Catalog No.
Product Name
Application
Product Information
Citations
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α9α10 nAChR/CaV2.2 Antagonist
GeX-2 is a truncated analogue of αO-conotoxin that serves as an antagonist of the α9α10 nicotinic acetylcholine receptor (nAChR) and CaV2.2 channels. This compound demonstrates significant analgesic properties, effectively alleviating pain in rat models exhibiting chronic constriction injury. GeX-2 is valuable in research focusing on pain mechanisms and the modulation of excitatory neurotransmission through its interactions with nAChR and calcium channels. -
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. -
Calcium Channel Blocker
RWJ 22108 is a bronchoselective calcium channel blocker that inhibits calcium influx in smooth muscle cells, demonstrating an IC50 value of 5.7 nM in the calcium-dependent contraction of canine bronchiolar smooth muscle. This compound is primarily utilized in research applications focused on respiratory physiology and the study of bronchial hyper-reactivity. Its specificity for bronchial tissues makes it a valuable tool in exploring mechanisms of airway relaxation and potential therapeutic interventions for respiratory disorders. -
α-Obscurine Derivative
α-Obscurine derivative-1 is a derivative of α-Obscurine that specifically targets CaV3.1 ion channels, exhibiting an inhibitory effect with an IC50 of 0.19 μM. This compound is valuable for research into neurological disorders, providing insights into calcium channel modulation and its implications in neurological function. Its unique properties make it a useful tool for exploring the role of ion channels in various pathophysiological conditions. -
Calcium Antagonist
SL-870495 is a calcium antagonist that selectively targets L-type calcium channels. It exhibits significant potential in investigating cardiovascular diseases, particularly hypertension and angina pectoris, by regulating calcium influx in cardiac and vascular smooth muscle cells. This compound is valuable for research applications aimed at understanding calcium-mediated mechanisms in cardiovascular pathology. -
Calcium Channel Blocker
Diproteverine hydrochloride is a calcium channel blocker that primarily targets L-type calcium channels, inhibiting calcium influx into cells. This compound exhibits significant antianginal properties, making it useful in research related to cardiovascular diseases. Additionally, studies have indicated that Diproteverine hydrochloride may have implications in embryonic toxicity assessment, highlighting its relevance in developmental biology research. -
Calcium Channel Ligand
PD-217014 is an α2δ ligand targeting calcium channels, demonstrating significant visceral analgesic activity. This compound effectively inhibits visceral hypersensitivity reactions, exhibiting a dose-dependent anti-allodynic effect. It serves as a valuable tool in research related to pain management and the mechanisms underlying visceral pain. -
Calcium Channel Blocker
Bencyclane fumarate is a potent vasodilating calcium channel blocker. It has demonstrated efficacy in attenuating mucosal damage in a rat model of intestinal ischemia-reperfusion injury. This compound serves as a valuable tool for research into peripheral arterial occlusive diseases and related vascular conditions. -
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 Antagonist
AH-1058 is a potent calcium channel antagonist primarily targeting L-type Ca2+ channels. This compound exhibits significant antiarrhythmic activity by effectively delaying premature ventricular complexes and preventing ventricular fibrillation in experimental arrhythmia models. AH-1058 has shown efficacy in suppressing ventricular tachycardia and ventricular fibrillation in reperfusion-induced arrhythmia models, making it a valuable tool for research in cardiac arrhythmias and related therapeutic approaches. -
Calcium Antagonist
S-312 is a calcium antagonist characterized by a bicyclic dihydrothienopyridine structure. This compound effectively relaxes helical strips of isolated rabbit arteries that have been pre-contracted with high potassium depolarization. S-312 acts as a competitive inhibitor of calcium-induced contractions in depolarized basilar and femoral arteries, and it also prolongs AV nodal conduction time in Langendorff-perfused isolated rabbit hearts. Additionally, S-312 demonstrates vasculoselectivity, particularly targeting cerebral vessels, making it a valuable tool for cardiovascular research applications. -
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. -
Calcium Channel Antagonist
FPL 62129 is a calcium channel antagonist that exhibits significant vasodilatory effects. It is effective in reducing blood pressure and total peripheral resistance while enhancing cardiac contractility and cardiac output in anesthetized beagle models. This reagent is valuable for research applications focusing on cardiovascular physiology and the modulation of vascular tone. -
