BAY-876 is the first highly selective GLUT1 inhibitor with IC50 of 0.002 uM. show good metabolic stability in vitro and high oral bioavailability in vivo.

Ancistrotecine B (Compound 2) is a Nav1.7 channel inhibitor (IC50: 0.73 μM). Ancistrotecine B relieves inflammatory pain in mice.

Guvacine hydrobromide, an alkaloid found in the nut of Areca catechu, is a potent GABA uptakp inhibitor. Guvacine hydrobromide inhibits rat GAT-1, rat GAT-2 and rat GAT-3 with IC50 values of 39 μM, 58 μM and 378 μM, respectively.

Arecaidine hydrobromide, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine hydrobromide is a substrate of H+-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake.

KC289 is a specific small-molecule agonist of PIEZO1 channel and Yoda1 analogue with EC50 of 150 nM in in calcium assays.

slCeMM1 is a potent, highly selective inhibitor of lactate transporter SLC16A3 (MCT4), inhibits intracellular lactate accumulation in SLC16A3 dependent cells (IC50=91 nM).

VPC01091.4 is a non-phosphorylatable FTY720 analogue and novel TRPM7 inhibitor, inhibits IM7 in a dose-dependent manner with IC50 of 0.665 uM.

Trpvicin is a potent and subtype-selective inhibitor of TRPV3 with IC50 of 0.41 and 0.22 uM for hTRPV3-WT and hTRPV3-G573S mutant, respectively.

Triphenylphosphine oxide (TPPO) is a selective and potent inhibitor of TRPM5 with IC50 of 12 and 30 uM for human and murine TRPM5 heterologously expressed in HEK293 cells.

SAR7334 (SAR-7334 ) is a highly potent and selective inhibitor of TRPC6 channel, reduces TRPC6-mediated Ca2+ influx with IC50 of 9.5 nM.

M085 (TRPC3/6/7 activator 4o) is a potent and selective TRPC3/6/7 activator with EC50 of 4.66 uM, also activates hTRPC6 with EC50 of 3.8 uM.

Libvatrep (SAF312) is a potent, selective non-competitive inhibitor/antagonist of the transient receptor potential cation channel subfamily V member 1 (TRPV1), shows potential for treatment of ocular surface pain.

KS0365 (KS 0365) is a potent and selective activator of transient receptor potential vanilloid 3 (TRPV3) channel with EC50 of 5.08 uM.

JNc-463 is a small-molecule that could increase the TRPV4-eNOS interaction, enhances vasodilation and exert antihypertensive effects in mice.

GNE551 is a potent, selective, non-covalent agonist of TRPA1 ion channel with EC50 of 254 nM in Ca2+ influx assays.

GDC-6599 is a potent, selective transient receptor potential ankyrin 1 (TRPA1) antagonist with IC50 of 5.3 nM (hTRPA1), exhibits TRPA1 cell potency (IC50=20 nM) in the Ca2+ influx assay in CHO cells.

AZ465 (AZ-465) is a potent selective TRPA1 inhibitor, potently inhibitor Zn2+ (100 μM)- and O-chlorobenzylidene malononitrile (CS) (10 nM)-induced TRPA1 activation with IC50 of 85 nM and 20 nM, respectively.

AMG2504 (AMG 2504) is a selective small molecule TRPA1 inhibitor, inhibits AITC-induced increase in intracellular calcium mediated by TRPA1 in CHO cells with IC50 of 35 nM.

AAL-149 is a non-phosphorylatable FTY720 analogue and novel TRPM7 inhibitor, inhibits IM7 in a dose-dependent manner with IC50 of 1.081 uM, shows potent anti-inflammatory effects in vivo.

XPC-7224 is a potent, selective NaV1.6 inhibitor with IC50 of 78 nM and 130 nM for human and mouse NaV1.6, respectively, interacts with the inactivated state of the channel.

XPC-5462 is a potent, selective dual inhibitor of NaV1.6 and NaV1.2 with IC50 of 10.9 nM and 10.3 nM, respectively.

UTX-143 is a potent, selective sodium-hydrogen exchange subtype 5 (NHE5) inhibitor with IC50 of 3.11 uM, 80-fold selective over NHE1.

DS43260857 is a potent, selective NaV1.7 inhibitor with IC50 of 15 nM (hNaV1.7), shows 440-fold and 930-fold selectivity over hNaV1.1 and hNaV1.5, respectively.

BW-031 iodide is a potent cationic sodium channel inhibitor, inhibited Nav 1.7 (IC50=9.5 uM) and Nav 1.1 channels with approximately sixfold greater potency than QX-314.

BW-031 chloride is a potent cationic sodium channel inhibitor, inhibited Nav 1.7 (IC50=9.5 uM) and Nav 1.1 channels with approximately sixfold greater potency than QX-314.

Benzocaine is a local anesthetic.

Aneratrigine is a sodium channel protein type 9 subunit alpha blocker.

ZVS-08 is a selective inhibitor of the voltage-gated potassium channel KV10.1 with IC50 of 3.7 uM.

VU0935685 is a potent, selective inhibitor of SLACK potassium channels with IC50 of 0.32 uM in in whole-cell, voltage-clamp electrophysiology (EP) assays, demonstrates selectivity versus hERG.

VU0542270 is the first selective inhibitor of vascular Kir6.1/SUR2B KATP channel with IC50 of 129 nM, >300-fold selective over other members of the Kir channel family.