Membrane Transporters-Ion Channels

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  1. SERT/NET Inhibitor

    Amitriptyline is a tricyclic antidepressant that primarily inhibits the serotonin transporter (SERT) and norepinephrine transporter (NET), enhancing synaptic levels of serotonin and norepinephrine. With a Ki value of 3.45 nM for SERT and 13.3 nM for NET, Amitriptyline demonstrates significant antidepressant activity. Additionally, it exhibits agonistic properties at α2A adrenergic and TrkA/TrkB receptors, contributing to its analgesic and neurotrophic effects. Furthermore, Amitriptyline interacts with various receptors, including muscarinic cholinergic and H1 receptors, which may lead to a variety of side effects, while its ability to block sodium channels and hERG potassium channels raises concerns regarding cardiotoxicity.
  2. V-ATPase Inhibitor

    RSC-1255 is a potent and selective inhibitor of Vacuolar H⁺-ATPase (V-ATPase), demonstrating a binding affinity with a Kd of 23 nM. This compound exhibits preferential cytotoxicity towards KRAS-mutant cancer cells, particularly those harboring KRASG13D and KRASG12V mutations. RSC-1255 effectively induces apoptosis while inhibiting lysosomal acidification, autophagy, and macropinocytosis. It serves as a valuable tool for researching KRAS-driven lung and colon cancers.
  3. ATPase Inhibitor

    ATPase-IN-3 is an ATPase inhibitor that demonstrates gastroprotective effects in models of ethanol-induced gastric ulcers. Its mechanism of action involves the modulation of anti-apoptotic pathways through the upregulation of BCL-2 and the activation of tumor suppressor protein P53. This compound is valuable for research applications aimed at investigating gastric ulcer pathophysiology and potential therapeutic interventions.
  4. Apoptosis Inducer

    Rabeprazole-d4 is a deuterated derivative of Rabeprazole, primarily acting as an apoptosis inducer through its irreversible inhibition of gastric H+/K+-ATPase. This second-generation proton pump inhibitor also functions as a uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole-d4 is valuable for research focused on gastric ulcerations and gastroesophageal reflux diseases, facilitating studies on its mechanisms of action and therapeutic potential.
  5. Calcium Antagonist

    Cycleanine is a potent vascular-selective calcium antagonist known for its analgesic, muscle relaxant, and anti-inflammatory properties. This compound exhibits potential anti-ovarian cancer effects by modulating the apoptosis pathway, making it a valuable tool for research in oncology and pain management. Its calcium-blocking mechanism allows for further exploration into vascular functions and related biological systems.
  6. MDR Reversal Agent

    Hydrocinchonine is a multidrug resistance (MDR) reversal agent that functions primarily by inhibiting the activity and expression of P-glycoprotein (P-gp). This inhibition plays a critical role in overcoming drug resistance in cancer treatment. Hydrocinchonine has demonstrated a synergistic apoptotic effect when combined with Paclitaxel in MES-SA/DX5 cells, making it a valuable tool for research aimed at addressing drug-resistant gynecological malignancies, such as uterine sarcoma.
  7. TRPC6 inhibitor

    TRPC6-IN-1 is a Transient Receptor Potential Canonical 6 Channel (TRPC6) inhibitor, with an EC50 of 4.66 μM.
  8. NHE3 inhibitor

    NHE3-IN-1 is a sodium/proton exchanger type 3 (NHE-3) inhibitor extracted from patent WO 2011019784 A1.
  9. T-type Ca2+ channel blocker

    ABT-639 is a novel, peripherally acting, selective T-type Ca2+ channel blocker.
  10. Cl- transport inhibitor

    H100 is a Cl- transport inhibitor, with partial effects against both the NaK2Cl cotransporter and the Band 3 anion exchanger, but no effect against KCl cotransporter, in human erythrocytes.
  11. Selamectin is a topical parasiticide and antihelminthic used on dogs and cats to treat and prevent infections of heartworms, fleas, ear mites, sarcoptic mange, and certain types of ticks in dogs as well as prevent heartworms, fleas, ear mites, hookworms, and roundworms in cats.
  12. ONO 2506 inhibits S100B synthesis in activated cultured astrocytes.
  13. K(Ca) 3.1 channel blocker

    NS6180 is a novel potent and selective KCa3.1 channel inhibitor(IC50= 9 nM) prevents T-cell activation and inflammation.
  14. LY404187 is a selective, potent and centrally active positive allosteric modulator of AMPA receptors.
  15. LY450108 is an alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptor potentiator.
  16. non-ionic emulsifying agent

    Polyoxyethylene stearate (POES) is a non-ionic emulsifying agent.
  17. Nav1.7 inhibitor

    AM-2099 is a potent and selective inhibitor of voltage-gated sodium channel Nav1.7 with an IC50 of 0.16 μM for human Nav1.7.
  18. Calcium channel blocker

    Mibefradil is a calcium channel blocker with moderate selectivity for T-type Ca2+ channels displaying IC50s of 2.7 μM and 18.6 μM for T-type and L-type currents, respectively.
  19. Calcium channel blocker

    Mibefradil 2Hcl is calcium channel blocker with moderate selectivity for T-type Ca2+ channels displaying IC50 values of 2.7 uM and 18.6 uM for T-type and L-type channels respectively.
  20. N-type calcium channel blocker-1 is an orally active analgesic agent which shows high affinity to functionally block N-type calcium channels with an IC50 of 0.7 μM in the IMR32 assay.
  21. T-type Ca2+ channel blocker

    ABT-639 hydrochloride is a novel, peripherally acting, selective T-type Ca2+ channel blocker.
  22. CNT2 Inhibitor

    CNT2 inhibitor-1 is a potent concentrative nucleoside transporter 2 Inhibitor (CNT2), with an IC50 of 640 nM for hCNT2.
  23. SGLT Inhibitor?€?

