Membrane Transporters-Ion Channels

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  1. DPP8/9 Inhibitor

    DPP8/9-IN-2 is a selective inhibitor of dipeptidyl peptidase 8 and 9 (DPP8/DPP9) with potent inhibitory activity, exhibiting IC50 values of 0.22 nM and 3 nM, respectively. This compound has been implicated in research related to tumor biology and other pathological conditions. Notably, DPP8/9-IN-2 demonstrates certain cardiotoxicity, indicated by its IC50 values of 0.7 μM for the hERG potassium channel, 29.0 μM for the Nav1.5 sodium channel, and 27.7 μM for the Cav1.2 calcium channel.
  2. TRPA1 Inhibitor

    Aurothiomalate disodium acts as a TRPA1 inhibitor, effectively blocking NF-κB activation and inhibiting iNOS expression. This compound fosters the M2 transformation of macrophages and enhances the expression of TREM-2 and arginase-1. Aurothiomalate disodium is applicable in research concerning liver fibrosis, cirrhosis, and arthritis, providing insights into inflammation and tissue repair mechanisms.
  3. TRPC6 inhibitor

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

    NHE3-IN-1 is a sodium/proton exchanger type 3 (NHE-3) inhibitor extracted from patent WO 2011019784 A1.
  5. 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.
  6. 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.
  7. CNT2 Inhibitor

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

    LX4211 is a Dual SGLT1/SGLT2 Inhibitor
  9. 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.
  10. p97 ATPase inhibitor

    Dbeq is a selective and reversible inhibitor of p97 ATPase (IC50 = 1.5 uM).
  11. SGLT1/SGLT2 inhibitor

    Licogliflozin is a sodium glucose cotransporter (SGLT1 and SGLT2) inhibitor.
  12. 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.
  13. Na+/H+ exchange inhibitor

    Cariporide (HOE-642) is a selective Na+/H+ exchange inhibitor.
  14. 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.
  15. 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.
  16. 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.
  17. 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.
  18. IBAT inhibitor

    S-8921 is an ileal Na+/bile acid cotransporter (IBAT) inhibitor.
  19. 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.
  20. 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.
  21. 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).
  22. 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).
  23. 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.
  24. 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.
  25. Protein translocation Inhibitor

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

    Ko 143 is potent and selective inhibitor of breast cancer resistance protein multidrug transporter (BCRP) with an EC90 value of 26 nM.
  27. PDE1 inhibitor

    Vinpocetine is a Ca2+-calmodulin-dependent phosphodiesterase I (PDE1) inhibitor.
  28. serotonin transporter (SER) inhibitor

    Vilazodone Hydrochloride (EMD 68843 Hydrochloride) is a serotonin transporter (SER) inhibitor and 5-HT1A receptor partial agonist.
  29. Proton Pump inhibitor

    Pantoprazole is a proton pump inhibitor drug that inhibits gastric acid secretion.
  30. Na+/Ca2+ Exchanger Inhibitor

    KB-R7943 mesylate is a cell permeable, potent, selective NCKX inhibitor of the reverse mode of Na+/Ca2+ exchange in cells expressing NCX1.
  31. T-type calcium channel inhibitor

    MK-8998 (compound 33) is a potent and selective inhibitor of the T-type calcium channel.
  32. Nav inhibitor

    Nav1.7-IN-2 is an inhibitor of voltage-gated sodium channels (Nav), in particular Nav 1.7, with IC50 of 80 nM.
  33. Ca2+ channel agonist/CDK2 inhibitor

    Ca2+ channel agonist 1 is an agonist of N-type Ca2+ channel and an inhibitor of Cdk2, with EC50s of 14.23 μM and 3.34 μM, respectively, and is used as a potential treatment for motor nerve terminal dysfunction.
  34. P-gp inhibitor

    Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.
  35. P-gp inhibitor

    P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.
  36. Serotonin transporter inhibitor

    Imipramine Hydrochloride is a tricyclic antidepressant. Inhibits the serotonin and norepinephrine transporters but has little effect on the dopamine transporter.
  37. 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).
  38. CFTR inhibitor

    IOWH032 is a CFTR inhibitor.
  39. 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.
  40. P-gp inhibitor

    Laniquidar is a third-generation P-gp inhibitor, which has been used in clinic trials for modulating multidrug resistance transporters.
  41. 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.
  42. 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.
  43. 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.
  44. 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).
  45. 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).
  46. hASBT inhibitor

    GSK2330672 is a highly potent, nonabsorbable apical sodium-dependent bile acid transporter inhibitor.
  47. 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.
  48. 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.
  49. sodium channel protein inhibitor

    Oxcarbazepine is a sodium channel protein inhibitor.
  50. P-glycoprotein inhibitor

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

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