Membrane Transporters-Ion Channels

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  1. Kir2 family channels inhibitor

    ML133 hydrochloride is a selective Kir2 family channels inhibitor, with an IC50 of 1.8 μM at pH 7.4 and 290 nM at pH 8.5.
  2. calcium channel blocker

    Nicardipine hydrochloride (YC-93) is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels.
  3. GlyT inhibitor/NMDA receptor

    Sarcosine is a glycine transporter type 1 (GlyT) inhibitor and an N-methyl-D-aspartate (NMDA) receptor co-agonist at the glycine binding site.
  4. TRP Channel blocker

    SKF-96365 hydrochloride is a non-selective TRP Channel blocker.
  5. elastogenesis inhibitor

    L-Ascorbic acid sodium salt (Sodium L-ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid sodium salt inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid sodium salt is also a collagen deposition enhancer and an elastogenesis inhibitor.
  6. SGLT2 inhibitor

    Canagliflozin hemihydrate is the hemihydrate form of canagliflozin, which is a SGLT2 inhibitor with IC50 of 2.2 nM for hSGLT2 in a cell-free assay, exhibits 413-fold selectivity over hSGLT1.
  7. Na+/Ca2+ exchange Inhibitor

    CGP 37157 is a benzothiazepine that acts as a selective inhibitor of the mitochondrial sodium-calcium exchanger (IC50 = 0.36 μM in isolated mitochondria).
  8. CRAC channel inhibitor

    GSK-7975A is a potent and orally available CRAC channel inhibitor.
  9. plasmodium ATP4 inhibitor

    (+)-SJ733 is an inhibitor of plasmodium ATP4, leading to rapid clearance in vivo by inducing physical changes in infected, treated red cells.
  10. Coelenterazine h is a derivative of Coelenterazine. Coelenterazine h is more sensitive to Ca2+ than is the native complex, thus providing a valuable tool for measuring small changes in Ca2+ concentrations.
  11. SERCA2 allosteric activator

    CDN1163 is a SERCA2 allosteric activator. It increases Ca2+-ATPase activity and Ca2+ uptake by ER microsomes from obese mice. Rescues HEK cells from ER stress-induced cell death.
  12. TREK-1/2 Activator

    ML335 is a potent and selective TREK-1/2 Activator. ML335 is an agonist for OPRM1-OPRD1 heterdimerization with an EC50 of 403 nM, and selectivities vs. OPRM1, OPRD1, and HTR5A of 37, 2.7, and >99, respectively.
  13. chloride channel blocker

    NPPB is a chloride channel blocker (IC50 = 80 nM) that has also been identified as a GPR35 agonist.
  14. Antimalarial

    Quinine is a primary alkaloid of various species of Cinchona, optical isomer of Quinidine and an anti-malarial, skeletal, muscle relaxant.
  15. TRPA1 Antagonist

    AM-0902 is a potent and selective Transient Receptor Potential A1 (TRPA1) Antagonist.
  16. AMPA antagonist

    GYKI53655 Hydrochloride is a non-competitive AMPA and kainate receptor antagonist. CAS: 143692-18-6 (Free Base); 143692-48-2 (HCl).
  17. TRPM8 Agonist

    WS-12 is a potent TRPM8 agonist that acts as a cooling agent (EC50 = 193 nM).
  18. TRPM8 agonist

    WS 3 is TRPM8 receptors agonist (EC50 = 3.7 μM) and cooling agent.
  19. Pgp1 inhibitor

    NSC 23925 is a plasma membrane glycoprotein 1 (Pgp1) inhibitor to reverse multidrug resistance (MDR1).
  20. NHE-1 inhibitor

    Rimeporide (EMD-87580) is a potent and selective inhibitor of the Na+/H+ exchanger (NHE-1).
  21. potassium channel activator

    SKA-31 is an activator of KCa2 and KCa3.1 calcium-activated potassium channels.
  22. BCRP/ABCG2 inhibitor

    YHO-13177 is a potent and specific inhibitor of breast cancer resistance protein (BCRP/ABCG2).
  23. TRPM8 Antagonist

    AMG-333 is a potent and selective TRPM8 Antagonist.
  24. exportin-1 inhibitor

    Eltanexor, also known as KPT-8602, is a second-generation exportin-1 inhibitor.
  25. TRPC6 inhibitor

    SAR7334 is a novel, highly potent and bioavailable inhibitor of TRPC6 channels that opens new opportunities for the investigation of TRPC channel function in vivo. SAR7334 inhibited TRPC6, TRPC3 and TRPC7-mediated Ca(2+) influx into cells with IC50 s of 9.5, 282 and 226 nM, whereas TRPC4 and TRPC5-mediated Ca(2+) entry was not affected.
  26. proton pump inhibitor

