Membrane Transporters-Ion Channels

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.

SEA0400 is a novel and selective inhibitor of the Na+-Ca2+ exchanger with IC50 of 5-33 nM (inhibiting Na+-dependent Ca2+ uptake in cultured neurons, astrocytes, and microglia).

Empagliflozin is a potent, selective sodium glucose co-transporter-2 inhibitor that is in development for the treatment of type 2 diabetes.

Canagliflozin is an inhibitor of subtype 2 sodium-glucose transport protein (SGLT2).

KPT-330 inhibitor of CRM1 (XPO1)-mediated nuclear export has selective anti-leukaemic activity in preclinical models of T-cell acute lymphoblastic leukaemia and acute myeloid leukaemia.

Amiloride hydrochloride is a Na+ channel blocker, also inhibits TRPP3 channels and Na+/H+ exchanger (NHE).

Amlodipin is L-type calcium channel blocker that displays antihypertensive properties. It inhibits Ca2+-induced contractions in depolarized rat aorta (IC50 = 1.9 nM) and displays vasoprotective effects in cardiovascular disease.

Amlodipine-besylate is L-type calcium channel blocker that displays antihypertensive properties. It inhibits Ca2+-induced contractions in depolarized rat aorta (IC50 = 1.9 nM) and displays vasoprotective effects in cardiovascular disease.

Aniracetam is an ampakine and nootropic of the racetam chemical class purported to be considerably more potent than piracetam.

Apigenin, found in many plants, is a natural product belonging to the flavone class that is the aglycone of several naturally-occurring glycosides. Apigenin acts as a monoamine transporter activator, one of the few chemicals demonstrated to possess this property. Apigenin is a ligand for central benzodiazepine receptors that competitively inhibited the binding of flunitrazepam with a Ki of 4μM, exerting anxiolytic and slight sedative effects.

Artemisinin and its derivatives are a group of drugs that possess the most rapid action of all current drugs against Plasmodium falciparum malaria.

EGT1442 is a potent and selective SGLT2 inhibitor.

Bupivacaine is a more potent inhibitor of cAMP production than are chemically related local anesthetics that are less prone to produce cardiovascular toxicity.

Cilnidipine is a dual blocker of L-type voltage-gated calcium channels in vascular smooth muscle and N-type calcium channels in sympathetic nerve terminals that supply.

Diethylstilbestrol is a synthetic nonsteroidal estrogen that was first synthesized in 1938. It is also classified as an endocrine disruptor.

Diltiazem is a nondihydropyridine (non-DHP) member of the class of drugs known as calcium channel blockers, used in the treatment of hypertension, angina pectoris, and some types of arrhythmia.

Esomeprazole sodium is a proton pump inhibitor which reduces acid secretion through inhibition of the H+ / K+ ATPase in gastric parietal cells.

Evodiamine is a chemical extracted from the Tetradium family of plants. It acts primarily as a thermogenic and stimulant.

Glimepiride is a potent Kir6.2/SUR inhibitor with IC50 of 3.0 nM, 5.4 nM, and 7.3 nM for SUR1, SUR2A and SUR2B, used in the treatment of type 2 diabetes mellitus.

GYKI-52466 dihydrochloride is selective non-competitive AMPA receptor antagonist (IC50 values are 10-20, ~ 450 and >> 50 μM for AMPA- , kainate- and NMDA-induced responses respectively).

Hydralazine hydrochloride is a hydrochloride salt of hydralazine (Apresoline) that is a direct-acting smooth muscle relaxant with an IC50 of 1.9 mM.

Ivermectin is a broad-spectrum antiparasitic avermectin medicine.

Lansoprazole(AG 1749) is a proton pump inhibitor which prevents the stomach from producing acid.

Lidocaine (Alphacaine) is an anasthetic and class Ib antiarrhythmic agent. Blocks voltage-gated sodium channels in the inactivated state.

Lubiprostone is a bicyclic fatty acid metabolite analog of Prostaglandin E1. It activates specific chloride channels in the gastrointestinal tract to stimulate intestinal fluid secretion, and increase gastrointestinal transit.

Luteolin is a PDE4 inhibitor, phosphodiesterase inhibitor, and an interleukin 6 inhibitor, affecting xylazine/ketamine-induced anesthesia in mice. Luteolin acts as a monoamine transporter activator, and is one of the few chemicals demonstrated to possess this property.

Manidipine is a dihydropyridine compound and calcium channel protein inhibitor and antagonist.

Minoxidil (U-10858) is a selective ATP dependent K+ (Kir6) channel activator.

Nateglinide(Starlix) is an insulin secretagog agent that lowers blood glucose levels by stimulating insulin secretion from the pancreas.

Nicorandil (SG-75) is potassium channel activator.

Nifedipine is a L-type calcium channel blocker.

Nisoldipine(BAY-k 5552; Sular) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC50 of 10 nM.

Omeprazole is a cell-permeable, selective proton pump inhibitor.

Oridonin (Isodonol), an entkaurane diterpenoid isolated from Rabdosia rubescens, is an important traditional Chinese herbal remedy.

Phenytoin is a sodium channel protein inhibitor.

Phenytoin sodium (Dilantin) is a sodium channel protein inhibitor.

Repaglinide is a potent short-acting insulin secretagogue that acts by closing ATP-sensitive potassium (KATP) channels in the plasma membrane of the pancreatic beta cell.

Riluzole preferentially blocks TTX-sensitive sodium channels, which are associated with damaged neurons.This reduces influx of calcium ions and indirectly prevents stimulation of glutamate receptors.

Sodium orthovanadate is the chemical compound Na3VO4. It is an inhibitor of protein tyrosine phosphatases, alkaline phosphatases and a number of ATPases, most likely acting as a phosphate analogue.

Tetrandrine is a calcium channel blocker. It inhibits the degranulation of mast cells.Tetrandrine has anti-inflammatory and anti-fibrogenic actions, which make tetrandrine and related compounds potentially useful in the treatment of lung silicosis, liver cirrhosis, and rheumatoid arthritis.

PF-04971729 is a potent and selective inhibitor of the sodium-dependent glucose cotransporter 2.

Verapamil is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor.

Felodipine is a 1,4-dihydropyridine antagonist and calcium channel protein inhibitor.

Gliclazide is used as an antidiabetic. It is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. 

BeKm-1 is a HERG (human ether-a-go-go-related gene) blocking compound. BeKm-1 can be used for the research of heart disease.

Sarcosine ethyl ester hydrochloride is a Glycine derivative.

Desipramine hydrochloride is a tricyclic antidepressant that is a selective inhibitor of noradrenalin transporters (K_i values are 4, 61 and 78720 nM for NET, SERT and DAT transporters respectively).

AER-271, a phosphonate prodrug derivative of AER-270, is an aquaporin-4 (AQP4) inhibitor for the research of acute ischemic stroke.

M8-B is an antagonist of transient receptor potential melastatin 8 (TRPM8) that blocks activation by cold, icilin (Item No. 10137), or menthol in vitro (IC50s = 7.8, 26.9, and 64.3 nM, respectively).