the study of therapeutic efficacy and drug transport mechanisms. Its selective inhibition of BCRP makes it an essential tool for understanding resistance pathways in oncology. -
Dihydropyridine Calcium Antagonist
(S)-Nimodipine is a potent dihydropyridine calcium antagonist known for its selective effect on calcium channels. It exhibits significant biological activity, primarily in the management of cerebrovascular disorders by improving cerebral blood flow. This compound is especially valuable in research focusing on neurological conditions and the effects of calcium modulation in neuronal tissue. -
Calcium Channel Blocker
Verapamil hydrochloride is a calcium channel blocker primarily targeting L-type calcium channels. It exhibits potent inhibitory activity on P-glycoprotein and CYP3A4, contributing to its pharmacological profile. This compound is widely utilized in research related to hypertension, cardiac arrhythmias, and angina, facilitating studies on cardiovascular function and drug metabolism. -
L-type Calcium Chanel Inhibitor
Diltiazem is an orally active L-type calcium channel blocker that exerts antihypertensive and antiarrhythmic effects. It is utilized in research related to cardiac arrhythmias, hypertension, and angina pectoris, making it valuable for studies focused on cardiovascular health. Its mechanism of action contributes to the modulation of calcium influx, which is critical in various cardiac and vascular functions. -
NMDA Receptor Inhibitor
Bupivacaine is an NMDA receptor inhibitor that modulates neuronal excitability by blocking sodium, L-calcium, and potassium channels. It exhibits potent inhibition of SCN5A channels, with an IC50 of 69.5 μM. This compound is primarily utilized in research focused on chronic pain mechanisms and therapeutic interventions. -
TRPM2 Agonist
Farnesyl pyrophosphate ammonium is an agonist of the TRPM2 channel, facilitating calcium influx and promoting cell death. It serves as a crucial intermediate in the mevalonate pathway, with significant roles in cholesterol and ubiquinone synthesis, as well as protein farnesylation. This compound is utilized in research focusing on cerebral ischemia, neurodegenerative diseases, pancreatic cancer, inflammation, and autoimmune disorders. -
TRPC6 Activator
Hyperforin dicyclohexylammonium salt is a selective activator of transient receptor potential canonical 6 (TRPC6) channels. By modulating Ca2+ flux, this compound influences a variety of biological processes and exhibits notable pharmacological activities, including anti-depression, anti-tumor, anti-dementia, and anti-diabetic effects. Additionally, Hyperforin dicyclohexylammonium salt has been shown to enhance the secretion of IL-17α from γδ T cells and demonstrates efficacy in improving psoriasis-like symptoms in the Imiquimod-induced mouse model. This compound serves as a valuable tool in research focused on calcium signaling and related therapeutic applications. -
Potassium Supplement
Potassium chloride, AR, 99.5% serves as an essential potassium supplement, playing a critical role in various biochemical applications. This compound is particularly valuable in research related to hyperkalemia, where it aids in studying potassium ion regulation in biological systems. Additionally, it functions as a potassium source in agronomy, contributing to plant nutrition and growth. -
Calcium Channels Antagonist
Fluspirilene is a non-competitive antagonist of L-type calcium channels, demonstrating an IC50 of 0.03 μM. This compound exhibits significant antipsychotic activity, making it a valuable tool for research on schizophrenia and related neuropsychiatric disorders. Its long-acting injectable formulation facilitates studies on sustained pharmacological effects in therapeutic applications. -
T Calcium Channel Antagonist
Ulixacaltamide is a potent T-type calcium channel antagonist that demonstrates significant efficacy in modulating neurological disorders. It has been shown to slow the progression of epilepsy and effectively reduce tremors in an alkaline tremor animal model. Additionally, Ulixacaltamide reverses thermal hyperalgesia, providing a mechanism for pain relief in various preclinical settings. This compound is valuable for research applications focusing on neurological function and pain management. -
SERCA Blocker
JTV-519 hemifumarate is a selective blocker of the sarcoplasmic reticulum Ca2+-stimulated ATPase (SERCA), with additional activity as a partial agonist of ryanodine receptors in striated muscle. It exhibits antiarrhythmic and cardioprotective properties, making it a valuable tool for research on cardiac function and rhythm disorders. This compound is useful in studies exploring calcium handling in myocardial cells and its implications for heart disease therapies. -
T-type Calcium Channel Blocker
TTA-P2 is a selective T-type calcium channel blocker with a primary mechanism of inhibiting calcium influx through T-type channels, exhibiting an IC50 of 22 nM. This compound demonstrates significant biological activity by reducing mechanical hypersensitivity and alleviating both acute and chronic pain. Additionally, TTA-P2 lowers firing rates in neurons associated with temporal lobe epilepsy, effectively controlling synaptically evoked burst firing. Research applications include investigations into neurological disorders such as tremor and absence epilepsy. -
Calcium Channel Inhibitor
Tetracaine hydrochloride is a calcium channel inhibitor that effectively blocks the voltage-sensitive release of Ca2+ from the sarcoplasmic reticulum. This compound exhibits significant biological activity and is primarily utilized in topical applications within ophthalmology, as well as serving as an antipruritic agent. Its mechanism of action makes it valuable for research in pain relief and modulation of calcium signaling pathways. -