    LX4211 is a Dual SGLT1/SGLT2 Inhibitor
  24. Pinaverium Bromide is a spasmolytic agent with low incidence of anticholinergic effects. Pinaverium Bromide is also an antispasmodic.
  25. SGLT2 inhibitor

    Tofogliflozin is an inhibitor of subtype 2 sodium-glucose transport protein (SGLT2), which is responsible for at least 90% of the glucose reabsorption in the kidney.
  26. p97 ATPase inhibitor

    Dbeq is a selective and reversible inhibitor of p97 ATPase (IC50 = 1.5 uM).
  27. TRPV1 antagonist

    NJ-17203212 is a novel and selective TRPV1 antagonist, with IC50 of 65 nM and 102 nM for human TRPV1 and rat TRPV1.
  28. SGLT1/SGLT2 inhibitor

    Licogliflozin is a sodium glucose cotransporter (SGLT1 and SGLT2) inhibitor.
  29. Na+/H+-exchange inhibitor

    FR183998 free base is a potent Na+/H+-exchange inhibitor, with IC50s of 0.3 nM, 3.1 nM and 6.5 nM by measurement of pHi change in rat lymphocytes, rat and human platelets, respectively.
  30. K+ channel blocker?€?

    E-4031 dihydrochloride is a selective blocker of KV11.1 (hERG) channels; inhibits the rapid delayed-rectifier K+ current (IKr).
  31. Na+/H+ exchange inhibitor

    Cariporide (HOE-642) is a selective Na+/H+ exchange inhibitor.
  32. Oct4 Activator

    OAC1 enhances iPSC reprogramming efficiency by enhancing Oct4 and Nanog driven gene expression.
  33. photoactive TRPA1 activator

    Optovin is a reversible photoactive TRPA1 activator.
  34. glutamate release inhibitor

    Sipatrigine, a neuroprotective agent, is a glutamate release inhibitor, voltage-dependent sodium channel and calcium channel inhibitor, penetrating the central nervous system. Has potential to treat focal cerebral ischemia and stroke.
  35. CRM1 Inhibitor

    KPT185 is a selective CRM1 inhibitor. KPT-185 significantly inhibits leukemia cell proliferation with IC50 ranging from 100 nM to 500 nM, and induces cell-cycle arrest and apoptosis of AML cell lines and primary AML blasts.
  36. SUR inhibitor

    Lesinurad is a selective uric acid re-absorption inhibitor (SURI) and is also a selective inhibitor of URAT1, a transporter in the kidney that regulates uric acid excretion from the body.
  37. Oct3/4 Inducer

    O4I1 increases Oct3/4 mRNA levels in HEK293 cells by 2.5- and 4-fold at 10 uM and 20 uM, respectively.
  38. CFTR chloride channel inhibitor

    PPQ-102 is a compound that targets intracellular nucleotide binding domain(s) of CFTR and inhibits CFTR- mediated chloride current in a voltage-dependent and reversible manner.
  39. IBAT inhibitor

    S-8921 is an ileal Na+/bile acid cotransporter (IBAT) inhibitor.
  40. Sodium channel blocker

    Raxatrigine (GSK1014802) is a novel sodium channel blocker and is an effective anticonvulsant agent. In rats, GSK1014802 (20 - 80 mg/kg p.o.) attenuated the deficit in reversal learning induced by phencyclidine (PCP) in a dose-dependent way, which suggested the potential of GSK1014802 in the treatment of cognitive symptoms of schizophrenia. GSK2 was also a potent inhibitor of human MAO-B with pIC50 value of 7.96 but did not inhibit human MAO-A.
  41. ABCB1 (P-gp/MDR1) inhibitor

    TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity.
  42. MCT Inhibitor

    UK 5099 is a potent inhibitor of plasma membrane monocarboxylate transporters (MCTs) and the mitochondrial pyruvate carrier (MPC); inhibits pyruvate-dependent O2 consumption with an IC50 of 50 nM.
  43. Istaroxime hydrochloride is a positive inotropic agent that mediates its action through inhibition of sodium/potassium adenosine triphosphatase (Na+/K+ ATPase).

  44. EAAT1 inhibitor

    UCPH 101 is a selective non-substrate inhibitor of EAAT1 (IC50 values are 660, >300000 and >300000 nM for EAAT1, EAAT2 and EAAT3 respectively).
  45. intracellular Ca2+ handling modulator

    Caldaret is an intracellular Ca2+ handling modulator that acts through reverse mode Na+/Ca2+ exchanger inhibition.
  46. dihydropyridine calcium entry blocker

    Lemildipine is a new dihydropyridine calcium entry blocker.
  47. Calcium channel blocker

    Amlodipine aspartic acid impurity is the impurity of Amlodipine aspartic acid. Amlodipine aspartic acid is a calcium channel blocker with antihypertensive and antianginal properties.
  48. TRPA1 inhibitor

    HC-030031 is a selective TRPA1 blocker, antagonizing TRPA1-mediated calcium influx induced by AITC and formalin (IC50 = 6.2 and 5.3 uM, respectively).
  49. Na+/K+ ATPase modulator

    Rostafuroxin (PST-2238) is an ouabain-inhibitor counteracting specific forms of hypertension.
  50. Monocrotaline is a natural 11-membered macrocyclic pyrrolizidine alkaloid used in an animal model of pulmonary hypertension.

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