Shop By
Catalog No.
Product Name
Application
Product Information
Citations
-
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. -
Ca2+‑ATPase Inhibitor
rel-(E)-6,7-Transdihydroxyligustilide is a potent inhibitor of Ca2+-ATPase, specifically in calmodulin-deficient human erythrocyte membranes. This compound, derived from the dried tuberous roots of Polygonum multiflorum, plays a significant role in the regulation of calcium homeostasis. It is particularly valuable in research related to hyperlipidemia and related metabolic disorders. -
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. -
Nav1.2 Inhibitor
Nav1.2-IN-2 is a potent inhibitor of the voltage-gated sodium channel Nav1.2, demonstrating an IC₅₀ of 0.18 μM for channel inactivation. It effectively reduces both the amplitude and frequency of spontaneous synchronous calcium oscillations with IC₅₀ values of 0.38 μM and 0.88 μM, respectively. Additionally, Nav1.2-IN-2 inhibits calcium influx triggered by Veratridine with an IC₅₀ of 1.89 μM. This reagent is relevant for research into neurological disorders such as epilepsy. -
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. -
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. -
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 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. -
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. -
P-gp Inhibitor
P-gp-IN-30 is a potent inhibitor of P-glycoprotein (P-gp) that acts by targeting Y-box binding protein 1 (YB-1). This compound enhances the sensitivity of cancer cells to Paclitaxel by decreasing both total and nuclear YB-1 protein levels, leading to the inhibition of P-gp expression and function, and consequently reducing the efflux of Paclitaxel. P-gp-IN-30 has demonstrated significant tumor growth inhibition in A549/Taxol xenograft mouse models and is applicable in research focused on non-small cell lung cancer (NSCLC). -
P-Glycoprotein Inhibitor
Reversin 205 is a selective inhibitor of P-glycoprotein (ABCB1), a crucial protein involved in drug transport and multidrug resistance. This compound serves as a peptide chemosensitizer, enhancing the efficacy of various chemotherapeutic agents by mitigating the efflux of drugs from cancer cells. Reversin 205 is applicable in research focused on overcoming drug resistance in cancer therapy and optimizing chemotherapy outcomes. -
P-glycoprotein Inhibitor
P-gp-IN-35 is a potent P-glycoprotein (P-gp) inhibitor, specifically designed to enhance the efficacy of chemotherapeutic agents. It demonstrates significant cytotoxic effects against breast and colorectal cancer cells, particularly in cases where P-gp is overexpressed, thus reversing multidrug resistance. This compound serves as a valuable tool in research focused on overcoming drug resistance in breast and colon cancers. -
P-glycoprotein Inhibitor
P-gp Inhibitor 5 is a selective inhibitor of P-glycoprotein (P-gp), a key player in multidrug resistance (MDR) in cancer. It exhibits notable antiproliferative activity against various cancer cell lines, effectively reinstating sensitivity to chemotherapeutic agents such as Vincristine and Paclitaxel in ABCB1/Flp-InTM-293 and KBvin cells. This property makes P-gp Inhibitor 5 a valuable tool for research aimed at overcoming drug resistance in cancer therapies. -
P-glycoprotein Inhibitor
KR30031 is a potent inhibitor of P-glycoprotein (P-gp), facilitating increased efficacy of anticancer drugs by overcoming multidrug resistance (MDR) pathways. This orally active compound is designed to enhance cytotoxic effects while minimizing cardiovascular side effects commonly associated with other P-gp inhibitors. KR30031 is valuable for research applications focused on understanding and reversing MDR in cancer therapeutic contexts. -
P-gp Inhibitor
P-gb-IN-1 is a potent P-glycoprotein (P-gp) inhibitor that effectively reverses P-gp-mediated drug efflux. This 2,5-disubstituted furan derivative demonstrates significant affinity for P-gp through hydrogen bonding interactions with Asn 721 and Met 986. Its broad-spectrum reversal activity, coupled with low toxicity in MCF-7/ADR cell lines, makes P-gb-IN-1 a valuable tool for enhancing the efficacy of chemotherapeutic agents in research applications. -
