Membrane Transporters-Ion Channels

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  1. P-gp modulator

    Biricodar dicitrate (VX-710 dicitrate) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.
  2. SGLT2 inhibitor

    Ipragliflozin is a highly potent and selective SGLT2 inhibitor with IC50 of 2.8 nM; little and NO potency for SGLT1/3/4/5/6.
  3. TRPM8 and TRPA1 activator

    Icilin is a cooling agent that activates the novel cold receptors TRPM8 (CMR1) and TRPA1 (ANKTM1/TRPN1), members of the TRP ion channel family. Induces currents in CMR1-expressing HEK 293 cells (EC50 = 0.36 μM)
  4. VMAT2 inhibitor

    GZ-793A is a selective inhibitor of vesicular monoamine transporter 2 (VMAT2), which transports the monoamine neurotransmitters from cellular cytosol into synaptic vesicles.
  5. ACA is a channel blocker that acts on several transient receptor potential (TRP) channels, including TRPM2, TRPM8, and TRPC6 (IC50 = 1.7, 3.8, and 2.3 uM, respectively).
  6. voltage-gated sodium channel Nav1.7 inhibitor

    Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC50 of 8 nM. Pain relief. Limited CNS penetration.
  7. AMPA desensitization inhibitor

    Cyclothiazide is a benzothiadiazide that acts as a potentiator of AMPA receptors, positively modulating its response to glutamic acid (EC50 = 3.8 M).
  8. CRAC intermediate 2 is a intermediate compound for CRAC inhibitor synthesis, extracted from patent WO 2013059666A1.
  9. Sodium channel Blocker

    QX 314 chloride is a membrane impermeable quaternary derivative of lidocaine, a voltage-activated Na+ channel blocker
  10. NaV1.3 and NaV1.1 channels inhibitor

    ICA-121431 is a potent and selective inhibitor of human NaV1.3 and NaV1.1 channels (IC50 values are 13 and 23 nM respectively).
  11. AMPA receptor modulator

    Farampator has been investigated for its effect on AMPA receptors and researched for potential use in the treatment of schizophrenia and Alzheimer's Disease. It was found to improve short-term memory, but impaired episodic memory.
  12. hASBT inhibitor

    GSK2330672 is a highly potent, nonabsorbable apical sodium-dependent bile acid transporter inhibitor.
  13. NMDA receptor antagonist

    DNQX is a non-N-methyl-D-aspartate (non-NMDA) receptor complex antagonist.
  14. Sodium channel blocker

    Encainide HCl is a sodium channel blocker and class Ic antiarrhythmic. Encainide is a non-chiral antiarrhythmic and benzanilide derivative.
  15. Na+/K+ ATPase inhibitor

    Melittin is a Na+/K+ ATPase inhibitor. It inhibits Gs and stimulates Gi activity. It inhibits protein kinase C and cAMP-dependent protein kinases.
  16. Ca2+ release inhibitor

    Dantrolene sodium is a muscle relaxant that acts by abolishing excitation-contraction coupling in muscle cells, probably by action on the ryanodine receptor.
  17. sodium channel protein inhibitor

    Oxcarbazepine is a sodium channel protein inhibitor.
  18. KCa2.1 channels activator

    GW 542573X is an activator of small-conductance Ca2+-activated K+ channels (KCa2).
  19. P-glycoprotein inhibitor

    XR9576 is a P-glycoprotein inhibitor undergoing research as an adjuvant against multidrug resistance in cancer
  20. SGLT2 inhibitor

    Remogliflozin inhibits the sodium-glucose transport (SGLT2) proteins, which are responsible for glucose reabsorption in the kidney.
  21. Selective calcium chelator

    BAPTA tetrapotassium is a selective calcium chelator with greater affinity for Ca2+ than Mg2+.
  22. TrpA1 channel agonist

    PF-4840154 is a non-electrophilic reference agonist of the TrpA1 channel. The TRPA1 channel is considered an attractive pain target based on the fact that TRPA1 knockout mice showed near complete attenuation of pain behaviors in some pre-clinical development models.
  23. ATP synthase inhibitor

