Membrane Transporters-Ion Channels

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  1. 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.
  2. 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.
  3. LY404187 is a selective, potent and centrally active positive allosteric modulator of AMPA receptors.
  4. LY450108 is an alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptor potentiator.
  5. Empagliflozin is a potent, selective sodium glucose co-transporter-2 inhibitor that is in development for the treatment of type 2 diabetes.
  6. non-ionic emulsifying agent

    Polyoxyethylene stearate (POES) is a non-ionic emulsifying agent.
  7. 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.
  8. 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.
  9. 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.
  10. CFTR corrector

    VX-661 is another cystic fibrosis transmembrane conductance regulator (CFTR) corrector in development for the treatment of cystic fibrosis.
  11. 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.
  12. T-type Ca2+ channel blocker

    ABT-639 hydrochloride is a novel, peripherally acting, selective T-type Ca2+ channel blocker.
  13. CRM1 inhibitor

    KPT-330 inhibitor of CRM1 (XPO1)-mediated nuclear export has selective anti-leukaemic activity in preclinical models of T-cell acute lymphoblastic leukaemia and acute myeloid leukaemia.
  14. SGLT Inhibitor?€?

    LX4211 is a Dual SGLT1/SGLT2 Inhibitor
  15. Pinaverium Bromide is a spasmolytic agent with low incidence of anticholinergic effects. Pinaverium Bromide is also an antispasmodic.
  16. 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.
  17. TRPV1 antagonist

    AMG 517 is a potent and selective TRPV1 antagonist.
  18. a-K-ATPase inhibitor

    Ouabain is a selective Na+, K+-ATPase inhibitor.
  19. 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.
  20. Potassium Channel Blocker

    TRAM-34 is a highly selective blocker of intermediate conductance Ca2+-activated K+ channels (KCa3.1) (Kd = 20 nM). Exhibits 200-1500-fold selectivity over KV, BKCa, KCa2, Na+, CRAC and Cl- channels. Suppresses the reactivation of lymphocytes by mitogenic stimuli.
  21. SGLT1/SGLT2 inhibitor

    Licogliflozin is a sodium glucose cotransporter (SGLT1 and SGLT2) inhibitor.
  22. 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.
  23. K+ channel blocker?€?

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

    Cariporide (HOE-642) is a selective Na+/H+ exchange inhibitor.
  25. CFTR inhibitor

    CFTRinh-172 is a voltage-independent, selective CFTR inhibitor
  26. Oct4 Activator

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

    Optovin is a reversible photoactive TRPA1 activator.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. 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.
  33. IBAT inhibitor

    S-8921 is an ileal Na+/bile acid cotransporter (IBAT) inhibitor.
  34. 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.
  35. 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.
  36. 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.
  37. Istaroxime hydrochloride is a positive inotropic agent that mediates its action through inhibition of sodium/potassium adenosine triphosphatase (Na+/K+ ATPase).

  38. 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).
  39. AMPA Receptor Antagonist

    NBQX is a potent, selective and competitive AMPA receptor antagonist.
  40. intracellular Ca2+ handling modulator

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

    Lemildipine is a new dihydropyridine calcium entry blocker.
  42. 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.
  43. 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).
  44. Na+/K+ ATPase modulator

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

    CP 465022 is a selective, non-competitive AMPA antagonist with IC50 of 25 nM in rat cortical neurons that displays potent anticonvulsant activity.
  47. CaCC blocker

    Talniflumate is a calcium-activated chloride channel (CaCC) (hCLCA1/mCLCA3) blocker; reduces mucin synthesis and release in cell culture and animal models.
  48. TRPC1/4/5 channels inhibitor

    Pico145 is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (?)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8.
  49. LAT1 inhibitor

    BCH is an inhibitor of L-type amino acid transporter LAT1. Suppresses growth and induces apoptosis via activation of caspases in KB, Saos2 and C6 cancer cell lines.
  50. MCT inhibitor

    CHC is a monocarboxylic acid transport (MCT) inhibitor. Exhibits antitumoral and antiangiogenic activity in gliomas; decreases glycolytic metabolism, migration, and invasion in U251 cells.

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