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Catalog No.
Product Name
Application
Product Information
Citations
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Calcium Channel Blocker, Cholesterol Acyltransferase Inhibitor
Belfosdil functions as a selective calcium channel blocker while also inhibiting acyl coenzyme A cholesterol acyltransferase (ACAT). This dual action contributes to its role in modulating calcium influx and lipid metabolism. Belfosdil is utilized in research focused on cardiovascular and metabolic diseases, exploring its potential for therapeutic applications. -
Cavα2δ1/NET Inhibitor
Cavα2δ1&NET-IN-2 is a dual inhibitor targeting the α2δ-1 subunit of voltage-gated calcium channels and the norepinephrine transporter (NET). It demonstrates effective inhibition of Cavα2δ-1 with a Ki of 454 nM and exhibits potent inhibition of NET with a Ki of 59 nM and an IC50 of 7 nM. This compound is valuable for research focused on pain mechanisms and the associated neurotransmitter systems. -
Calcium Channel Inhibitor
Levosemotiadil is a calcium channel inhibitor that demonstrates increased binding affinity to human serum albumin (HSA) compared to its R-isomer. Research utilizing high-performance frontal analysis (HPFA) indicates that levosemotiadil binds approximately three times more strongly to HSA than semotiadil, with specific interactions at the diazepam binding site. The binding affinity of both enantiomers is diminished in the presence of diazepam, while warfarin shows no effect. These properties underscore levosemotiadil's potential as a Ca- and Na-channel blocker, making it a valuable compound for exploring its pharmacokinetics and therapeutic applications. -
Calcium Channels Inhibitor
ω-Grammotoxin SIA is a selective inhibitor of P/Q and N-type voltage-gated calcium channels, derived from spider venom. This protein toxin is instrumental in studying calcium's role in neuronal and cardiovascular signaling pathways. Its unique mechanism allows researchers to explore its potential applications in understanding and treating various neurological and cardiovascular diseases. -
α2δ-1 Inhibitor
(rel)-Mirogabalin is an inhibitor of the α2δ-1 subunit of voltage-dependent calcium channels. It is primarily used in research focused on neuropathic pain modulation and may also play a role in studying anxiety disorders. Its ability to regulate calcium influx makes it a significant compound for investigating therapeutic potentials in calcium-related pathophysiologies. -
Calcium Channel Inhibitor
(S)-Lercanidipine is a calcium channel blocker that exhibits antihypertensive and neuroprotective activities. It effectively reduces oxidative stress and has been shown to protect auditory sensory hair cells from noise-induced damage. In vitro studies demonstrate that (S)-Lercanidipine enhances cell viability, particularly at lower concentrations, and significantly lowers the hearing threshold in mice following noise exposure. Its antioxidant properties are characterized by an increase in the expression of antioxidant enzyme genes and a decrease in oxidative enzyme gene expression, suggesting its potential for mitigating noise-induced hearing loss and preserving outer hair cell viability. -
Cavα2δ1/NET Inhibitor
Cavα2δ1&NET-IN-1 is a dual inhibitor targeting the α2δ-1 subunit of voltage-gated calcium channels and the norepinephrine transporter (NET). This compound demonstrates inhibition of Cavα2δ-1 with a Ki value of 112 nM, and inhibits NET with a Ki of 383 nM and an IC50 of 67 nM. Cavα2δ1&NET-IN-1 is suitable for research applications focused on pain mechanisms and related therapeutic pathways. -
Calcium Channel Inhibitor
Cav 3.2 inhibitor 2 is a selective inhibitor of Cav3.2 T-type Ca2+ channels, exhibiting an IC50 of 0.09339 μM under a -80 mV holding potential. This compound effectively reduces T-channel-dependent somatic and visceral pain in murine models, making it a valuable tool for investigating intractable pain mechanisms. Its ability to modulate calcium channel activity positions Cav 3.2 inhibitor 2 as a significant agent in pain research and therapeutic development. -
Calcium Channel Inhibitor
Pincainide is a calcium channel inhibitor that specifically targets voltage-gated calcium channels in smooth muscle. It effectively reduces calcium influx, leading to the inhibition of norepinephrine- and high potassium-induced contractile responses. Pincainide is relevant in the study of cardiovascular diseases, providing insights into mechanisms related to smooth muscle function and regulation. -
Cavα2δ1/NET Inhibitor