    Oligomycin is a macrolide that acts as a specific inhibitor of the mitochondrial ATP-synthase and blocks oxidative phosphorylation.
  24. SERCA inhibitor

    Cyclopiazonic acid is an inhibitor of SERCA (endoplasmic reticulum Ca2+-ATPase) which induces the release of intracellular stored Ca2+, without increasing IP3 levels.
  25. AMPA Receptor Blocker

    IEM 1754 Dihydrobromide is a voltage-dependent open-channel blocker of AMPA receptors.
  26. H3R antagonist/TRPV1 antagonist

    ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist and a transient receptor potential vanilloid type 1 (TRPV1) antagonist.
  27. Potassium Channel inhibitor

    Repaglinide is a potent short-acting insulin secretagogue that acts by closing ATP-sensitive potassium (KATP) channels in the plasma membrane of the pancreatic beta cell.
  28. Riluzole preferentially blocks TTX-sensitive sodium channels, which are associated with damaged neurons.This reduces influx of calcium ions and indirectly prevents stimulation of glutamate receptors.
  29. protein tyrosine phosphatases inhibitor

    Sodium orthovanadate is the chemical compound Na3VO4. It is an inhibitor of protein tyrosine phosphatases, alkaline phosphatases and a number of ATPases, most likely acting as a phosphate analogue.
  30. Calcium Channel inhibitor

    Tetrandrine is a calcium channel blocker. It inhibits the degranulation of mast cells.Tetrandrine has anti-inflammatory and anti-fibrogenic actions, which make tetrandrine and related compounds potentially useful in the treatment of lung silicosis, liver cirrhosis, and rheumatoid arthritis.
  31. SGLT2 inhibitor

    PF-04971729 is a potent and selective inhibitor of the sodium-dependent glucose cotransporter 2.
  32. TrxR1/CRM1 inhibitor

    Piperlongumine selectively kills cancer cells regardless of p53 status without harming normal cells. It binds to and inihbits proteins known to regulate oxidative stress, in particular, Glutathione S-transferase pi 1 (GSTP1).
  33. TRPA1 channel blocker

    TCS 5861528 is a TRPA1 channel blocker and an antagonizer of AITC- and 4-HNE-evoked calcium influx.
  34. Na(+)/H(+) exchange inhibitor

    ENIPORIDE is a potent Na+/H+ exchange inhibitor.
  35. TRPV4 blocker

    GSK2193874 was identified as a selective, orally active TRPV4 blocker that inhibits Ca(2+) influx through recombinant TRPV4 channels and native endothelial TRPV4 currents.
  36. Sodium channel blocker/DNMT inhibitor

    Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor.
  37. Chloroprocaine HCl is a local anesthetic during surgical procedures.
  38. proton pump inhibitor

    Tenatoprazole is a prodrug of the proton pump inhibitor (PPI) class, which inhibits proton transport with IC50 of 3.2 uM.
  39. F1 Fo-ATPase inhibitor

    BTB06584 is an IF1-dependent, selective inhibitor of the mitochondrial F1 Fo-ATPase.
  40. MCT1 inhibitor

    AR-C117977 is a potent MCT1 inhibitor, which can reduce vimmune responses both in vitro and in vivo, maintains long-term graft survival, and induces operational tolerance.
  41. late INa Inhibitor

    GS967 is a novel, potent, and selective inhibitor of cardiac late sodium current(late INa); inhibits ATX-II-induced late I(Na) in ventricular myocytes and isolated hearts with IC(50) values of 0.13 and 0.21 uM, respectively.
  42. P-Glycoprotein Inhibitor

    (R)-Verapamil hydrochloride is an orally active P-Glycoprotein inhibitor that effectively blocks MRP1-mediated transport. This compound induces apoptosis and inhibits L-type calcium channels, including BZPcc, DHPcc, and PLLcc. Additionally, (R)-Verapamil hydrochloride demonstrates potential anti-septic shock and anti-diabetic effects, making it suitable for a range of research applications in cellular signaling and drug transport studies.
  43. Nucleotide Analogue

