Membrane Transporters-Ion Channels

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  1. Sodium Channel inhibitor

    Sodium Channel inhibitor 1, one of 3-Oxoisoindoline-1-carboxamides, is a novel and selective voltage-gated sodium channel for pain treatment.
  2. P-gp inhibitor

    Zosuquidar is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM.
  3. Na+-glucose transporter inhibitor

    T-1095 is a potent and selective inhibitor of Na+-glucose cotransporters (SGLTs).
  4. elastogenesis inhibitor

    L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor.
  5. CaCCs Inhibitor

    CaCCinh-A01 inhibits CaCC currents in human bronchial and intestinal cells. Also inhibits TMEM16A channels (IC50 = 2.1 uM, in TMEM16A-expressing FRT cells).
  6. TMEM16A Inhibitor

    T16Ainh-A01 is a selective TMEM16A calcium-activated chloride channel inhibitor that strongly inhibits chloride current in salivary gland cells.
  7. ATPase and GTPase inhibitor

    Etidronate Disodium is a bisphosphonate bone resorption inhibitor.
  8. TRPC4/C5 inhibitor

    ML204 is a novel potent antagonist that selectively modulates native TRPC4/C5 ion channels.
  9. 5-HT3 receptor inhibitor

    Eucalyptol is a bicyclic monoterpene that has been found in Eucalyptus and other plants. It is an inhibitor of 5-HT3 receptor ,potassium channel, TNF-α and IL-1β.
  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. MCT Inhibitor?€?

    7ACC1 selectively interfere with lactate fluxes in the lactate-rich tumor microenvironment; inhibits lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters.
  12. Ferroptosis inhibitor

    RSL3 is a ferroptosis activator in a VDAC-independent manner,exhibiting selectivity for tumor cells bearing oncogenic RAS.
  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. MSCs Inhibitor

    GsMTX4 is a 34 amino acid peptidyl toxin isolated from the Grammostola rosea (Chilean rose) tarantula venom and belongs to the huwentoxin-1 family.
  19. voltage-gated sodium channel inhibitor

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

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

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

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

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

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

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

    AmbroxolHCl is a potent inhibitor of the neuronal Na+ channels, inhibits TTX-resistant Na+ currents with IC50 of 35.2 uM and 22.5 μM for tonic and phasic block, inhibits TTX-sensitive Na+ currents with IC50 of 100 μM. Phase 3.
  31. proton pump inhibitor

    (R)-Lansoprazole is a proton pump inhibitor which prevents the stomach from producing acid.
  32. 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.
  33. 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.
  34. 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.
  35. SGLT2 inhibitor

    Canagliflozin hemihydrate is the hemihydrate form of canagliflozin, which is a SGLT2 inhibitor with IC50 of 2.2 nM for hSGLT2 in a cell-free assay, exhibits 413-fold selectivity over hSGLT1.
  36. 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).
  37. CRAC channel inhibitor

    GSK-7975A is a potent and orally available CRAC channel inhibitor.
  38. 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.
  39. Pgp1 inhibitor

    NSC 23925 is a plasma membrane glycoprotein 1 (Pgp1) inhibitor to reverse multidrug resistance (MDR1).
  40. NHE-1 inhibitor

    Rimeporide (EMD-87580) is a potent and selective inhibitor of the Na+/H+ exchanger (NHE-1).
  41. BCRP/ABCG2 inhibitor

    YHO-13177 is a potent and specific inhibitor of breast cancer resistance protein (BCRP/ABCG2).
  42. exportin-1 inhibitor

    Eltanexor, also known as KPT-8602, is a second-generation exportin-1 inhibitor.
  43. TRPC6 inhibitor

    SAR7334 is a novel, highly potent and bioavailable inhibitor of TRPC6 channels that opens new opportunities for the investigation of TRPC channel function in vivo. SAR7334 inhibited TRPC6, TRPC3 and TRPC7-mediated Ca(2+) influx into cells with IC50 s of 9.5, 282 and 226 nM, whereas TRPC4 and TRPC5-mediated Ca(2+) entry was not affected.
  44. proton pump inhibitor

    Ilaprazole (IY-81149) is a proton pump inhibitor; inhibits H+/K+-ATPase with an IC50 of 6.0 μM.
  45. H(+)-K(+)-exchanging ATPase inhibitor

    Rabeprazole is an inhibitor of H(+)-K(+)-exchanging atpase in gastric parietal cells.
  46. serotonin uptake inhibitor

    Paroxetine Mesylate is a serotonin uptake inhibitor that is effective in the treatment of depression.
  47. 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.
  48. 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.
  49. 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.
  50. 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.

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