Cavα2δ1&NET-IN-3 is a selective inhibitor targeting the α2δ subunit of voltage-gated calcium channels (VGCC) and the noradrenaline transporter (NET). This compound exhibits inhibitory constants (Kis) in the range of 100-500 nM for the human α2δ-1 subunit of the Cav2.2 calcium channel and for NET. Cavα2δ1&NET-IN-3 is utilized in research applications focused on pain modulation and neurotransmitter regulation, contributing to the understanding of various neurological disorders. -
Calcium Channel inhibitor
Calcium Channel Antagonist 4 is a potent inhibitor of voltage-gated calcium channels, exhibiting an IC50 value within the range of 5-20 μM. This compound's ability to selectively block calcium influx makes it a valuable tool for studying calcium signaling pathways in various cellular processes. It is particularly useful in research applications related to neurology, cardiology, and muscle physiology. -
SERCA Inhibitor
CXL 017 is a selective inhibitor of the sarco/endoplasmic reticulum Ca2+-ATPase (SERCA), functioning by competing with ATP for binding and thereby inhibiting ATPase activity. This compound demonstrates notable cytotoxicity specifically against multidrug-resistant acute myeloid leukemia cells, such as HL60/MX2. CXL 017 is valuable in research related to multidrug-resistant acute myeloid leukemia and offers insights into potential therapeutic approaches for overcoming drug resistance in cancer. -
Calcium Channel Inhibitor
A-1048400 is a selective calcium channel inhibitor that demonstrates potent activity against N-type and T-type calcium channels, with IC50 values of 1.4 μM and 1.2 μM, respectively. By inhibiting neurotransmitter release and reducing membrane hyperexcitability, A-1048400 exhibits significant analgesic properties. This compound is particularly valuable for investigating mechanisms and treatments related to neuropathic pain, such as that resulting from spinal nerve ligation and chronic constriction injury. -
Cav3.2 Inhibitor
Cav 3.2 inhibitor 3 is a selective inhibitor of the Cav3.2 T-type calcium channel, exhibiting an IC50 of 0.1534 μM. This compound demonstrates minimal binding affinity for D2 receptors, making it a valuable tool for studying the role of Cav3.2 channels in various physiological processes. Its use is particularly relevant in research areas focused on neuronal excitability and pain modulation. -
Calcium Channel Inhibitor
TTA-P1 is a potent inhibitor of human T-type calcium channels, exhibiting state-independent characteristics. This compound is crucial for studying various physiological processes such as neuronal burst firing, hormone secretion, and cell proliferation. TTA-P1 is particularly valuable for research related to absence epilepsy and other neurological disorders linked to calcium signaling. -
Calcium Channel Inhibitor
Agelenin is a polypeptide composed of 35 amino acids, functioning primarily as a calcium channel inhibitor. Isolated from the Agelena opulenta spider, this compound exhibits structural similarity to insect-specific calcium channel inhibitors, making it a valuable tool for studying calcium signaling pathways. Research applications include investigations into neuromuscular transmission and calcium-dependent cellular processes. -
L-/T-type Calcium Channel Inhibitor
HM12 is a covalent inhibitor targeting L-/T-type calcium channels, specifically Cav1.2 and Cav3.2, while demonstrating selectivity for N-type channels. This compound induces irreversible inhibition that remains effective post-washout, making it a valuable tool for investigating calcium channel dynamics. HM12 is applicable in research focused on various diseases, including hypertension, pain, and epilepsy, facilitating the exploration of calcium channel modulation in therapeutic contexts. -
Calcium Channel Inhibitor
ω-Hexatoxin-Hv1a is a selective inhibitor of L-type voltage-dependent calcium channels. This neurotoxin reduces intracellular calcium ion concentration, thereby mitigating apoptosis, necroptosis, and oxidative stress, while enhancing cellular recovery and energy levels. Its ability to induce paralysis and mortality in insects through the disruption of central nervous system neurotransmission underscores its potency, although it has limited oral toxicity. Consequently, ω-Hexatoxin-Hv1a is a valuable tool for research into ischemia-reperfusion injury, atopic dermatitis, and ischemic damage in cardiomyocytes and neurons. -
T-Type Calcium Channel Inhibitor
T-Type Calcium Channel Inhibitor 2 is a selective inhibitor of T-type calcium channels, specifically targeting Cav3.1 (α1G), Cav3.2 (α1H), and Cav3.3 (α1I), with IC50 values of 31.0, 83.1, and 69.3 µM, respectively. This compound exhibits significant cytotoxic activity against A549 and HCT-116 cancer cell lines, with IC50 values of 5.0 and 6.4 µM. It serves as a useful tool in the investigation of calcium channel involvement in various physiological processes and potential therapeutic targets in cancer research. -