P-glycoprotein Inhibitor
FM04 is a potent inhibitor of P-glycoprotein (P-gp) with an EC50 of 83 nM. It operates through two primary mechanisms: firstly, by binding to Q1193 and interacting with critical residues H1195 and T1226, and secondly, by engaging I1115, disrupting essential interactions within the R262-Q1081-Q1118 pocket, and uncoupling the ICL2-NBD2 interaction. FM04 is valuable for research exploring drug transport mechanisms and multidrug resistance in cancer therapies. -
P-gp Inhibitor
P-gp inhibitor 3 is a potent inhibitor of P-glycoprotein (P-gp), primarily targeting its ATPase activity to inhibit the efflux function. This compound demonstrates significant multidrug resistance (MDR) reversal capabilities, effectively enhancing the cytotoxic effects of antitumor agents such as Paclitaxel. P-gp inhibitor 3 is valuable in cancer research, particularly for studies focused on overcoming drug resistance in chemotherapy. -
P-gp Inhibitor
P-gp inhibitor 29 is a potent inhibitor of P-glycoprotein (P-gp) with an IC50 of 8.9 nM in Eca109/VCR cells. This compound not only inhibits P-gp activity but also induces apoptosis, making it a valuable tool in the study of drug resistance mechanisms in esophageal cancer. Its efficacy in modulating P-gp can facilitate research aimed at improving therapeutic strategies for this malignancy. -
P-gp Inhibitor
P-gp-IN-32 is a potent P-glycoprotein (P-gp) inhibitor that demonstrates significant ability to reverse multidrug resistance (MDR) in cancer cells. It exhibits low cytotoxicity with an IC50 of 0.11 μM and a reversal fold of 215.9 against Doxorubicin in MCF7/ADR cells. P-gp-IN-32 binds directly to P-gp, inducing conformational changes that inhibit its efflux function, making it a valuable tool for cancer research, particularly in studies focused on breast cancer. -
P-gp Inhibitor
P-gp Inhibitor 2 is a potent inhibitor of P-glycoprotein (P-gp), a critical transporter implicated in multidrug resistance. This compound effectively reverses Doxorubicin resistance with an IC50 of 0.22 µM in P-gp overexpressing human colorectal carcinoma SW600 Ad300 cells. Its application in cancer research highlights its potential as a valuable tool for overcoming P-gp-mediated drug efflux in therapeutic strategies. -
Pgp Inhibitor
P-gp inhibitor 15 is a nonsubstrate inhibitor targeting P-glycoprotein (P-gp), primarily acting to inhibit P-gp-ATPase activity. This compound effectively disrupts the P-gp-mediated efflux of Rhodamine123, leading to increased intracellular accumulation of chemotherapeutic agents. P-gp inhibitor 15 has demonstrated the ability to enhance the efficacy of Paclitaxel and shows potential in inhibiting tumor progression in xenograft models, specifically in nude mice with KBV tumors. -
P-glycoprotein Inhibitor
Dofequidar sesquifumarate is an orally active quinoline compound that functions as an inhibitor of P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). It exhibits a potent ability to reverse multidrug resistance in tumor cells by competitively inhibiting ABCB1/P-gp and ABCC1/MRP-1. This inhibition effectively blocks the efflux of chemotherapeutic agents, resulting in increased drug accumulation within cancer cells and enhanced chemotherapeutic efficacy. Dofequidar sesquifumarate is valuable for research applications aimed at overcoming drug resistance in cancer treatment. -
P-glycoprotein Inhibitor
(S)-Tenacissoside F is a polyoxypregnane compound that functions as a P-glycoprotein inhibitor. By effectively inhibiting the drug efflux activity of P-glycoprotein (P-gp/ABCB1), (S)-Tenacissoside F is capable of reversing multidrug resistance, making it a valuable compound in cancer research, particularly in the study of colon cancer. Its mechanism may provide insights into novel therapeutic approaches for overcoming drug resistance in tumors.
