Membrane Transporters-Ion Channels

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  1. Na+/K+ ATPase modulator

    Rostafuroxin (PST-2238) is an ouabain-inhibitor counteracting specific forms of hypertension.
  2. Monocrotaline is a natural 11-membered macrocyclic pyrrolizidine alkaloid used in an animal model of pulmonary hypertension.
  3. 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.
  4. COX inhibitor

    Flufenamic acid is a nonsteroidal anti-inflammatory drug (NSAID). Inhibits calcium-activated chloride channels (CaCCs). Also increases currents through TRPC6 channels and inhibits currents through TRPC3 and TRPC7 channels.
  5. CaCC blocker

    Talniflumate is a calcium-activated chloride channel (CaCC) (hCLCA1/mCLCA3) blocker; reduces mucin synthesis and release in cell culture and animal models.
  6. 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.
  7. BCH

    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.
  8. CHC

    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.
  9. P-gp inhibitor

    P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.
  10. Atagabalin is related to gabapentin, which similarly binds to the α2δ calcium channels (1 and 2).
  11. Serotonin transporter inhibitor

    Imipramine Hydrochloride is a tricyclic antidepressant. Inhibits the serotonin and norepinephrine transporters but has little effect on the dopamine transporter.
  12. SGLT2 Inhibitor

    Luseogliflozin is an orally active second-generation sodium-glucose co-transporter 2 (SGLT2) inhibitor developed by Taisho Pharmaceutical for the treatment of patients with type 2 diabetes mellitus (T2DM).
  13. TRPV1 receptor antagonist

    A-889425 is a selective TRPV1 receptor antagonist. A-889425 blocks TRPV1 channels with an IC50 of 335 nM (rat) and 34 nM (human).
  14. CFTR inhibitor

    IOWH032 is a CFTR inhibitor.
  15. P-gp inhibitor

    ONT-093 is an orally bioavailable P-glycoprotein pump inhibitor, for the potential reversal of multidrug resistance in patients undergoing cancer chemotherapy.
  16. P-gp inhibitor

    Laniquidar is a third-generation P-gp inhibitor, which has been used in clinic trials for modulating multidrug resistance transporters.
  17. P-gp modulator

    Biricodar dicitrate (VX-710 dicitrate) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.
  18. SGLT2 inhibitor

    Ipragliflozin is a highly potent and selective SGLT2 inhibitor with IC50 of 2.8 nM; little and NO potency for SGLT1/3/4/5/6.
  19. TRPM8 and TRPA1 activator

    Icilin is a cooling agent that activates the novel cold receptors TRPM8 (CMR1) and TRPA1 (ANKTM1/TRPN1), members of the TRP ion channel family. Induces currents in CMR1-expressing HEK 293 cells (EC50 = 0.36 μM)
  20. VMAT2 inhibitor

    GZ-793A is a selective inhibitor of vesicular monoamine transporter 2 (VMAT2), which transports the monoamine neurotransmitters from cellular cytosol into synaptic vesicles.
  21. ACA is a channel blocker that acts on several transient receptor potential (TRP) channels, including TRPM2, TRPM8, and TRPC6 (IC50 = 1.7, 3.8, and 2.3 uM, respectively).
  22. voltage-gated sodium channel Nav1.7 inhibitor

    Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC50 of 8 nM. Pain relief. Limited CNS penetration.
  23. myosin II inhibitor

    Blebbistatin, a myosin II inhibitor, is photoinactivated by blue light.
  24. AMPA desensitization inhibitor

    Cyclothiazide is a benzothiadiazide that acts as a potentiator of AMPA receptors, positively modulating its response to glutamic acid (EC50 = 3.8 M).
  25. CFTR inhibitor

    CFTR inhibitor II, also known as GlyH-101, is a glycine hydrazide that selectively and reversibly blocks the CFTR channel (Ki = 4.3 uM).
  26. CRAC intermediate 2 is a intermediate compound for CRAC inhibitor synthesis, extracted from patent WO 2013059666A1.
  27. Sodium channel Blocker

    QX 314 chloride is a membrane impermeable quaternary derivative of lidocaine, a voltage-activated Na+ channel blocker
  28. NaV1.3 and NaV1.1 channels inhibitor

