Membrane Transporters-Ion Channels

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  1. TRPA1 agonist

    JT010 is a potent agonist of TRPA1 with an EC50 of 0.65 nM.
  2. CatSper channels blocker

    HC-056456 is an effective but not perfectly-selective blocker of CatSper channels. The [Na+]i rise is slowed by HC-056456 (IC50~3 ?M).
  3. calcium channel blocker

    ACT-709478 is a potent, selective, orally active, and brain penetrating T-type calcium channel blocker. ACT-709478 is used in the research of generalized epilepsies.
  4. Benzocaine is the ethyl ester of p-aminobenzoic acid (PABA), it is a local anesthetic commonly used as a topical pain reliever or in cough drops.
  5. Calcium channel blocker

    Berbamine is a calcium channel blocker.
  6. Ca 2+ /Mg 2+ -ATPase inhibitor

    Glucagon (19-29) (human) is a potent Ca 2+ /Mg 2+ -ATPase inhibitor.
  7. Calcium channel blocker

    (S)-Amlodipine is a (S)-Enantiomer of Amlodipine and a dihydropyridine calcium channel blocker with activity resides mainly in the (-)-isomer.
  8. 20-HETE is a potent vasoconstrictor produced in vascular smooth muscle (VSM) cells.
  9. serotonin reuptake inhibitor

    Azaphen is a potent inhibitor of the reuptake of serotonin.
  10. Glycine reuptake inhibitor

    RG1678 (Bitopertin) is a potent and noncompetitive glycine reuptake inhibitor (GlyT1).
  11. Glycine reuptake inhibitor

    RG1678 (Bitopertin) is a potent and noncompetitive glycine reuptake inhibitor (GlyT1).
  12. Calcium-Sensing Receptor Antagonist

    Calcium-Sensing Receptor Antagonists I is an antagonist of calcium-sensing parathyroid hormone receptors.
  13. P-gp inhibitor

    Elacridar hydrochloride is a P-glycoprotein inhibitor, and has been used both in vitro and in vivo as a tool inhibitor of P-glycoprotein (Pgp) to investigate the role of transporters in the disposition of various test molecules.
  14. Proton pump inhibitor

    Esomeprazole Magnesium trihydrate is a proton pump inhibitor which reduces acid secretion through inhibition of the H+ / K+ ATPase in gastric parietal cells.
  15. Cardiac Na+ channel blocker

    Flecainide is a class 1C antiarrhythmic drug especially used for the management of supraventricular arrhythmia; works by blocking the Nav1.5 sodium channel in the heart, causing prolongation of the cardiac action potential.
  16. Na+,K+-ATPase inhibitor

    Istaroxime (PST2744) is a potent inhibitor of Na+,K+-ATPase with IC50 of 0.11 μM.
  17. CFTR potentiator

    Ivacaftor benzenesulfonate is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment.
  18. CFTR potentiator

    Ivacaftor hydrate is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment.
  19. M2 ion channel blocker is capable of inhibiting and blocking the activity of M2 ion channel. Antiviral agents.
  20. Calcium channel blocker

    NNC 55-0396, Mibefradil derivative, is a highly selective T-type calcium channel blocker; displays IC50 values of 6.8 and > 100 μM for inhibition of Cav3.1 T-type channels and HVA currents respectively in INS-1 cells.
  21. N-type calcium channel blocker

    NP118809 is a potent N-type calcium channel blockers(IC50= 0.11 uM) ; good selectivity over L-type calcium channels.
  22. NBC inhibitor

    S0859, an N-cyanosulphonamide compound, reversibly inhibit NBC-mediated pH(i) recovery (K (i)=1.7 microM, full inhibition at approximately 30 microM).
  23. Sodium Channel inhibitor

    Sodium Channel inhibitor 1, one of 3-Oxoisoindoline-1-carboxamides, is a novel and selective voltage-gated sodium channel for pain treatment.
  24. AMPA antagonist

    Tezampanel is an antagonist at the AMPA and kainate families of ionotropic glutamate receptors, with selectivity for the GluR5 subtype of the kainate receptor.
  25. P-gp inhibitor

    Zosuquidar is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM.
  26. Potassium channel blocker

    Cesium chloride is a potassium channel blocker; inhibits the pacemaker current (If) and the hyperpolarization-activated cationic current (Ih). Prevents activation of caspase-3 and neuronal apoptosis in serum- and potassium-deprived cerebellar granule neurons by inactivating GSK-3β.
  27. Slows neuronal Na+ channel inactivation

    beta-Pompilidotoxin is a peptide with the sequence H2N-Arg.
  28. glutamate receptors agonist

    (S)-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA).
  29. Na+-glucose transporter inhibitor

    T-1095 is a potent and selective inhibitor of Na+-glucose cotransporters (SGLTs).
  30. elastogenesis inhibitor

    L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor.
  31. CaCCs Inhibitor

    CaCCinh-A01 inhibits CaCC currents in human bronchial and intestinal cells. Also inhibits TMEM16A channels (IC50 = 2.1 uM, in TMEM16A-expressing FRT cells).
  32. TMEM16A Inhibitor

    T16Ainh-A01 is a selective TMEM16A calcium-activated chloride channel inhibitor that strongly inhibits chloride current in salivary gland cells.
  33. ATPase and GTPase inhibitor

    Etidronate Disodium is a bisphosphonate bone resorption inhibitor.
  34. hERG1 potassium channel activator

    KB130015 is a novel activator of hERG1 potassium channels, blocking native and recombinant hERG1 channels at high voltages, but activating them at low voltages.
  35. AMPA antagonist

    YM90K hydrochloride is a selective AMPA receptor antagonist that delays neuronal death in a global ischemia model and cerebral infarction in a focal ischemia model following postischemic administration.
  36. Linoleylethanolamide is an endocannabinoid that also binds to TRPV1 (Ki = 5.60 uM).
  37. TRPA1 activatior/TRPM8 blocker

    Cannabichromene is a major non-psychotropic phytocannabinoid that inhibits endocannabinoid inactivation and activates the transient receptor potential ankyrin-1 (TRPA1). Both endocannabinoids and TRPA1 may modulate gastrointestinal motility.
  38. TRPV1 modulator

    MRS1477 is a TRPV1 positive allosteric modulator.
  39. KV7.2/7.3 activator

    ICA-110381 is a KV7.2/7.3 activator with EC50 of 0.38 uM.
  40. AMPA/kainate receptor antagonist

    Talampanel is a non-competitive antagonist of AMPA-receptor.
  41. TRPC4/C5 inhibitor

    ML204 is a novel potent antagonist that selectively modulates native TRPC4/C5 ion channels.
  42. (-)-Menthol is a key component of peppermint oil that binds and activates transient receptor potential melastatin 8 (TRPM8), a Ca2+-permeable nonselective cation channel, to increase [Ca2+]i. Antitumor activity.
  43. 5-HT3 receptor inhibitor

    Eucalyptol is a bicyclic monoterpene that has been found in Eucalyptus and other plants. It is an inhibitor of 5-HT3 receptor ,potassium channel, TNF-α and IL-1β.
  44. 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.
  45. 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.
  46. 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.
  47. 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.
  48. 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.
  49. 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.
  50. 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.

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