Membrane Transporters-Ion Channels

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  1. dual T-type and L-type calcium channel blocker

    Efonidipine hydrochloride monoethanolate (NZ-105 hydrochloride monoethanolate) is a dual T-type and L-type calcium channel blocker (CCB).
  2. SGLT inhibitor

    Ertugliflozin pidolate belongs to the class of potent and selective inhibitors of the sodium-dependent glucose cotransporters (SGLT), more specifically the type 2 which is responsible for about 90% of the glucose reabsorption from glomerulus.
  3. Fluralaner (INN) is a systemic insecticide and acaricide Fluralaner through potent blockage of GABA and L-glutamate gated chloride channels.
  4. L-type calcium-channel antagonist

    Etripamil (MSP-2017) is a short-acting L-type calcium-channel antagonist with a rapid onset of action designed for intranasal administration, used to treat Paroxysmal Supraventricular Tachycardia (PSVT). Etripamil (MSP-2017) slows atrioventricular nodal conduction and prolongs atrioventricular nodal refractory periods by inhibiting calcium ion influx through the calcium slow channels in the atrioventricular node cells.
  5. IP3R inhibitor

    2-Aminoethyl diphenylborinate (2-APB) is a cell-permeable inhibitor of IP3R. 2-Aminoethyl diphenylborinate also inhibits the store-operated Ca2+ (SOC) channel and activates some TRP channels (V1, V2 and V3).
  6. μ- opioid receptor agonist

    Trimebutine Maleate is a drug with antimuscarinic and weak mu opioid agonist effects. Trimebutine Maleate modulates the calcium and potassium channels, relieves abdominal pain in patients with irritable bowel syndrome.
  7. TRPV1 agonist

    Zucapsaicin, also known as cis-Capsaicin, is a medication used to treat osteoarthritis of the knee and other neuropathic pain. It is applied three times daily for a maximum of three months. It reduces pain, and improves articular functions.
  8. 5-HT receptor /dopamine receptors antagonist

    Metergoline is a psychoactive drug of the ergoline chemical class which acts as a ligand for various serotonin and dopamine receptors.
  9. Calcium channel antagonist

    Aranidipine (MPC1304) is a Ca2+ channel antagonist with potent and long-lasting antihypertensive effects.
  10. proton pump inhibitor

    Lansoprazole sodium(AG-1749) is a proton pump inhibitor which prevents the stomach from producing acid.
  11. CFTR potentiator

    PG 01 is a cystic fibrosis transmembrane conductance regulator (CFTR) potentiator. PG 01 is effective on G970R although with a significant decrease in potency relative to E193K and δF508.
  12. VDAC inhibitor

    WEHI-9625 is a tricyclic sulfone small molecule inhibitor of apoptosis with an EC50 of 69 nM. WEHI-9625 binds to VDAC2 and promotes its ability to inhibit apoptosis driven by mouse BAK, but is completely inactive against both human BAK and the closely related apoptosis effector BAX.
  13. P-gp/BCRP dual inhibitor

    FD 12-9 is a flavonoid dimer, acts as a dual inhibitor of P-gp and BCRP, with EC50s of 285 nM and 0.9 nM, respectively. Anti-glioblastoma activity.
  14. AQP7 inhibitor

    Z433927330 is a potent and selective inhibitor of Aquaporin-7 (AQP7), less potently inhibits AQP3 and AQPs9, with IC50s of ~0.2 ?M, ~0.7 ?M and ~1.1 ?M for mAQP7, mAQP3 and mAQP9, respectively.
  15. Na+/Ca2+ exchanger (NCX) inhibitor

    ORM-10103 is a specific inhibitor of the Na+/Ca2+ exchanger (NCX), which decreases the NCX current with estimated IC50s of 55 and 67 nM at -80 and at 20 mV, respectively.
  16. Piezo1 channel antagonist

    Dooku1, an analog of Yoda1, is a selective antagonist of the endogenous Piezo1 channel.
  17. Kir7.1 potassium channels blocker

    ML418 is a selective, sub-micromolar pore blocker of Kir7.1 potassium channels. The inward rectifier potassium (Kir) channel Kir7.1 (KCNJ13) is a key regulator of melanocortin signaling in the brain, electrolyte homeostasis in the eye, and uterine muscle contractility during pregnancy.
  18. CFTR corrector

    CFTR corrector 2 is a cystic fibrosis transmembrane conductance corrector (CFTR), extracted from patent US20140274933.
  19. Nav1.7/Nav1.8 blocker

    DSP-2230 is a selective Nav1.7/Nav1.8 blocker.
  20. potassium channel blocker

    VU0134992 is a selective inward rectifier potassium (Kir) channel Kir4.1 blocker with an IC50 of 0.97 ?M.
  21. MCT1 inhibitor

    BAY-8002 is a potent, selective, orally active inhibitor of monocarboxylate transporter 1 (MCT1), with an IC50 of 85 nM in the MCT1-expressing DLD-1 cells, displays excellent selectivity against MCT4. Anti-tumor activity.
  22. EAAT2 modulator

    GT 949 is a selective excitatory amino acid transporter-2 (EAAT2) positive allosteric modulator with an EC50 of 0.26 nM.
  23. Kv3 potassium channel modulator

    AUT1 is a Kv3 potassium channel modulator with pEC50s of 5.33 and 5.31 for human recombinant Kv3.1b and Kv3.2a, respectively, exhibits 10-fold lower potency at human recombinant Kv3.3 channel (pEC50, 4.5).
  24. URAT1 inhibitor

