Ion Channels & Transporters

1-EBIO

CAS 10045-45-1

1-EBIO is an Epithelial KCa channel activator. Promotes ESC differentiation into cardiomyocytes.

ML365

CAS 947914-18-3

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).ML365 possesses more than 60-fold selectivity for inhibition of TASK1 over a closely-related,…

ASP 7663

CAS 1190217-35-6

ASP7663 is an orally active and selective TRPA1 agonist. ASP7663 exerts both anti-constipation and anti-abdominal pain actions[1][2].

Brivaracetam

CAS 357336-20-0

Brivaracetam(UCB-34714) is a 4-substituted pyrrolidone butanamide as agent with significant antiepileptic activity; high affinity SV2A ligand and also shows an ability to inhibit Na+ channels. in vitro: Brivaracetam has been tested in a comprehensive safety…

Sematilide hydrochloride

CAS 101526-62-9

Sematilide hydrochloride (CK-1752 hydrochloride) is a selective IKr channel blocker. Sematilide causes a concentration-dependent inhibition of the delayed rectifier K+ current (IC50=25 μM). Sematilide is a class III antiarrhythmic agent[1].

cardamonin

CAS 19309-14-9

Cardamonin is a novel antagonist of hTRPA1 cation channel with an IC50 of 454 nM

ml335

CAS 825658-06-8

ML335 is a selective activator of both TREK-1 and TREK-2.

PNU120596

CAS 501925-31-1

PNU-120596 (NSC 216666 ) is a potent and selective positive allosteric α7 nAChR modulator with an EC50 of 0.2 μM.

Tariquidar (XR9576)

CAS 206873-63-4

Description of Tariquidar: Tariquidar is a P-glycoprotein inhibitor undergoing research as an adjuvant against multidrug resistance in cancer. Tariquidar non-competitively binds to the p-glycoprotein transporter, thereby inhibiting transmembrane transport of…

Zamicastat

CAS 1080028-80-3

Zamicastat is a concentration-dependent dual P-gp and BCRP inhibitor with IC50 values of 73.8±7.2 μM and 17.0±2.7 μM, respectively.

Lercanidipine HCl

CAS 132866-11-6

Lercanidipine hydrochloride is a calcium channel blocker of the dihydropyridine class.Lercanidipine is a calcium channel blocker of the dihydropyridine class, which works by relaxing and opening the blood vessels allowing the blood to circulate more freely…

Rebeprazole sodium

CAS 117976-90-6

Rabeprazole sodium(LY307640 sodium) is an antiulcer drug in the class of proton pump inhibitors.Rabeprazole belongs to a class of antisecretory compounds (substituted benzimidazole proton-pump inhibitors) that do not exhibit anticholinergic or histamine…

Ranolazine HCl

CAS 95635-56-6

Ranolazine(RS-43285) is an antianginal agent with antiarrhythmic properties that achieves its effects via a novel mechanism of action (inhibition of the late phase of the inward sodium current), without affecting heart rate or blood pressure (BP).Ranolazine…

NUCC-0200590

CAS 1060461-67-7

NUCC-0200590 is a small-molecule inhibitor of the TRIP8b-HCN interaction with IC50 of 7.0 uM in AlphaScreen assays, effectively disrupts the TRIP8b-HCN interaction in vitro and in vivo.

NMDAR/TRPM4 inhibitor 8

CAS 1353979-43-7

NMDAR/TRPM4 inhibitor 8 (Compound 8) is a neuroprotective NMDAR-TRPM4 interaction interface inhibitor but spare the critical healthy NMDAR function.

Gabapentin

CAS 60142-96-3

Gabapentin (Neurontin) is a pharmaceutical drug, specifically a GABA analog. It was originally developed to treat epilepsy, and currently is also used to relieve neuropathic pain.