Neuroprotective Compound
REM127 is a neuroprotective small molecule that modulates calcium homeostasis in cells. It effectively restores calcium balance in cellular models affected by the pathological accumulation of tau protein, demonstrating potential to mitigate synaptic and cognitive deficits in Alzheimer's disease models. REM127 is capable of crossing the blood-brain barrier and may slow the progression of amyloid-beta and tau protein pathologies. This compound is suitable for research applications in neurodegenerative diseases. -
SERCA2a Activator
SERCA2a Activator 1 is an activator of the sarco/endoplasmic reticulum Ca2+-dependent ATPase 2a (SERCA2a). This compound alleviates the inhibitory effects of phospholamban, thereby improving both systolic and diastolic cardiac functions. SERCA2a Activator 1 is primarily utilized in research related to heart failure and cardiac physiology. -
Potassium Channel Blocker
Azimilide dihydrochloride is a class III antiarrhythmic agent that functions primarily as a potassium channel blocker, targeting both IKs and IKr channels with IC50 values of 2.6 μM and 1 μM, respectively. Additionally, it inhibits the HERG channel at frequencies of 0.1 and 1 Hz, with IC50 values of 1.4 μM and 5.2 μM. Azimilide dihydrochloride also suppresses L-type calcium current and sodium current, with IC50 values of 17.8 μM and 19 μM, respectively. This compound is valuable for researching conditions such as atrial fibrillation and ventricular fibrillation. -
Calcium Ions Activator
Calcium citrate tetrahydrate is a calcium ions activator that efficiently releases calcium ions, enhancing biological activity in various applications. Its rapid solubility and ability to maintain elevated calcium ion concentrations make it particularly useful for research focused on bone formation and mineralization. This reagent is essential for studies investigating calcium-related signaling pathways and the effects of calcium on cellular processes. -
Calcium Channel Blocker
Prenylamine is a calcium channel blocker belonging to the amphetamine chemical class. It acts by inhibiting calcium influx through voltage-gated calcium channels, leading to vasodilation. This compound has potential applications in the research of cardiovascular conditions, particularly angina pectoris, by modulating vascular tone and reducing myocardial oxygen demand. -
Stable Isotope
Verapamil-d3 hydrochloride is a deuterium-labeled derivative of the calcium channel blocker, verapamil hydrochloride. It serves as a potent inhibitor of P-glycoprotein (P-gp) and CYP3A4, facilitating detailed pharmacological studies. This stable isotope is primarily utilized in research related to hypertension, cardiac arrhythmias, and angina, providing insight into drug metabolism and transport mechanisms in various biological systems. -
Ca2+-ATPase Inhibitor
IPrAuCl is a gold compound that functions as a selective inhibitor of sarcoplasmic reticulum Ca2+-ATPase, demonstrating an IC50 value of 16.3 µM. Its primary mechanism involves hindering calcium ion transport, making it a valuable tool for researching calcium homeostasis and muscle contraction dynamics. IPrAuCl may also be useful in studies investigating the role of Ca2+-ATPase in various cellular processes and diseases. -
Calcium Receptor Activator
γ-Glutamylserine (γ-Glu-Ser) is a calcium receptor activator that plays a critical role in various cellular signaling pathways. This compound exhibits potential neuroprotective effects, making it relevant for research in Parkinson's disease. Additionally, γ-Glutamylserine may be utilized in studies focused on metabolic disorders, including diabetes and obesity. -
mNCX Blocker
ITH12575 is a potent and selective blocker of the mitochondrial sodium-calcium exchanger (mNCX). This compound effectively reduces calcium influx through CALHM1 channels at low micromolar concentrations. ITH12575 is valuable for research applications focused on calcium homeostasis, cell signaling, and mitochondrial function. -
Phenylalkylamine Calcium Antagonist
Gallopamil hydrochloride is a phenylalkylamine calcium antagonist that exhibits potent antiarrhythmic and vasodilatory properties. It effectively inhibits acid secretion in a concentration-dependent manner, with an IC50 value of 10.9 μM. This compound is utilized in various research applications focused on cardiovascular function and gastrointestinal acid regulation. -
NMDA Receptor Inhibitor
Bupivacaine-d9 is a deuterium-labeled analog of Bupivacaine, primarily targeting NMDA receptors. This compound exhibits inhibitory effects on sodium, L-calcium, and potassium channels, with a notable potency against SCN5A channels, characterized by an IC50 value of 69.5 μM. Bupivacaine-d9 is utilized in research related to chronic pain mechanisms and the modulation of excitatory neurotransmission, offering valuable insights into therapeutic applications in pain management. -
Calcium Channel
D-myo-Inositol-1,3,4,5-tetraphosphate sodium functions as a signaling molecule by regulating calcium channels. It is produced through the phosphorylation of inositol 1,4,5-trisphosphate by inositol 1,4,5-triphosphate 3-kinase. This compound is utilized in research focused on cellular signaling pathways, particularly those involving calcium mobilization and inositol phosphate metabolism. Its key biological activity makes it valuable for studies exploring neurotransmission, smooth muscle contraction, and other calcium-dependent processes. -
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.