Calcium Antagonist
MCI-176 is a calcium antagonist that selectively inhibits calcium-induced constriction in coronary arteries. This compound demonstrates significant capacity to modulate vascular tone, making it valuable for studying cardiovascular function and related pathologies. MCI-176 is particularly useful in research focusing on the mechanisms of calcium signaling and potential therapeutic interventions for coronary artery diseases. -
IP3 Receptor Modulator
Adenophostin A is a potent modulator of inositol 1,4,5-trisphosphate receptors (IP3) that functions as a calcium (Ca2+) releaser, exhibiting an IC50 of 1.3 nM and an EC50 of 1.4 nM in rat models. This compound effectively stimulates Ca2+ release from intracellular stores and microsomes, inhibits the binding of [3H]IP3 to plasma membrane receptors, and activates chloride channels. Notably, Adenophostin A is resistant to phosphorylation and dephosphorylation by metabolic enzymes, thereby sustaining its activity and enhancing cytoplasmic Ca2+ levels in vascular smooth muscle cells. This reagent is highly relevant for research on hemorrhagic shock and related physiological studies. -
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. -
Antitumor Compound
S 16317 is an orally active dihydropyridine derivative that demonstrates low affinity for calcium channels (Ki: 0.55 μM). It effectively inhibits P-glycoprotein-mediated efflux of doxorubicin (ADR), thus potentially reversing multidrug resistance in tumor cells. This compound is particularly relevant for research in cancer biology and the development of novel therapeutic strategies against resistant tumors. -
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. -
N-type Calcium Channel Antagonist
Huwentoxin XVI is a selective antagonist of N-type calcium channels, demonstrating a potent inhibitory effect with an IC50 of approximately 60 nM. Derived from the Chinese tarantula Ornithoctonus huwena, it serves as an analgesic and exhibits no activity against voltage-gated T-type calcium channels, potassium channels, or sodium channels. This specificity makes Huwentoxin XVI valuable in research aimed at understanding pain mechanisms and the role of calcium channels in various physiological processes. -
T-type Calcium Channel Antagonist
TTA-A8 is a potent T-type calcium channel antagonist, demonstrating an IC50 value of 31.3 nM in the FLIPR depolarization assay. This compound exhibits favorable pharmacokinetic properties, making it an ideal candidate for research applications focused on epilepsy and sleep disorders. Its short-acting profile allows for detailed studies into the physiological roles of T-type calcium channels in related conditions. -
Broad-Spectrum Antiepileptic Agent
JNJ-26990990 is a broad-spectrum antiepileptic agent that primarily targets voltage-gated sodium channels and N-type calcium channels. It exhibits significant anticonvulsant activity, making it suitable for the study of various seizure models. Although it shows minimal inhibition of human carbonic anhydrase-II with an IC50 of 110 μM, its primary applications lie in the investigation of epilepsy and related neurological disorders. -
Antihypertensive Agent
Vatanidipine hydrochloride is an orally active dihydropyridine (DHP) calcium channel blocker that primarily functions as an antihypertensive agent. It exhibits vasodilatory effects, resulting in reduced vascular resistance, and additionally inhibits the release of noradrenaline from sympathetic nerve endings. This dual action makes Vatanidipine hydrochloride valuable in research related to hypertension and cardiovascular health. -
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. -
Sodium/Calcium Channel Blocker
KT 2-230 is a sodium and calcium channel blocker that exhibits significant anti-inflammatory properties. This compound is utilized in research applications focused on neuropathic pain and various inflammatory conditions. Its ability to modulate ion channel activity makes it a valuable tool for studying the underlying mechanisms of synaptic transmission and neuroprotection. -
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. -
Ca2+ Channel α2δ Ligand
PD-0299685 is a potent ligand for the Ca2+ channel α2δ subunit. This compound exhibits significant potential in the study of refractory genito-urinary pain conditions, including interstitial cystitis and bladder pain syndrome. Its ability to modulate calcium channel activity makes it a valuable tool in pain research and related therapeutic investigations. -
Calcium Antagonists
KT-362 free acid is an intracellular calcium antagonist that exhibits antiarrhythmic and vasodilatory properties. It antagonizes norepinephrine-induced vasoconstriction by reducing inositol phospholipid hydrolysis, leading to decreased intracellular calcium mobilization. This reagent is suitable for investigating the mechanisms of contraction and relaxation in vascular smooth muscle, particularly the roles of intracellular calcium dynamics and inositol phospholipid pathways in vascular contraction. -
