Membrane Transporters-Ion Channels

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  1. Calcium channel proteins inhibitor

    Dantrolene sodium is a inhibitor of calcium channel proteins, inhibiting the release of Ca2+ from the sarcoplasm. Dantrolene sodium is a skeletal muscle relaxant which acts by blocking muscle contraction beyond the neuromuscular junction.
  2. SChE inhibitor

    Dibucaine (USAN) is an amide local anesthetic. Dibucaine reversibly binds to and inactivates sodium channels in the neuronal cell membrane. Inhibition of sodium channels prevents the depolarization of nerve cell membranes and inhibits subsequent propagation of impulses along the course of the nerve, thereby limiting the excitation of nerve endings. This results in loss of sensation.
  3. 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.
  4. 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.
  5. 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.
  6. 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).
  7. proton pump inhibitor

    Lansoprazole sodium(AG-1749) is a proton pump inhibitor which prevents the stomach from producing acid.
  8. 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.
  9. 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.
  10. 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.
  11. 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.
  12. 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.
  13. 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.
  14. sodium channel inhibitor

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

    ML241 is a potent and selective inhibitors of p97 ATPase. ML241 inhibit p97 ATPase with IC(50) values of 100 nM.
  16. 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.
  17. P-gp inhibitor

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

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

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

    K+ Channel inhibitor, building block for synthesis of dihydropyrazolopyrimidine inhibitors of Kv1.5 (IKur).
  21. 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.
  22. 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).
  23. VMAT2 inhibitor

    Valbenazine is a potent and selective VMAT2 inhibitor.
  24. 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.
  25. SINE/CRM1 inhibitor

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

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

    Lauric acid is a proton pump inhibitor potentially for the treatment of helicobacter pylori infections.
  28. 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.
  29. proton pump inhibitor

    (R)-Lansoprazole is a proton pump inhibitor which prevents the stomach from producing acid.
  30. 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.
  31. 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.
  32. 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.
  33. 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).
  34. CRAC channel inhibitor

    GSK-7975A is a potent and orally available CRAC channel inhibitor.
  35. 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.
  36. TRPC6 inhibitor

    DS88790512 is a potent, selective, and orally bioavailable TRPC6 inhibitor with an IC50 of 11 nM.
  37. CRM1 inhibitor

    CBS9106 (SL-801) is a reversible oral CRM1 inhibitor with CRM1 degrading and antitumor activities.
  38. NaV1.7 inhibitor

    GNE-131 is a potent and selective inhibitor of human sodium channel NaV1.7, with an IC50 of 3 nM.
  39. NCX inhibitor

    SN 6 is a selective Na+/Ca2+ exchanger (NCX) inhibitor, and inhibits 45Ca2+ uptake by NCX1, NCX2, and NCX3, with IC50s of 2.9, 16, and 8.6 μM, respectively.
  40. serotonin-norepinephrine reuptake inhibitor

    Nitroxazepine is a tricyclic antidepressant (TCA) for the treatment of depression. Nitroxazepine acts as a serotonin-norepinephrine reuptake inhibitor.
  41. MRP1/Pgp inhibitor

    Reversan (CBLC4H10) is a potent and nontoxic multidrug resistance-associated protein 1 (MRP1) and P-glycoprotein (Pgp) inhibitor.
  42. GLT-1/EAAT2 reuptake inhibitor

    WAY-213613 is a potent, selective nonsubstrate reuptake inhibitor of GLT-1/EAAT2 with IC50 of 85 nM EAAT2.
  43. ROMK inhibitor

    VU591 hydrochloride is a potent, selective renal outer medullary potassium channel (ROMK or Kir1.1) inhibitor, with an IC50 of 0.24 μM.
  44. SERT inhibitor

    DSP-1053 is a potent Serotonin Transporter (SERT) (Ki=1.02 nM) inhibitor with partial 5-HT1A receptor (Ki=5.05 nM) agonistic activity.
  45. SOCE inhibitor

    SOCE inhibitor 1 is a store-operated calcium entry (SOCE) inhibitor with an IC50 of 4.4 μM.
  46. Nav1.7 inhibitor

    PF-05241328 is a potent and selective inhibitor of human Nav1.7 voltage-dependent sodium channels (Nav1.7), with an IC50 of 31 nM.
  47. ENT1 inhibitor

    Draflazine (R-75231) is a ENT1 inhibitor.
  48. TRPC3 inhibitor

    Pyr3 is a selective inhibitor of transient receptor potential canonical channel 3 (TRPC3), with an IC50 of 700 nM for TRPC3-mediated Ca2+ influx.
  49. ABCG2 inhibitor

    ML230 (CID44640177; SID 88095709) is a selective inhibitor of ATP-binding cassette (ABC) transporter ABCG2, and 36-fold selective for ABCG2 over ABCB1 with EC50s values of 0.13 μM and 4.65 μM, respectively.
  50. tropomyosin inhibitor

    ATM-3507 is a potent tropomyosin inhibitor with IC50s from 3.83-6.84 μM in human melanoma cell lines.

Items 51-100 of 957

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