    URAT1 inhibitor 1 (1g) is a uric acid transporter 1 (URAT1) inhibitor, with an IC50 of 32 nM. URAT1 inhibitor 1 has potential to treat hyperuricemia associated with gout.
  25. SGLT1 inhibitor

    SGL5213 is a potent, oral active and low-absorbable sodium-dependent glucose cotransporter 1 (SGLT1) inhibitor, with IC50 values of 29 nM and 20 nM for hSGLT1 and hSGLT2, respectively.
  26. NaV1.8 blocker

    PF-06305591 is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile.
  27. L-Palmitoylcarnitine is a fatty acid metabolite.
  28. Sodium channel blocker

    Metaflumizone is a semicarbazone insecticide, acts as a potent sodium channel blocker.
  29. SLC13A5 inhibitor

    BI01383298 is a potent inhibitor of SLC13A5, being selective over other family members and other transporters.
  30. Iron mobilizer

    Guanosine 5'-diphosphate is a nucleoside diphosphate. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulating the interleukin-6 (IL-6)/stat-3 pathway.
  31. Na+/H+ exchanger inhibitor

    5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) derives from an amiloride and is a potent Na+/H+ exchanger inhibitor, which decreases the intracellular pH (pHi) and induces apoptosis in leukemic cells.
  32. CFTR potentiator

    GLPG2451 is a cystic fibrosis transmembrane conductance regulator (CFTR) potentiator, which effectively potentiates low temperature rescued F508del CFTR with an EC50 of 11.1 nM.
  33. NaV 1.7 inhibitor

    NaV1.7 inhibitor-1 is an efficacious voltage-gated sodium channel (NaV) 1.7 inhibitor with an IC50 of 0.6 nM for hNaV1.7, exhibits 80-fold selectivity versus hNaV1.5.
  34. Kv3.1/Kv3.2 modulator

    Kv3 modulator 4 is a Kv3.1 (pEC50=5.45) and Kv3.2 modulator extracted from patent WO2018020263A1, Cyclobutyl structure.
  35. Kv3.1/Kv3.2/Kv3.3 channels modulator

    Kv3 modulator 3 (Compound 4) is a selective modulator of Kv3.1 and/or Kv3.2 and/or Kv3.3 channels extracted from patent WO2017098254A1, compound 4, has analgesic activity for use in the prophylaxis o or treatment of pain.
  36. nucleoside transport inhibitor

    Soluflazine is a nucleoside transport inhibitor with anticonvulsant action. Soluflazine can be used as an antiepileptic agent.
  37. Eslicarbazepine is an oral anticonvulsant indicated for the adjunctive treatment of partial seizures.
  38. Nav1.7 inhibitor

    GNE-616 is a highly potent, metabolically stable, orally bioavailable, and subtype selective Nav1.7 inhibitor (Ki of 0.79 nM and Kd of 0.38 nM for hNav1.7) for the treatment of chronic pain.
  39. Cav 2.2 blocker

    Cav 2.2 blocker 1 (compound 9) is a N-type calcium channel (Cav 2.2) blocker for the treatment of pain, with an IC50 of 1 nM.
  40. SGLT2 inhibitor

    Dapagliflozin impurity is an enantiomer of Dapagliflozin which is a sodium-glucose transporter 2 inhibitor.
  41. Nav1.7-selective inhibitor

    GNE-0439 is a novel Nav1.7-selective inhibitor with IC50 of 0.34 uM and inhibits Nav1.5 with an IC50 of 38.3 μM.
  42. NCX inhibitor

    ORM-10962 is a potent, highly selective sodium-calcium exchanger (NCX) inhibitor, with IC50 values of 67 and 55 nM for the reverse and forward mode inhibition, respectively.
  43. anion channel inhibitor

    Endovion (NS3728) is a pharmacological anion channel inhibitor (like chloride channel) and the specific VRAC/VSOAC blocker. Endovion (NS3728) is also an Anoctamin-1 (ANO 1) channel inhibitor.
  44. SGLT inhibitor

    SGLT inhibitor-1 is a potent dual inhibitor of sodium glucose co-transporter proteins (SGLTs), inhibits hSGLT1 and hSGLT2 with IC50s of 43 nM and 9 nM, respectively.
  45. SLC34A1 inhibitor

    PF-06869206 is an orally bioavailable selective inhibitor of the sodium-phosphate cotransporter NaPi2a (SLC34A1) with an IC50 of 380 nM.
  46. SGLT2 inhibitor

    HSK0935 is a potent, highly selective and orally available SGLT2 inhibitor with an IC50 of 1.3 nM. Antihyperglycemic activities.
  47. Tulrampator (CX-1632) is an orally bioavailable positive AMPAR (allosteric modulator of AMPA receptor). Antidepressant.
  48. VRAC inhibitor

    DCPIB is a selective, reversible and potent inhibitor of volume-regulated anion channels (VRAC), voltage-dependently activates potassium channels TREK1 and TRAAK, inhibits TRESK, TASK1 and TASK3 (IC50s, 0.14, 0.95, 50.72 μM, respectively).
  49. L-type calcium antagonist

    Barnidipine hydrochloride (Mepirodipine hydrochloride) is an L-type calcium antagonist (CaA) with high affinity for [3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors.
  50. NaV1.8 blocker

    PF 04531083 is a selective NaV1.8 blocker, and used for the research of neuropathic/inflammatory pain.

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