Calcium Channel Blocker
RS-5773 is a calcium channel blocker that acts as a congener of diltiazem. This compound exhibits antianginal properties and is distinguished by its minimal impact on hypotension and atrioventricular conduction, making it suitable for cardiovascular research. RS-5773 can be utilized in studies focused on calcium dynamics in cardiac function and related therapeutic applications. -
Ca2+-Channel Antagonist
Monatepil maleate is a potent orally active calcium channel antagonist that functions as a noncompetitive ACAT inhibitor. It has demonstrated the ability to decrease blood pressure and enhance plasma lipid metabolism. This compound shows promise for research applications related to hyperlipidemia and cardiovascular health. -
Calcium Antagonist
Semotiadil is a benzothiazine compound that functions as a calcium antagonist. It demonstrates significant antiplatelet activity, making it valuable for research into cardiovascular diseases and thrombotic disorders. Semotiadil can be used to explore mechanisms related to calcium signaling and its role in platelet function and aggregation. -
Calcium Channel Blocker
Nicardipine-d3 hydrochloride is a deuterium-labeled analog of Nicardipine hydrochloride, a potent calcium channel blocker. It effectively inhibits cardiac calcium channels, exhibiting an IC50 of 1 μM. This compound is utilized in research related to cardiovascular diseases, particularly for studying conditions such as chronic stable angina and hypertension management. -
ATPase
Creatine phosphokinase, Rabbit muscle (CPK) is an enzyme that catalyzes the reversible conversion of creatine and ATP into phosphocreatine and ADP. By facilitating the maintenance of an optimal ATP/ADP ratio, CPK plays a critical role in energy metabolism, particularly during periods of high energy demand. This enzyme is widely used in biochemical research to study cellular energy dynamics and various metabolic disorders. -
BCRP Inhibitor
5,7-Dimethoxyflavone is a potent inhibitor of the Breast Cancer Resistance Protein (BCRP). It exhibits significant biological activities, including anti-obesity, anti-inflammatory, and antineoplastic effects. Additionally, this compound has been shown to inhibit cytochrome P450 (CYP) 3A enzymes, making it valuable for research applications focused on drug resistance and metabolic pathways in cancer therapy. -
Sodium Channel Blocker
CAY10568 is a sodium channel blocker that modulates neuronal excitability. This compound, a derivative of QX-314, exhibits a smaller and less hydrophobic profile, making it suitable for exploring its effects on inflammation and pain perception. CAY10568 is valuable for research applications aimed at understanding pain mechanisms and developing analgesic therapies. -
Sodium Channel Inhibitor
(-)-Sparteine sulfate pentahydrate is a sodium channel inhibitor that acts as a class 1a antiarrhythmic agent. It has demonstrated notable biological activity in modulating cardiac excitability and can be utilized in research focusing on arrhythmias and pharmacological studies related to ion channel function. This reagent is suitable for investigating the effects of sodium channel blockade in various biological models. -
Nav1.7 Inhibitor
Nav1.7-IN-6 is a selective inhibitor targeting the voltage-gated sodium channel Nav1.7, which is important in pain signaling pathways. This compound demonstrates significant biological activity in modulating neuronal excitability, making it a valuable tool for research on pain mechanisms and potential therapeutic interventions in pain disorders. Its specificity for Nav1.7 enhances its utility in elucidating the role of this channel in nociception and related studies. -
NaV1.7 Antagonist
AMG8379 is a selective sulfonamide antagonist targeting the voltage-gated sodium channel NaV1.7. It demonstrates potent inhibition with IC50 values of 8.5 nM for human NaV1.7 and 18.6 nM for mouse NaV1.7, effectively blocking TTX-sensitive sodium channels in dorsal root ganglia (DRG) neurons with an IC50 of 3.1 nM. This compound is useful for research applications related to pain pathways and sodium channel modulation. -
Sodium Channel Inhibitor
B-GYKI-38233 hydrochloride is a sodium channel inhibitor that exhibits potent antiarrhythmic properties. This compound is utilized in research focused on the modulation of sodium channels, which play a critical role in cardiac excitability and conductivity. Its mechanism of action makes it a valuable tool for the investigation of arrhythmias and related cardiovascular disorders. -
Nav1.8 channel Inhibitor
