Membrane Transporters-Ion Channels

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  1. SGLT2 inhibitor

    Dapagliflozin ((2S)-1,2-propanediol, hydrate), a new type of drug used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine.
  2. SGLT2 inhibitor

    Tofogliflozin hydrate (CSG-452 hydrate) is a potent and highly specific sodium/glucose cotransporter 2 (SGLT2) inhibitor with an IC50 of 2.9 nM and Ki values of 2.9 nM, 14.9 nM, and 6.4 nM for human, rat, and mouse SGLT2.
  3. 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.
  4. 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).
  5. proton pump inhibitor

    Lansoprazole sodium(AG-1749) is a proton pump inhibitor which prevents the stomach from producing acid.
  6. 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.
  7. 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.
  8. 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.
  9. 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.
  10. MCT inhibitor

    7ACC2 is a new potent MCT inhibitor with IC50 of 11 nM for inhibition of [14C]-lactate influx; new antitumor treatment targeting lactate transport in cancer cells.
  11. SUR/URAT1 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.
  12. sodium channel inhibitor

    Levobupivacaine is a local anaesthetic drug belonging to the amino amide group.
  13. p97 ATPase inhibitor

    ML241 is a potent and selective inhibitors of p97 ATPase. ML241 inhibit p97 ATPase with IC(50) values of 100 nM.
  14. HIV integrase inhibitor

    GSK744 is a potent HIV integrase inhibitor as an oral lead-in tablet and long-acting injectable for the treatment and prevention of HIV infection.
  15. P-gp inhibitor

    MC-70 is a potent P-gp inhibitor (EC50 = 0.69 uM).
  16. voltage-gated sodium channel inhibitor

    Procaine is a benzoic acid derivative with local anesthetic and antiarrhythmic properties.
  17. proton pump inhibitor

    Rabeprazole sodium is an antiulcer drug in the class of proton pump inhibitors.
  18. K+ Channel inhibitor

    K+ Channel inhibitor, building block for synthesis of dihydropyrazolopyrimidine inhibitors of Kv1.5 (IKur).
  19. URAT1 inhibitor

    UR 1102, inhibitor of the renal urate transporter URAT1 with high selectivity to URAT1 over OAT1 and OAT3 in vitro (Ki values 0.057 uM, 7.2 uM, and 2.4 uM, respectively), capable of increasing the fractional excretion of urinary uric acid, and reducing plasma uric acid more effectively than Benzbromarone.
  20. BCRP inhibitor

    KS-176 is a potent and selective inhibitor of the breast cancer resistance protein (BCRP) multidrug transporter (IC50 values are 0.59 and 1.39 uM in Pheo A and Hoechst 33342 assays respectively).
  21. VMAT2 inhibitor

    Valbenazine is a potent and selective VMAT2 inhibitor.
  22. Wnt/beta-catenin inhibitor

    Hexachlorophene is a potent KCNQ1/KCNE1 potassium channel activator with EC50 of 4.61 ?? 1.29 uM; also is an inhibitor of Wnt/beta-catenin signaling.
  23. SINE/CRM1 inhibitor

    KPT276, analog of KPT-185, is a selective inhibitor of nuclear export (SINE) and CRM1.
  24. CRAC channel inhibitor

    YM-58483 is the first selective and potent inhibitor of CRAC channels and subsequent Ca2+ signals.
  25. Proton pump inhibitor

    Lauric acid is a proton pump inhibitor potentially for the treatment of helicobacter pylori infections.
  26. Nav1.7 Inhibitor

    PF-05089771 is a Selective Nav1.7 Inhibitor (IC50 = 11 nM) that interacts with the voltage-sensor domain (VSD) of domain IV.
  27. proton pump inhibitor

    (R)-Lansoprazole is a proton pump inhibitor which prevents the stomach from producing acid.
  28. Kir2 family channels inhibitor

