Membrane Transporters-Ion Channels

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  1. inhibitor of Kv2.1 and Kv2.2

    RY785 (Kv2-IN-A1) is an inhibitor of Kv2.1 and Kv2.2.
  2. sodium channel blocker

    Levobupivacaine hydrochloride is a sodium channel blocker.
  3. VK-II-36 is a carvedilol analog that suppresses sarcoplasmic reticulum (SR) Ca(2+) release but does not block the β-receptor.
  4. OPRM1/OPRD1 agonist

    ML335 (CYM 51010, CID-23723457) is an agonist for OPRM1(μ-opioid receptor)-OPRD1(δ-opioid receptor) heterodimerization with EC50 of 403 nM demonstrating selectivity over the individual OPRM1 and OPRD1 receptors and the serotonin HT5A receptor with EC50 of 14.9 μM, 1.1 μM, and >40 μM, respectively.
  5. antagonist of Vanilloid receptor type 1

    A-784168 is a potent and selective antagonist of Vanilloid receptor type 1 (TRPV1).
  6. TRPC5 inhibitor

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

    Solamargine, a derivative from the steroidal solasodine in Solanum species, exhibits anticancer activities in numerous types of cancer. Solamargine induces non-selective cytotoxicity and P-glycoprotein inhibition.
  8. anticancer agent

    5,7,4'-Trimethoxyflavone is isolated from Kaempferia parviflora (KP) that is a famous medicinal plant from Thailand. 5,7,4'-Trimethoxyflavone induces apoptosis, as evidenced by increments of sub-G1 phase, DNA fragmentation, annexin-V/PI staining, the Bax/Bcl-xL ratio, proteolytic activation of caspase-3, and degradation of poly (ADP-ribose) polymerase (PARP) protein.5,7,4'-Trimethoxyflavone is significantly effective at inhibiting proliferation of SNU-16 human gastric cancer cells in a concentration dependent manner.
  9. VDAC1/Apoptosis inhibitor

    NSC 15364 is an inhibitor of VDAC1 oligomerization and apoptosis.
  10. ATPase activator

    Periplocin is a cardiotonic steroid isolated from Periploca forrestii. Periplocin promotes tumor cell apoptosis and inhibits tumor growth. Periplocin has the potential to facilitate wound healing through the activation of Src/ERK and PI3K/Akt pathways mediated by Na/K-ATPase.
  11. glutamine transporter ASCT2 inhibitor

    GPNA hydrochloride is a well known substrate of the enzyme γ-glutamyltransferase (GGT). GPNA hydrochloride is a specific glutamine (Gln) transporter ASCT2 inhibitor.
  12. Eleclazine, also known as GS-6615, is a selective late sodium current inhibitor. Eleclazine is potentially useful for treatment of coronary vasodilators, antiarrhythmics and vasodilators.
  13. Caroverine hydrochloride is a potent, competitive and reversible antagonist of NMDA and AMPA glutamate receptor. Caroverine hydrochloride is also an antioxidant and calcium-blocking agent that exhibits vasorelaxant action. Caroverine hydrochloride can be used for the research of inner ear tinnitus.
  14. MCU modulator

    MCU-i4 is a novel negative modulator of the MCU, binding MICU1 and impairing muscle cell growth.
  15. Ampa Receptor Antagonist

    ATPO is a potent and Selective Ampa Receptor Antagonist.
  16. gastric H+/K+ ATPase inhibitor

    Soraprazan is a reversible, and fast-acting inhibitor of gastric H+/K+ ATPase.
  17. Proton Pump inhibitor

    Linaprazan (AZD0865) inhibits gastric H+,K+-ATPase by K+-competitive binding. (IC50: 1.0 ± 0.2 μM) It is a acid-suppressing agents with rapid onset of action and potent acid inhibition.
  18. KCNQ2/Q3 potassium channel activator

    ICA-069673 is a KCNQ2/Q3 potassium channel activator with an IC50 of 0.69 μM.
  19. BCRP inhibitor

    (S)-ML753286 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter.
  20. TRPV4 antagonist

    HC-067047 is a potent and selective TRPV4 antagonist and reversibly inhibits currents through the human, rat, and mouse TRPV4 orthologs with IC50 values of 48 nM, 133 nM, and 17 nM, respectively.
  21. Nav1.8 channel blocker

    PF-01247324 is a selective and orally bioavailable Nav1.8 channel blocker with an IC50 of 196 nM for recombinant human Nav1.8 channel.
  22. SGLT1/SGLT2 inhibitor

    LX2761 is chemically stable and potent inhibitor against sodium-dependent glucose cotransporter 1 (SGLT1) and SGLT2 in vitro with IC50s of 2.2 nM and 2.7nM for hSGLT1 and hSGLT2, but displays specific SGLT1 inhibition in the gastrointestinal (GI) tract.
  23. TRPV4 agonist