Nav1.8-IN-10 is a selective inhibitor of the Nav1.8 ion channel. At a concentration of 4 nM, it achieves an impressive blocking rate of 79.4%, demonstrating its potency. This compound is primarily utilized in the research of pain disorders, facilitating investigations into the modulation of pain pathways and potential therapeutic interventions. -
Nav1.8 Inhibitor
Nav1.8-IN-5 is a selective inhibitor of the voltage-gated sodium channel Nav1.8. It demonstrates potent biological activity against Nav1.8-mediated pain and pain-related disorders, making it a valuable tool for research in these areas. Additionally, Nav1.8-IN-5 can facilitate studies related to cardiovascular diseases, including conditions such as atrial fibrillation, by modulating sodium channel activity. -
Sodium Channel Inhibitor
R 59494 is a sodium channel inhibitor that effectively blocks Na+ and Ca2+ uptake triggered by veratridine exposure. This compound exhibits significant anti-ischemic properties, making it valuable for research in cardiovascular and neuroprotective studies. Its ability to modulate ion channel activity positions R 59494 as a useful tool for investigating the mechanisms of ischemia-related cellular damage. -
Nav1.7 Blocker
NAV 26 is a selective blocker of the voltage-gated sodium channel Nav1.7, exhibiting an IC50 of 0.37 μM. This compound is valuable for investigating pain mechanisms and developing novel analgesics. Its specificity for Nav1.7 makes it a crucial tool in researching pain pathways and potential therapeutic interventions. -
NaV1.8 Channel Inhibitor
Analgesic agent-2 is a selective NaV1.8 channel inhibitor, exhibiting a reported IC50 of 50.18 nM in HEK293 cells expressing the human NaV1.8 channel. It demonstrates significant analgesic activity, making it a valuable tool for pain research. This compound is ideal for studies investigating the role of NaV1.8 in nociception and the development of novel analgesic therapies. -
Nav1.8 Inhibitor
Nav1.8-IN-15 is a potent inhibitor of the voltage-gated sodium channel Nav1.8. It demonstrates significant analgesic effects and is relevant for research exploring pathways involved in chronic pain management. This compound can facilitate the study of Nav1.8's role in pain signaling and aid in the development of novel therapeutic strategies for pain relief. -
NaV1.7 Antagonist
AMG8380 is a selective antagonist of the voltage-gated sodium channel NaV1.7, exhibiting IC50 values of 0.907 µM and 0.387 µM in human and mouse tissues, respectively. This compound effectively inhibits Tetrodotoxin (TTX)-sensitive native channels with an IC50 of 2560 nM, making it a valuable tool for research on pain pathways and sodium channel function. Its properties allow for exploration of NaV1.7's role in nociception and related applications in pharmacological studies. -
NaV1.7 Inhibitor
Sodium Channel-IN-7 is a selective inhibitor of the NaV1.7 voltage-gated sodium channel. It interacts with the voltage-sensor domain 4 (VSD4) binding pocket of NaV1.7, demonstrating limited interaction with residue Try1537. This compound is primarily utilized in research focused on pain mechanisms and pain-related disorders. -
Sodium Channel Inhibitor
Cofirasersen is a sodium channel inhibitor that targets the epithelial sodium channel (ENaC). It is specifically developed to downregulate ENaC expression in the lungs, where hyperactivity of ENaC is implicated in cystic fibrosis, a disorder linked to mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) gene. This compound has potential applications in research related to cystic fibrosis and the modulation of sodium transport in pulmonary tissues. -
Nav1.7 Antagonist
Nav1.7-IN-15 is a potent state-dependent antagonist of the sodium channel Nav1.7, exhibiting an IC50 of 0.42 μM for human Nav1.7 PX. This compound is valuable for studying pain mechanisms and is useful in research focusing on neuropathic pain and other conditions associated with Nav1.7 activity. Its ability to selectively inhibit Nav1.7 makes it an important tool for investigating the therapeutic potential of sodium channel modulation. -
NaV1.7 Inhibitor
PF-06456384 is a potent and selective inhibitor of NaV1.7, exhibiting an IC50 of 0.01 nM. This compound is primarily utilized in research involving pain mechanisms, particularly in formalin pain model studies, to elucidate the role of NaV1.7 in nociceptive signaling. Its high selectivity makes it an important reagent for exploring therapeutic strategies targeting chronic pain conditions. -
Sodium Channel Inhibitor
Nav1.8-IN-1 is a selective inhibitor of the Na(v)1.8 sodium channel, demonstrating significant potency in blocking its activity. This compound is particularly relevant for research focused on inflammatory and neuropathic pain pathways, providing valuable insights into pain mechanisms and potential therapeutic strategies. Its ability to modulate sodium channel function makes it a promising tool for understanding pain-related conditions.
