Membrane Transporters-Ion Channels

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  1. Na+ channel blocker

    Amiloride hydrochloride is a Na+ channel blocker, also inhibits TRPP3 channels and Na+/H+ exchanger (NHE).
  2. L-type calcium channel blocker

    Amlodipin is L-type calcium channel blocker that displays antihypertensive properties. It inhibits Ca2+-induced contractions in depolarized rat aorta (IC50 = 1.9 nM) and displays vasoprotective effects in cardiovascular disease.
  3. L-type calcium channel blocker

    Amlodipine-besylate is L-type calcium channel blocker that displays antihypertensive properties. It inhibits Ca2+-induced contractions in depolarized rat aorta (IC50 = 1.9 nM) and displays vasoprotective effects in cardiovascular disease.
  4. AMPA Receptor Inhibitor

    Aniracetam is an ampakine and nootropic of the racetam chemical class purported to be considerably more potent than piracetam.
  5. Artemisinin and its derivatives are a group of drugs that possess the most rapid action of all current drugs against Plasmodium falciparum malaria.
  6. SGLT2 inhibitor

    EGT1442 is a potent and selective SGLT2 inhibitor.
  7. Bupivacaine is a more potent inhibitor of cAMP production than are chemically related local anesthetics that are less prone to produce cardiovascular toxicity.
  8. Carbamazepine is an anticonvulsant and mood-stabilizing drug used primarily in the treatment of epilepsy and bipolar disorder, as well as trigeminal neuralgia.
  9. Ciclopirox is currently being investigated as an alternative treatment to ketoconazole for seborrhoeic dermatitis as it suppresses growth of the yeast Malassezia furfur.It acts by inhibiting the membrane transfer system by interrupting the Na+ K+ ATPase.
  10. Calcium channel blocker

    Cilnidipine is a dual blocker of L-type voltage-gated calcium channels in vascular smooth muscle and N-type calcium channels in sympathetic nerve terminals that supply.
  11. SGLT2 inhibitor

    Dapagliflozin inhibits subtype 2 of the sodium-glucose transport proteins (SGLT2), which is responsible for at least 90% of the glucose reabsorption in the kidney.
  12. Diethylstilbestrol is a synthetic nonsteroidal estrogen that was first synthesized in 1938. It is also classified as an endocrine disruptor.
  13. Diltiazem is a nondihydropyridine (non-DHP) member of the class of drugs known as calcium channel blockers, used in the treatment of hypertension, angina pectoris, and some types of arrhythmia.
  14. Proton pump inhibitor

    Esomeprazole sodium is a proton pump inhibitor which reduces acid secretion through inhibition of the H+ / K+ ATPase in gastric parietal cells.
  15. TRP agonist

    Evodiamine is a chemical extracted from the Tetradium family of plants. It acts primarily as a thermogenic and stimulant.
  16. Kir6.2/SUR inhibitor

    Glimepiride is a potent Kir6.2/SUR inhibitor with IC50 of 3.0 nM, 5.4 nM, and 7.3 nM for SUR1, SUR2A and SUR2B, used in the treatment of type 2 diabetes mellitus.
  17. K+ channel and CFTR Cl- channel blocker

  18. AMPA and Kainate antagonist

    GYKI-52466 dihydrochloride is selective non-competitive AMPA receptor antagonist (IC50 values are 10-20, ~ 450 and >> 50 μM for AMPA- , kainate- and NMDA-induced responses respectively).
  19. Hydralazine hydrochloride is a hydrochloride salt of hydralazine (Apresoline) that is a direct-acting smooth muscle relaxant with an IC50 of 1.9 mM.
  20. calcium channel blocker

    Isradipine is a calcium channel blocker of the dihydropyridine class.
  21. Ivermectin is a broad-spectrum antiparasitic avermectin medicine.
  22. proton pump inhibitor

    Lansoprazole(AG 1749) is a proton pump inhibitor which prevents the stomach from producing acid.
  23. Lidocaine (Alphacaine) is an anasthetic and class Ib antiarrhythmic agent. Blocks voltage-gated sodium channels in the inactivated state.
  24. P-gp modulator

    LY335979 (Zosuquidar trihydrochloride) is a potent highly selective P-gp inhibitor.
  25. Manidipine is a dihydropyridine compound and calcium channel protein inhibitor and antagonist.
  26. Manidipine 2HCl is a HCl salt form of Manidipine which is a calcium channel blocker for Ca2+ current with IC50 of 2.6 nM.
  27. Minoxidil (U-10858) is a selective ATP dependent K+ (Kir6) channel activator.
  28. Nateglinide(Starlix) is an insulin secretagog agent that lowers blood glucose levels by stimulating insulin secretion from the pancreas.
  29. Kir6 (KATP) channel opener

    Nicorandil (SG-75) is potassium channel activator.
  30. L-type calcium channel blocker.

    Nifedipine is a L-type calcium channel blocker.
  31. Calcium Channel inhibitor

    Nimodipine is a L-type Ca2+ channel blocker.
  32. calcium channel blocker

    Nisoldipine(BAY-k 5552; Sular) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC50 of 10 nM.
  33. ATPase inhibitor

    Oligomycin A is a mitochondrial ATPase inhibitor. Oligomycin A inhibits ATP5 (mitochondrial ATPases, F1F0) bound to the cell membrane.
  34. ATPase Inhibitors

    Omeprazole is a cell-permeable, selective proton pump inhibitor.
  35. CFTR Inhibitor

    Oridonin (Isodonol), an entkaurane diterpenoid isolated from Rabdosia rubescens, is an important traditional Chinese herbal remedy.
  36. Phenytoin is a sodium channel protein inhibitor.
  37. Phenytoin sodium (Dilantin) is a sodium channel protein inhibitor.
  38. SGLT1/SGLT2 inhibitor

    Phlorizin is a competitive inhibitor of SGLT1 and SGLT2; this reduces renal glucose transport, lowering the amount of glucose in the blood.
  39. CFTR inhibitor

    PTC124 also known as Ataluren is CFTR-G542X nonsense allele inhibitor.
  40. 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.
  41. 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.
  42. 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.
  43. 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.
  44. CFTR activator

    VX-770 (Ivacaftor) is known as a CFTR potentiator.
  45. CFTR modulator

    VX-809 is the second investigational oral candidate compound for the treatment of cystic fibrosis (CF).
  46. MDR1/P-gp Inhibitor

    PSC-833 is a kind of P-glycoprotein (P-gp) modulator that inhibits P-gp-mediated multidrug-resistance (MDR).
  47. SGLT2 Inhibitor

    Canagliflozin is an inhibitor of subtype 2 sodium-glucose transport protein (SGLT2).
  48. SGLT2 inhibitor

    PF-04971729 is a potent and selective inhibitor of the sodium-dependent glucose cotransporter 2.
  49. TRPV1 antagonist

    SB-705498 is a potent, selective and orally bioavailable TRPV1 antagonist.
  50. Protein translocation Inhibitor

    Brefeldin A blocks binding of ADP-ribosylation factor to the Golgi apparatus and inhibits GDP-GTP exchange.

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