    Ilaprazole (IY-81149) is a proton pump inhibitor; inhibits H+/K+-ATPase with an IC50 of 6.0 μM.
  27. Nonivamide is a capsaicin analogue that exhibits anti-inflammatory properties in peripheral blood mononuclear cells and U-937 macrophages. Nonivamide is a agonist, which exhibits 4d-EC50 value of 5.1 mg/L in static toxicity tests.
  28. Meticrane is a diuretic. Meticrane inhibits the reabsorption of sodium and chloride ions in the distal convoluted tubule. Meticrane is used to treat essential hypertension.
  29. Potassium Channel activator

    Pinacidil monohydrate, an antihypertensive drug, is a potassium channel activator.
  30. Chloride Channel/GABA Receptor blocker

    Picrotoxinin negatively modulate the action of GABA on GABAA receptors.
  31. H(+)-K(+)-exchanging ATPase inhibitor

    Rabeprazole is an inhibitor of H(+)-K(+)-exchanging atpase in gastric parietal cells.
  32. Calcium channel blocker

    Efonidipine is a dihydropyridine calcium channel blocker that blocks both T-type and L-type calcium channels. It has also been studied in atherosclerosis and acute renal failure.
  33. Potassium channel blocker

    Dalfampridine is a potassium channel blocker used to help multiple sclerosis patients walk.
  34. serotonin uptake inhibitor

    Paroxetine Mesylate is a serotonin uptake inhibitor that is effective in the treatment of depression.
  35. TRPM4 blocker

    Selective TRPM4 blocker (IC50 = 20 μM in HEK293 cells). Exhibits no effect on CFTR or TRPM5 (at 0.25 and 1 mM respectively). Abolishes arrhythmias induced by hypoxia in a mouse heart model.
  36. Calcium channel blockers

    Nicardipine(YC-93) is a calcium channel blocker that has been widely used to control blood pressure in severe hypertension following events such as ischemic stroke, traumatic brain injury, and intracerebral hemorrhage.
  37. Na/K ATPase partial agonist

    Canrenone is a metabolite of spironolactone, Na/K ATPase partial agonist and aldosterone and androgen receptor antagonist used as a diuretic.
  38. Calcium channel blocker

    Fendiline hydrochloride is a nonselective calcium channel blocker.
  39. Fipronil is a broad-spectrum insecticide that belongs to the phenylpyrazole chemical family. Fipronil disrupts the insect central nervous system by blocking GABA-gated chloride channels and glutamate-gated chloride (GluCl) channels.
  40. Calcium channel proteins inhibitor

    Dantrolene sodium is a inhibitor of calcium channel proteins, inhibiting the release of Ca2+ from the sarcoplasm. Dantrolene sodium is a skeletal muscle relaxant which acts by blocking muscle contraction beyond the neuromuscular junction.
  41. SChE inhibitor

    Dibucaine (USAN) is an amide local anesthetic. Dibucaine reversibly binds to and inactivates sodium channels in the neuronal cell membrane. Inhibition of sodium channels prevents the depolarization of nerve cell membranes and inhibits subsequent propagation of impulses along the course of the nerve, thereby limiting the excitation of nerve endings. This results in loss of sensation.
  42. SGLT2 inhibitor

    Dapagliflozin ((2S)-1,2-propanediol, hydrate), a new type of drug used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine.
  43. Trimethadione is an oxazolidinedione anticonvulsant. It is most commonly used to treat epileptic conditions that are resistant to other treatments. Trimethadione (TMO) has the properties required of probe drugs for the evaluation of hepatic drug-oxidizing capacity in humans in vivo.
  44. Citronellal or rhodinal or 3,7-dimethyloct-6-en-1-al is a monoterpenoid, the main component in the mixture of terpenoid chemical compounds that give citronella oil its distinctive lemon scent.
  45. Calcium channel blocker

    Lercanidipine is a calcium channel blocker of the dihydropyridine class, which works by relaxing and opening the blood vessels allowing the blood to circulate more freely around the body. This lowers the blood pressure and allows the heart to work more efficiently.
  46. SGLT2 inhibitor

    Tofogliflozin hydrate (CSG-452 hydrate) is a potent and highly specific sodium/glucose cotransporter 2 (SGLT2) inhibitor with an IC50 of 2.9 nM and Ki values of 2.9 nM, 14.9 nM, and 6.4 nM for human, rat, and mouse SGLT2.
  47. potassium-competitive acid blocker

    Vonoprazan (TAK-438 free base) is an orally active potassium-competitive acid blocker which inhibits H+, K+-ATPase activity with an IC50 of 19 nM.
  48. Pirmenol hydrochloride inhibits IK.ACh by blocking muscarinic receptors. The IC50 of Pirmenol for inhibition of Carbachol-induced IK.ACh is 0.1 μM.
  49. calcium channel blocker

    Bepridil hydrochloride (CERM 1978) is a calcium channel blocker, with antianginal activity.
  50. Peripheral chemoreceptor agonist

    Almitrine mesylate, a peripheral chemoreceptor agonist, inhibits selectively the Ca2+-dependent K+ channel.

Items 301-350 of 2532

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