SERCA Inhibitor
4,4'-Methylenebis(2,6-di-tert-butylphenol) is a selective inhibitor of sarco/endoplasmic reticulum calcium ATPase (SERCA), with an IC50 value of 17 μM. This compound plays a critical role in modulating calcium homeostasis and is valuable for research into cellular processes and disorders linked to calcium dysregulation. Its application extends to studying various diseases where altered calcium signaling is implicated. -
Calcium Channel Inhibitor
A-39355 is a calcium channel inhibitor that effectively reverses multidrug resistance in tumor cells. It enhances the cytotoxicity of antitumor compounds by increasing their accumulation within resistant cells and inhibiting their efflux. Unlike traditional calcium antagonists, A-39355 exhibits minimal hypotensive effects. This compound is particularly useful for research focused on overcoming treatment resistance in cancer therapy. -
L-type Calcium Channel Inhibitor
Diltiazem malate is a potent inhibitor of L-type calcium channels, effectively modulating calcium influx in cardiac and vascular smooth muscle. It exhibits significant antihypertensive and antiarrhythmic properties, making it valuable for the investigation of cardiovascular conditions. Diltiazem malate is commonly used in research related to cardiac arrhythmia, hypertension, and angina pectoris. -
P-glycoprotein Inhibitor
Niguldipine monohydrochloride is a selective P-glycoprotein inhibitor known for its action as a calcium channel blocker. It demonstrates significant anticancer properties by inhibiting Cav 3.2, with an IC50 of 0.9 μM. This compound is primarily utilized in tumor research to explore its effects on drug resistance and the transport of therapeutic agents across cellular membranes. -
Calcium Channel Inhibitor
Piprofurol is a potent calcium channel inhibitor that effectively reduces calcium-induced contractions in isolated potassium depolarized rat aorta preparations in a concentration-dependent manner. This compound demonstrates the ability to relax K+-induced contractions in both dog coronary arteries and rabbit basilar arteries. Additionally, Piprofurol exhibits a negative inotropic effect on guinea-pig papillary muscle, with an EC50 value of 5 μM, highlighting its potential utility in cardiovascular research and related studies. -
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 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 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. -
SERCA Inhibitor
2,5-Di-tert-butylhydroquinone is a potent inhibitor of Sarco/endoplasmic reticulum Ca2+ ATPase (SERCA), demonstrating an IC50 of 400 nM. This compound disrupts the gating function of Glu309, thereby preventing calcium ions from accessing their binding site. Additionally, 2,5-Di-tert-butylhydroquinone influences the activity of key enzymes such as 5-lipoxygenase and COX-2, with IC50 values of 1.8 μM and 14.1 μM, respectively. It is utilized in research focused on cellular calcium regulation and inflammatory processes. -
Calcium Channel Inhibitor
Ethosuximide is a calcium channel inhibitor primarily targeting T-type calcium channels, specifically blocking low voltage-activated currents. This compound is extensively used in research for its anti-epileptic properties as well as its potential therapeutic effects in various neurodegenerative disease models. Ethosuximide facilitates the study of calcium signaling pathways and their involvement in neuronal excitability and degeneration. -
T-channels Inhibitor
1-Octanol is a saturated fatty alcohol that selectively inhibits T-type calcium channels, demonstrating an IC50 of 4 μM for native T-currents. This compound serves as a valuable tool in pharmacological research aimed at understanding calcium signaling pathways. Additionally, its properties as a biofuel with diesel-like characteristics make it an interesting candidate for energy applications. -
Ca2+ Channel Inhibitor
Ethaverine hydrochloride is a potent inhibitor of L-type calcium channels, primarily affecting cardiac tissues. It serves as a peripheral vasodilator and antispasmodic agent, demonstrating significant biological activity in relaxing smooth muscle. This compound is commonly utilized in research related to peripheral vascular disease and its associated disorders. -
Auxin Transport Inhibitor
3,4,5-Triiodobenzoic acid is an auxin transport inhibitor that modulates auxin distribution in plant systems. This compound enhances specific [3H]verapamil binding in zucchini microsomes and rabbit skeletal muscle membranes, highlighting its potential role in studying calcium channel interactions. 3,4,5-Triiodobenzoic acid is valuable for research focused on smooth muscle contraction and the biochemical pathways influencing plant hormone transport.