    ICA-121431 is a potent and selective inhibitor of human NaV1.3 and NaV1.1 channels (IC50 values are 13 and 23 nM respectively).
  29. AMPA receptor modulator

    Farampator has been investigated for its effect on AMPA receptors and researched for potential use in the treatment of schizophrenia and Alzheimer's Disease. It was found to improve short-term memory, but impaired episodic memory.
  30. VDAC inhibitor

    Erastin is a cell-permeable piperazinyl-quinazolinone compound that exhibits oncogene-selective lethality in cells with H-Ras mutations.
  31. hASBT inhibitor

    GSK2330672 is a highly potent, nonabsorbable apical sodium-dependent bile acid transporter inhibitor.
  32. NMDA receptor antagonist

    DNQX is a non-N-methyl-D-aspartate (non-NMDA) receptor complex antagonist.
  33. Sodium channel blocker

    Encainide HCl is a sodium channel blocker and class Ic antiarrhythmic. Encainide is a non-chiral antiarrhythmic and benzanilide derivative.
  34. Sodium channel blocker

    Disopyramide is an antiarrhythmic (class IA) and a sodium channel blocker.
  35. Na+/K+ ATPase inhibitor

    Melittin is a Na+/K+ ATPase inhibitor. It inhibits Gs and stimulates Gi activity. It inhibits protein kinase C and cAMP-dependent protein kinases.
  36. Ca2+ release inhibitor

    Dantrolene sodium is a muscle relaxant that acts by abolishing excitation-contraction coupling in muscle cells, probably by action on the ryanodine receptor.
  37. sodium channel protein inhibitor

    Oxcarbazepine is a sodium channel protein inhibitor.
  38. KCa2.1 channels activator

    GW 542573X is an activator of small-conductance Ca2+-activated K+ channels (KCa2).
  39. P-glycoprotein inhibitor

    XR9576 is a P-glycoprotein inhibitor undergoing research as an adjuvant against multidrug resistance in cancer
  40. SGLT2 inhibitor

    Remogliflozin inhibits the sodium-glucose transport (SGLT2) proteins, which are responsible for glucose reabsorption in the kidney.
  41. Selective calcium chelator

    BAPTA tetrapotassium is a selective calcium chelator with greater affinity for Ca2+ than Mg2+.
  42. TrpA1 channel agonist

    PF-4840154 is a non-electrophilic reference agonist of the TrpA1 channel. The TRPA1 channel is considered an attractive pain target based on the fact that TRPA1 knockout mice showed near complete attenuation of pain behaviors in some pre-clinical development models.
  43. ATP synthase inhibitor

    Oligomycin is a macrolide that acts as a specific inhibitor of the mitochondrial ATP-synthase and blocks oxidative phosphorylation.
  44. SERCA inhibitor

    Cyclopiazonic acid is an inhibitor of SERCA (endoplasmic reticulum Ca2+-ATPase) which induces the release of intracellular stored Ca2+, without increasing IP3 levels.
  45. AMPA Receptor Blocker

    IEM 1754 Dihydrobromide is a voltage-dependent open-channel blocker of AMPA receptors.
  46. NHE3 inhibitor

    Tenapanor acts as an inhibitor of the sodium-proton exchanger NHE3. This antiporter protein is found in the kidney and intestines, and normally acts to regulate the levels of sodium absorbed and secreted by the body.
  47. Selective calcium chelator

    BAPTA/AM, an intracellular calcium chelator, induces delayed necrosis by lipoxygenase-mediated free radicals in mouse cortical cultures.
  48. H3R antagonist/TRPV1 antagonist

    ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist and a transient receptor potential vanilloid type 1 (TRPV1) antagonist.
  49. TrxR1/CRM1 inhibitor

    Piperlongumine selectively kills cancer cells regardless of p53 status without harming normal cells. It binds to and inihbits proteins known to regulate oxidative stress, in particular, Glutathione S-transferase pi 1 (GSTP1).
  50. TRPA1 channel blocker

    TCS 5861528 is a TRPA1 channel blocker and an antagonizer of AITC- and 4-HNE-evoked calcium influx.

Items 151-200 of 2532

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