    RN-1747 is a selective transient receptor potential cation channel subfamily V member 4 (TRPV4) agonist, with EC50 values are 0.77 μM, 4.0 μM and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4 respectively. RN-1747 also antagonizes TRPM8, with an IC50 of 4 μM.
  24. TRPV4 antagonist

    RN-1734 is selective antagonist of the TRPV4 channel, completely antagonizes 4αPDD-mediated activation of TRPV4 with comparable, low micromolar IC50s for all three species (hTRPV4: 2.3 μM, mTRPV4: 5.9 μM, rTRPV4: 3.2 μM).
  25. TRPM8 inhibitor

    BCTC is a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells.
  26. NaV1.7 blocker

    XEN907 is a novel spirooxindole NaV1.7 blocker, inhibits hNaV1.7 with IC50 of 3 nM.
  27. Memory-enhancing agent

    1-BCP is a centrally active drug that modulates AMPA receptor gated currents. 1-BCP is a memory-enhancing agent.
  28. AMPA receptor blocker

    gamma-DGG is a competitive AMPA receptor blocker.
  29. HCN channel blocker

    ZD7288 is a selective hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker.
  30. proton pump antagonist

    Pumaprazole is a reversible proton pump antagonist.
  31. SMN2 splicing modulator

    Branaplam (LMI070) is a highly potent, selective and orally active small molecule SMN2 splicing modulator.
  32. calcium channel antagonist

    SM-6586 is a calcium channel antagonist and inhibitor of Na+/H+ and Na+/Ca2+ exchange transport, potentially for the treatment of cerebrovasular diseases and hypertension.
  33. dihydropyridine Ca2+ antagonist

    CV-159 is a unique dihydropyridine Ca2+ antagonist with an anti-calmodulin (CaM) action, and has antiinflammatory activities.
  34. CFTR inhibitor

    (R)-BPO-27 is a potent CFTR inhibitor with an IC50 of 4 nM.
  35. TRPV4 ion channel blocker

    GSK2798745 is a first-in-class, highly potent, selective, orally active transient receptor potential vanilloid 4 (TRPV4) ion channel blocker with IC50s of 1.8 and 1.6 nM for hTRPV4 and rTRPV4, respectively.
  36. Na+-dependent glutamate transporter inhibitor

    MPDC is a potent and competitive inhibitor of the Na+-dependent high-affinity glutamate transporter in forebrain synaptosomes.
  37. TRPC6 inhibitor

    SAR7334 is a potent and specific TRPC6 inhibitor, inhibiting TRPC6 currents with IC50 of 7.9 nM.
  38. TRPML3 ion channel activator

    SN 2 is a novel and potent activator of TRPML3 ion channel with EC50 of 1.8??0.13 μM.
  39. AMPA receptor antagonist

    SYM 2206 is a novel, potent, non-competitive AMPA receptor antagonist.
  40. BTS

    Myosin S1 ATPase Inhibitor

    BTS is a potent inhibitor of Ca2+-stimulated myosin S1 ATPase (IC50 ~ 5 μM) and reversibly blocks the gliding motility.
  41. KCC2 inhibitor

    VU 0240551 is a small molecule inhibitor of the neuronal K-Cl cotransporter, KCC2 (IC50 = 560 nM for K+ uptake assay in KCC2-overexpressing cells).
  42. gastric H+/K+-ATPase inhibitor

    Tegoprazan, a potassium-competitive acid blocker, is a potent, oral active and highly selective inhibitor of gastric H+/K+-ATPase that could control gastric acid secretion and motility, with IC50 values ranging from 0.29-0.52 μM for porcine, canine, and human H+/K+-ATPases in vitro.
  43. Calcium Channel Inhibitor

    Gabapentin enacarbil (XP-13512) is a prodrug for the anticonvulsant and analgesic drug gabapentin.
  44. TRPM8 agonist

    D-3263 is an agonist of transient receptor potential melastatin member 8 (TRPM8) with potential antineoplastic activity.
  45. non-voltage dependent calcium channel blocker

    Carboxyamidotriazole (L 651582) is a blocker of non-voltage dependent calcium channel.
  46. Potassium Channel inhibitor

    Azimilide(NE-10064) is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes.
  47. IKs blocker

    JNJ 303 is a potent IKs blocker with an IC50 value of 64 nM.
  48. HERG activator

    RPR-260243 is a novel activator of HERG; modifies HERG currents inhibited by dofetilide (IC50 = 58 nM); little effect on HERG current amplitude and no significant effects on steady-state activation parameters or on channel inactivation processes.
  49. VMAT2 inhibtior

    NBI-98782(alpha-dihydrotetrabenazine) is a vesicular monoamine transporter (VMAT2) inhibtior with an Ki value of 0.97 nM.
  50. IBAT inhibitor

    Elobixibat is a potent ileal bile acid transporter (IBAT) inhibitor with IC50 values of 0.53 ?? 0.17 nM, 0.13 ?? 0.03 nM, and 5.8 ?? 1.6 nM for human IBAT, mouse IBAT, and canine IBAT.

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