Ropivacaine HCL

CAS 132112-35-7

Ropivacaine HCl is an anaesthetic agent and blocks impulse conduction in nerve fibres through inhibiting sodium ion influx reversibly.Ropivacaine is a new long-acting local anesthetic, with vasoconstrictive properties. Ropivacaine given epidurally provided…

Ganaxolone

CAS 38398-32-2

Ganaxolone, also known as CCD 1042 and C1042, is a CNS-selective GABAA modulator that acts on well-characterized targets in the brain known to have anxiolytic and anticonvulsant effects. Ganaxolone protects against seizures in diverse animal models, including…

4BP-TQS

CAS 360791-49-7

Potent Allosteric Agonist-Positive Allosteric Modulator of α7 Nicotinic Acetylcholine Receptors

VX-150

CAS 1793080-72-4

VX-150 is an orally active, highly selective NaV1.8 inhibitor. VX-150 has the potential for various pain indications research[1].

Allopregnanolone

CAS 516-54-1

Allopregnanolone is a progesterone metabolite. Allopregnanolone is an allosteric modulator of the GABA receptor.

T-Type calcium channel inhibitor(TTA-P2)

CAS 1072018-68-8

T-Type calcium channel inhibitor is a potent inhibitor of T-Type calcium channel. T-Type calcium channel inhibitor penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished…

KM822

KM822 is avselective, noncompetitive modulator of human dopamine transporter (DAT) with IC50 3.7 μM, which shows 30 and 50 folds higher than for human norepinephrine transporter (hNET) and human serotonin transporter (SERT), respectively.

TRPC6 activator compound 2

CAS 931591-94-5

TRPC6 activator compound 2 is selective activator of TRPC6 that does not potentiate TRPC3 and mTRPC7. Comp2 is able to cross BBB.

Nimodipine

CAS 66085-59-4

Nimodipine(Nimotop) is a dihydropyridine derivative and an analogue of the calcium channel blocker nifedipine, with antihypertensive activity.Nimodipine decreases intracellular free Ca2+,Beclin-1 and autophagy.Nimodipine is main use is in the prevention of…

Trpm2 Inhibitor A23

CAS 2765256-12-8

Novel selective inhibitor of the transient receptor potential melastatin 2 (TRPM2) channel, exhibiting TRPM2 selectivity over TRPM8 and TRPV1 channels as well as phospholipase A2 and showing neuroprotective activity in vitro, and significantly reducing ce

Elacridar hydrochloride

CAS 143851-98-3

Elacridar Hcl (GF120918; GW0918) is a P-glycoprotein inhibitor, and has been used both in vitro and in vivo as a tool inhibitor of P-glycoprotein (Pgp) to investigate the role of transporters in the disposition of various test molecules.IC50 value:Target:…

CLC-2-IN AK42

CAS 2408824-56-4

CLC-2-IN-AK42 (CLC-2 inhibitor AK42, AK42) is a potent, specific small-molecule inhibitor of voltage-gated chloride channel CLC-2 with IC50 of 17 nM (human CLC-2).AK42 displays unprecedented selectivity (>1,000-fold) over CLC-1, the closest CLC-2 homolog, and…

Chlorpromazine HCl

CAS 69-09-0

Chlorpromazine Hydrochloride is an antagonist of the dopamine D2, 5HT2A, potassium channel andsodium channel. Chlorpromazine binds with D2 and 5HT2A with Kis of 363 nM and 8.3 nM, respectively.

Safinamide mesylate

CAS 202825-46-5

Safinamide mesylate mesylate (FCE 26743 mesylate; EMD 1195686 mesylate) is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM)[1]. Safinamide mesylate also blocks sodium channels and modulates…

ML-T531

CAS 791127-70-3

ML-T531 is a potent, selective hERG potassium channel (Kv11.1) activator with EC50 of 3.13 uM; exhibits no potentiation for KCNQ1 and KCNE1, and no noticeable effects on other cardiac channels including Cav1.2, Kir2.1, Nav1.5, and Kv4.3; significantly…

Riluzole

CAS 1744-22-5

Riluzole is an anticonvulsant drug and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.

