Cation channel

EIPA (L593754) is a TRPP3 channel inhibitor (IC50=10.5 μM) and an inhibitor of Na+ H+ exchange (NHE). EIPA inhibits megacytosis, promotes autophagy, and can be used in inflammation and tumor studies.

D-GsMTx4 TFA, a selective spider venom peptide, is a TRPC1 6 and Piezo2 inhibitor that inhibits cation-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families, blocks cation-selective stretch-activated channels (SACs), and attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglia reactivity. toxicity and microglia reactivity.D-GsMTx4 TFA prevented myocardial infarction in a mouse model of ischemia reperfusion and can be used to characterize the role of excitatory MSCs in normal physiology and pathology.

GsMTx4 TFA (1209500-46-8 free base) is a spider venom peptide that selectively inhibits cation permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families.

Broad spectrum cation channel blocker .This compound is unstable in powder form and other related salt forms are recommended.

Pinokalant (LOE-908) is a novel non-selective cation channel inhibitor.Pinokalant significantly reduces cortical infarct volume in in vivo experiments, improves the metabolic and electrophysiological status of the ischemic penumbra region, and reduces the size of the lesion on magnetic resonance images in the acute phase after middle cerebral artery occlusion in rats.Pinokalant is a potential SARS-CoV-2 protease inhibitor for the study of stroke.

Aspartame (SC-18862), an artificial, non-carbohydrate sweetener, is aspartyl-phenylalanine-1-methyl ester.

Prazosin hydrochloride (Vasoflex) reduces peripheral resistance and relaxes vascular smooth muscles as a selective adrenergic alpha-1 antagonist by a mechanism not completely known. Prazosin hydrochloride is a synthetic piperazine derivative with hypotensive antiadrenergic properties, It is used in the treatment of heart failure, hypertension, pheochromocytoma, Raynaud's syndrome, prostatic hypertrophy, and urinary retention.

Cytidine 5'-triphosphate disodium salt is one of the endogenous metabolites and is a cation-permeable ligand-gated ion channel agonist.

Tetraethylammonium chloride is a quaternary ammonium compound. It is a non-selective potassium channel blocker. It is a good substrate for organic cation transporter proteins and has antitumor properties.

(E)-Cardamonin (Alpinetin chalcone) is a chalconoid that has been isolated from several plants including Alpinia katsumadai and Alpinia conchigera. It is a novel antagonist of hTRPA1 cation channel with an IC50 of 454 nM. It has received growing attention from the scientific community due to the expectations toward its benefits to human health.

RN-1747 is a selective transient receptor potential cation channel subfamily V member 4 agonist (EC50: hTRPV4 of 0.77 μM, mTRPV4 of 4.0 μM, and rTRPV4 of 4.1 μM) and also acts as an antagonist for TRPM8 (IC50: 4 μM).

TRV120027 TFA is a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R) and engages ß-arrestins while blocking G-protein signaling.

Adenosine 5'-diphosphoribose sodium (ADP ribose sodium) is a metabolite of nicotinamide adenine nucleotide (NAD+), which is widely present in organisms.Adenosine 5'-diphosphoribose sodium (ADP ribose sodium) is a potent intracellular Ca2+-permeable cation TRPM2 channel activator. Adenosine 5'-diphosphoribose sodium (ADP ribose sodium) is a potent intracellular Ca2+ permeable cation TRPM2 channel activator that also induces autophagy.)

AS1269574 (AS 1269574) is a potent, orally available GPR119 agonist with potential for type 2 diabetes research.

A-784168, a potent and orally active inhibitor of vanilloid receptor type 1 (TRPV1), acts on a ligand-gated nonselective cation channel pivotal in integrating pain stimuli including endogenous lipids, capsaicin, heat, and low pH. It demonstrates commendable central nervous system (CNS) penetration upon oral administration [1].

9-Phenanthrol is inhibitor of the transient receptor potential melastatin 4 (TRPM) channel, a Ca2+ -activated non-selective cation channel.

Mesendogen is an inhibitor of TRPM6. Mesendogen alters magnesium homeostasis, promotes mesoderm and definitive endoderm differentiation.

Gramicidin A is a peptide antibiotic isolated from B. brevis.Gramicidin A is a highly hydrophobic channel-forming ion carrier that forms monovalent cation-permeable channels in artificial membranes.Gramicidin A induces the degradation of hypoxia-inducible factor 1 alpha (HIF-1 alpha) and reduces the growth of a mouse xenograft model of human renal cell carcinoma. Gramicidin A has antibacterial, antimalarial and hemolytic activities.

PDDHV is a resiniferatoxin-type phorboid vanilloid with capsaicin-like selectivity for the cloned rat transient receptor potential cation channel subfamily V member 1 (TRPV1), formerly known as vanilloid receptor 1. It induces Ca2+-uptake by rat dorsal root ganglion neurons with an EC50 value of 70 nM.

TRPC6-IN-3 (compound 17) is an orally active inhibitor of the transient receptor potential C6 ion channel (TRPC6), which regulates intracellular calcium concentration and modulates the flux of cations, including calcium and sodium ions, thereby affecting membrane potential.

AZ12099548 is a transient receptor potential cation channel subfamily V member 1 (TRPV1) antagonist.

SOR-C13 is an inhibitor of transient receptor potential cation channel vanilloid family member 6 (TRPV6, CaT1 or CATL) with potential antineoplastic activity. TRPV6 calcium channel inhibitor SOR-C13 binds to TRPV6 and prevents the influx of calcium ions into TRPV6-expressing tumor cells. This inhibits the activation of nuclear factor of activated T-cell (NFAT) transcription complex which may result in an inhibition of calcium-dependent cancer cell proliferation and an induction of apoptosis in tumor cells overexpressing TRPV6.

CALP1 TFA, a calmodulin (CaM) agonist with a dissociation constant (Kd) of 88 µM, selectively binds to the CaM EF-hand Ca2+-binding site, inhibiting calcium channel opening. This action blocks calcium influx and apoptosis with an IC50 of 44.78 µM, modulates glutamate receptor channel activity, and impedes a store-operated nonselective cation channel. Additionally, CALP1 TFA enhances CaM-dependent phosphodiesterase activity, denoting its multifaceted role in modulating cellular calcium dynamics [1] [2] [3] [4].

Sp-8-Br-cGMPS, an analogue of cGMP, acts as an agonist for cGMP gated cation channels (CNG channels) with an EC50 of 106.5 μM. While Sp-8-Br-cGMPS can induce currents, it does not stabilize channel open states as effectively as a full agonist.