    ML133 hydrochloride is a selective Kir2 family channels inhibitor, with an IC50 of 1.8 μM at pH 7.4 and 290 nM at pH 8.5.
  29. GlyT inhibitor/NMDA receptor

    Sarcosine is a glycine transporter type 1 (GlyT) inhibitor and an N-methyl-D-aspartate (NMDA) receptor co-agonist at the glycine binding site.
  30. elastogenesis inhibitor

    L-Ascorbic acid sodium salt (Sodium L-ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid sodium salt inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid sodium salt is also a collagen deposition enhancer and an elastogenesis inhibitor.
  31. Na+/Ca2+ exchange Inhibitor

    CGP 37157 is a benzothiazepine that acts as a selective inhibitor of the mitochondrial sodium-calcium exchanger (IC50 = 0.36 μM in isolated mitochondria).
  32. CRAC channel inhibitor

    GSK-7975A is a potent and orally available CRAC channel inhibitor.
  33. plasmodium ATP4 inhibitor

    (+)-SJ733 is an inhibitor of plasmodium ATP4, leading to rapid clearance in vivo by inducing physical changes in infected, treated red cells.
  34. P-glycoprotein inhibitor

    Encequidar mesylate (HM30181 mesylate; HM30181A mesylate) is a competitive and potent P-glycoprotein inhibitor.
  35. BCRP inhibitor

    YHO-13351 (free base) is the water-soluble prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP.
  36. SGLT2 inhibitor

    Ipragliflozin (L-Proline) is a highly potent and selective SGLT2 inhibitor with an IC50 of 2.8 nM; little and NO potency for SGLT1/3/4/5/6.
  37. triple reuptake inhibitor

    Dasotraline is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.
  38. Nav1.7 sodium channel inhibitor

    Raxatrigine hydrochloride (GSK-1014802 hydrochloride) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.
  39. HCN channels inhibitor

    Zatebradine (UL-FS-49 (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 values 1.96 ?M.
  40. triple reuptake inhibitor

    Dasotraline hydrochloride (SEP-225289 hydrochloride) is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.
  41. TASK1(KCNK3) inhibitor

    ML365 is a novel selective small molecule inhibitor of TASK1(KCNK3) with IC50 of 4 nM(thallium influx fluorescent assay) and 16 nM(automated electrophysiology assay).
  42. CRM1 inhibitor

    Eltanexor Z-isomer (KPT-8602 Z-isomer) is the less active isomer of KPT-8602. KPT-8602 is a potent CRM1 inhibitor.
  43. Na+/H+ exchange inhibitor

    Eniporide hydrochloride (EMD-96785 hydrochloride) is a potent Na+/H+ exchange inhibitor.
  44. TRPC3 inhibitor

    Pyr6 is a selective inhibitor of TRPC3 with IC50 of 0.49 uM(Ca2+ influx inhibition in thapsigargin depleted native RBL-2H3 cells).
  45. sphingomyelin synthase inhibitor

    Dofequidar, also known as MS-209, is a quinolone-derived sphingomyelin synthase inhibitor that blocks P-glycoprotein and multidrug resistance-associated protein-1, is under development by Schering for the potential treatment of multidrug resistant tumors.
  46. SGLT1 inhibitor

    Mizagliflozin (DSP-3235 free base) is a potent, orally active and selective SGLT1 inhibitor, with a Ki of 27 nM for human SGLT1.
  47. SGLT1 inhibitor

    KGA-2727 is a first selective, high-affinity and orally active SGLT1 inhibitor with Kis of 97.4 nM and 43.5 nM for human and rat SGLT1, respectively.
  48. CRAC inhibitor

    RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM.
  49. inhibitor of Kv2.1 and Kv2.2

    RY785 (Kv2-IN-A1) is an inhibitor of Kv2.1 and Kv2.2.
  50. TRPC5 inhibitor

    AC1903 is a specific and selective inhibitor of TRPC5 and has podocyte-protective properties.

Items 101-150 of 957

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