Membrane Transporter/Ion Channel

UCCF-853 is a CFTR modulator.

AVE1231 (A293) is a dual-pore potassium channel TASK-1 inhibitor with antiarrthmic activity.

(1S,2S)-ML-SI3 is a trans-isomer of ML-SI3 that targets all three isoforms of TRPML.

(rel)-ML-SI3 is one of the active ingredients of ML-SI3 (another component is (cis)-ML-SI3) that targets three isoforms of TRPML.

FFN246 is a fluorescent, dual substrate of serotonin transporter (SERT) probe and vesicular monoamine transporter 2 (VMAT2) with excitation and emission spectra 392/427 nm.

MCT-IN-1 (compound 2) is a potent inhibitor of monocarboxylate transporter (MCT), with the IC50 of 9 nM and 14 nM for MCT1 and MCT4, respectively.

nAChR-IN-1 is a tetrametlpiperidine heptanoate, a selective nicotinic acetylcholine receptor (nAChR) inhibitor that inhibits nAChRs lacking α5, α6, or β3 subunits.

bPiDI is a novel selective α6β2 nicotinic receptor antagonist. bPiDI inhibits nicotine-evoked striatal dopamine (DA) release through an interaction with α6β2-containing nAChRs.

Tezacaftor-d4 (VX-661-d4) is the deuterium-labeled Tezacaftor , a F508del CFTR corrector.

hCA/Wnt/β-catenin-IN-1 (Compd 15) is an inhibitor of hCA (Ki: 33.6, 24.1, 6.8 nM for hCA II, hCA IX, hCA XII). hCA/Wnt/β-catenin-IN-1 reduces P-gp activity.

PU-48 is a potent urea transporters A (UT-A) inhibitor (IC50=0.32 μM).

h-NTPDase-IN-4 (compound 4c) is a pan-inhibitor of NTPDase with IC50s of 3.58 μM (h-NTPDase1), 10.21 μM (h-NTPDase2), 0.13 μM (h-NTPDase3), 13.57 μM (h- NTPDase8).

XPC-7724 is a selective Nav1.6 channel inhibitor with a IC50 value of 0.078 μM.

LTGO-33 is a potent and selective voltage-gated sodium channel NaV1.8 inhibitor.

(S)-LTGO-33 is a small molecule inhibitor of voltage-gated sodium channel NaV1.8.

CVN293 is a selective and brain permeable potassium ion (K+) channel KCNK13 inhibtor with IC50s of 41 nM and 28 nM for hKCNK13 and mKCNK13, respectively.

Glutor is a selective GLUT 1/2/3 inhibitor that can suppress glucose uptake.

Remacemide (FPL 12924) is an orally active, non-competitive, low-affinity NMDA receptor antagonist.

RN-1665 is an orally active TRPV4 antagonist that exhibits excellent selectivity for related TRP receptors such as TRPV1, TRPV3 and TRPM8.

KIO-301 chloride is an azobenzene photoswitchable compound that blocks voltage-gated ion channels, including perpolarization-activated cyclic nucleotide gating and voltage-gated potassium channels.

VU0542270 is a selective vascular Kir6.1/SUR2B KATP channel inhibitor with a IC50 value of 100 nM.

NA-014 (40) is a selective EAAT2 positive allosteric modulator (PAM), with an EC50 of 3 nM.

Yaddle1 (compound 34) a novel Piezo1 agonist, and induces Ca2+ influx in human CD4+ T cell.

CPK20 is a potent and highly selective KCNT1 channel blocker, and CPK20 can be used in the study of epilepsy.