RN-1734

CAS 946387-07-1

RN-1734 is selective antagonist of the TRPV4 channel, completely antagonizes 4αPDD-mediated activation of TRPV4 with comparable, low micromolar IC50values for all three species (hTRPV4: IC50 = 2.3 μM, mTRPV4: IC50 = 5.9 μM, rTRPV4: IC50 = 3.2 μM).IC50 value:…

Triamterene

CAS 396-01-0

Triamterene blocks epithelial Na+ channel (ENaC) in a voltage-dependent manner, which used as a mild diuretic.Triamterene blocked rENaC in a voltage-dependent manner, and was 100-fold less potent than amiloride at pH 7.5. At -90 mV and -40 mV, the IC50 values…

NAB-14

CAS 1237541-73-9

NAB-14 is a potent, selective negative allosteric modulator of GluN2C/2D-containing NMDA receptors with IC50 of 580 nM, >800-fold selective over GluN2A/GluN2 receptors; inhibits triheteromeric (GluN1/GluN2A/GluN2C) NMDARs with modestly reduced potency and…

MsbA inhibitor 1

CAS 52535-76-9

MsbA inhibitor 1 is a novel small molecule lipopolysaccharide biogenesis inhibitor, inhibits MsbA, an ATP-dependent flippase that translocates LPS across the inner membrane; causes mislocalization of LPS to the cell interior, inhibits Δ5 strain with MIC of…

STOML3 inhibitor OB-1

CAS 300803-69-4

A small-molecule inhibitor of STOML3 oligomerization that reverses pathological mechanical hypersensitivity in vivo; effectively inhibits the self-association of stomatin, STOML1 and STOML2 at 2 uM, but not podocin; reversibly reduces the sensitivity of…

VU0606170

CAS 879054-55-4

VU 0606170 (also referred to as VU0606170) is a selective inhibitor of the sodium-activated potassium channel KNa1.1, also known as Slack or Slo2.2. This compound has shown specificity for Slack channels over other related potassium channels, making it a…

3-Guanidinopropionic acid

CAS 353-09-3

RGX-202 is an oral small-molecule SLC6A8 transporter inhibitor. RGX-202 robustly inhibits creatine import in vitro and in vivo, reduces intracellular phosphocreatine and ATP levels, and induces tumor apoptosis. RGX-202 can be used for the research of…

UK-5099

CAS 56396-35-1

UK-5099 is a potent inhibitor of the mitochondrial pyruvate carrier (MPC). UK-5099 ihibits pyruvate-dependent O2 consumption with an IC50 of 50 nM.

ETH 2120(Sodium ionophore III)

CAS 81686-22-8

Sodium ionophore III (ETH2120) is a Na+ ionophore suitable for the assay of sodium activity in blood, plasma, serum. etc.

Nigericin sodium salt

CAS 28643-80-3

Nigericin sodium salt is an antibiotic from Streptomyces hygroscopicus that works by acting as an H+, K+, and Pb2+ ionophore.

Vanoxerine dihydrochloride

CAS 67469-78-7

Vanoxerine dihydrochloride is a potent and selective dopamine reuptake inhibitor.

GBR 12935 (free base)

CAS 76778-22-8

GBR 12935 is a potent, and selective dopamine reuptake inhibitor.

Ivacaftor-d9

CAS 1413431-07-8

Ivacaftor-D9 (CTP-656) is a potent CFTR modulator and exhibits an EC50 value of 255 nM for CFTR potentiation in G551D/F508del HBE Cells. Ivacaftor-D9 acts as an orally active and improved deuterated Ivacaftor analog for cystic fibrosis research.

Naspm trihydrochloride

CAS 1049731-36-3

Naspm is a selective antagonist of Ca2+-permeable AMPA receptors, blocks GluR2-lacking AMPARs, suppresses current responses induced by kainate in type II neurons with IC50 of 0.33 uM; greatly reduces the late rise in intracellular free Zn(2+) in postischemic…

MK-571 sodium salt

CAS 115103-85-0

MK-571 sodium salt (L-660711) is a selective, orally active antagonist of leukotriene D4 receptor. It is also an inhibitor of multidrug resistance-associated protein MRP4 (ABCC4) and ABCC1 (MRP1).

Ifenprodil tartrate (2:1)

CAS 23210-58-4

Ifenprodil tartrate is a novel N-methyl-D-aspartate (NMDA) receptor antagonist that selectively inhibits receptors containing the NR2B subunit.