    Uridine 5'-monophosphate disodium salt is a nucleotide analogue that activates mitochondrial ATP-dependent potassium channels, providing cardioprotective effects. This compound facilitates the synthesis of CDP-choline and induces apoptosis in intestinal epithelial cells, supporting gut development and reducing the incidence of diarrhea. It serves as a valuable tool for studies related to cardiac health and gastrointestinal function.
  44. NF-κB Expression Reducer, ERK 1/2 Activator, Beta-Adrenergic Receptor Modulator, Calcium Channel Inhibitor

    Eupatorin is a flavonoid that functions primarily as an NF-κB expression reducer and an ERK 1/2 activator, while also modulating beta-adrenergic receptors and inhibiting calcium channels. It demonstrates significant antiproliferative and vasodilatory effects, inducing apoptosis and causing G2/M phase cell cycle arrest, alongside reactive oxygen species (ROS) production. Eupatorin has been shown to impact inflammatory mediators and calcium signaling pathways, making it relevant for research in breast cancer, hypertension, and leukemia. Metabolized by CYP1A1 and other CYP1 enzymes, Eupatorin yields bioactive metabolites that maintain antiproliferative properties.
  45. Calcium Channel Modulator

    4-Bromo A23187 is a halogenated analog of the selective calcium ionophore A-23187, acting as a calcium channel modulator. This compound facilitates the transport of calcium ions across cellular membranes, leading to increased intracellular calcium levels. It has demonstrated efficacy in inducing apoptosis in various cell types, including HL-60 cells, and is useful for research applications related to calcium-mediated signaling pathways and cell death mechanisms.
  46. PP Inhibitor

    Pantoprazole sodium hydrate is a potent proton pump inhibitor (PPI) that targets the H+/K+-ATPase enzyme. With an IC50 value of 6.8 μM, it exhibits significant anti-secretory and anti-ulcer properties. This compound has been demonstrated to enhance tumor growth delay when used in combination with Doxorubicin, making it a valuable reagent for studies involving cancer treatment and gastrointestinal disorders.
  47. Calcium Sensitiser

    OR-1896 is a potent calcium sensitizer and active metabolite of Levosimendan, primarily targeting phosphodiesterase (PDE) III isoforms. It exhibits significant vasodilatory effects and can activate ATP-sensitive potassium channels, enhancing calcium sensitivity. OR-1896 has been shown to reduce cardiomyocyte apoptosis, alleviate cardiac remodeling, and mitigate myocardial inflammation, making it valuable for research in cardiovascular disease therapies.
  48. F0F1-ATPase Inhibitor

    Apoptolidin is a polyketide compound that selectively inhibits the mitochondrial F0F1-ATPase. It has been demonstrated to induce apoptotic cell death specifically in cells transformed with adenovirus type 12 oncogenes, such as ElA, with an IC50 of 10-17 ng/ml. Apoptolidin serves as a valuable tool for studying apoptotic mechanisms and mitochondrial function in cancer research.
  49. Kv2.1 Inhibitor

    Kv2.1-IN-1 is a selective inhibitor of the Kv2.1 potassium channel, demonstrating a potent inhibitory activity with an IC50 of 0.07 μM. It exhibits over 130-fold selectivity against other potassium, sodium, and calcium channels. Kv2.1-IN-1 has been shown to reduce H2O2-induced apoptosis in HEK293 cells and provides significant neuroprotective effects in models of middle cerebral artery occlusion (MCAO) in rats. This compound is useful for research into ischemic stroke and related neurological conditions.
  50. Potassium Binder

    Patiromer is a selective, non-absorbable intestinal potassium binder that targets potassium ions through a reversible exchange with calcium ions. It effectively lowers serum potassium levels while promoting fecal potassium excretion and reducing serum aldosterone levels. Patiromer is utilized in research on hyperkalemia associated with conditions such as chronic kidney disease, diabetes, and heart failure, and is particularly beneficial in studies aimed at enhancing the efficacy of renin-angiotensin-aldosterone system inhibitor (RAASi) therapies.

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