calcium-activated

Ethosuximide (Zarontin) is an anticonvulsant, blocks the low voltage-activated T-type calcium channel used in the treatment of absence seizures unaccompanied by other types of seizures.

Flufenamic acid (Arlef) is an anthranilic acid derivative with analgesic, anti-inflammatory, and antipyretic properties. It is used in musculoskeletal and joint disorders and administered by mouth and topically.

Tanshinone IIA sulfonate sodium (Tanshinone IIA sodium sulfonate) is a water-soluble derivative of tanshinone IIA extracted from Savia miltiorrhiza; a potent negative allosteric modulator of the human purinergic receptor P2X7. Tanshinone IIA sulfonate sodium (12.5 μM) inhibits hypoxia-induced PKG and PPAR-γ downregulation in PASMCs and distal pulmonary arteries of rats.

Tetrandrine (Sinomenine A) is a naturally occurring biphenylisoquinoline alkaloid, a calcium channel inhibitor. Tetrandrine inhibits voltage-gated calcium channels (ICa) and Ca2+-activated potassium channels.

Synta66 is a store-operated calcium entry channel Orai inhibitor, and used for the research of neurological disease.

T16Ainh-A01 is a potent inhibitor of TMEM16A Chloride channel, inhibiting TMEM16A-mediated chloride currents (IC50 of 1 µM),and functions as a calcium-activated chloride channel (CaCC).

Dihydrocapsaicin (CCRIS1589) is isolated from Capsicum fruit. Capsaicin is the primary active component of the heat and pain-eliciting lipid soluble fraction of the Capsicum pepper. Like capsaicin, dihydrocapsaicin is an irritant. Capsaicin is found in natural hot pepper extracts along with a number of impurities, including dihydrocapsaicin and several lesser impurities. Separation by HPLC is required in order to obtain pure dihydrocapsaicin. Dihydrocapsaicin represents about 10% of the compound present in commercial preparations purporting to be pure capsaicin, but it has about the same pungency as capsaicin. VR1 (vanilloid receptor 1) is a heat activated calcium ion channel which functions as a part of the normal nociceptive pain pathway. Capsaicin elicits a sensation of burning pain by activation of VR1 on small, non-myelinated polymodal C-type nociceptive nerve fibers. The potency of dihydrocapsaicin at VR1 appears equivalent to capsaicin. Antioxidant. Reduces oxidation of serum lipids. Mutagenic. Dihydrocapsaicin is an activator of VR1.

SKF-96365 hydrochloride (SKF96365) , a SOCE inhibitor, exhibits potent anti-neoplastic activity by inducing cell-cycle arrest and apoptosis in colorectal Y cells. SKF-96365 hydrochloride can induce cytoprotective autophagy to delay apoptosis by preventing the release of cytochrome c (cyt c) from the mitochondria into the cytoplasm. Mechanistically, SKF-96365 hydrochloride treatment inhibited the calcium calmodulin-dependent protein kinase IIγ (CaMKIIγ) AKT signaling cascade in vitro and in vivo. Overexpression of CaMKIIγ or AKT abolished the effects of SKF-96365 on Y cells, suggesting a critical role of the CaMKIIγ AKT signaling pathway in SFK-96365-induced biological effects. SKF-96365 hydrochloride inhibited hERG current in a concentration-dependent manner.

N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is a broad-spectrum Phospholipase A2 (PLA2) inhibitor and a TRP channel blocker.

CRAC intermediate 1 is a key intermediate used in the synthesis of the CRAC ion channel series of compounds, details from patent WO 2010122089.

CRAC intermediate 2 is used as an intermediate compound in the synthesis of CRAC inhibitors.

Flindokalner (BMS-204352) is a potassium channel modulator and a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. It is also a positive modulator of large conductance calcium-activated K channels (BKca) and displays negative modulatory activity at Kv7.1 channels (Ki = 3.7 μM). Additionally, Flindokalner acts as a negative modulator of GABAA receptors and demonstrates anxiolytic efficacy in vivo.

CaCCinh-A01 is an inhibitor of the calcium-activated chloride channel (CaCC, 10 μM) and TMEM16A (IC50: 2.1 μM).

Talniflumate (Somalgen) is a calcium-activated chloride channel (hCLCA1 mCLCA3) blocker that reduces mucin synthesis and releases in animal models and cell culture. It possesses anti-inflammatory actions via inhibition of Cox (cyclooxygenase) and inhibits Cl- HCO3- exchange activity. It also increases survival in a cystic fibrosis mouse model of the distal intestinal obstructive syndrome.

Rimtuzalcap (CAD-1883) (CAD-1883), a pioneering selective positive allosteric modulator of small-conductance calcium-activated potassium channels (SK channels), is employed in the study of movement disorders such as spinocerebellar ataxia (SCA) and essential tremor (ET).

Benzthiazide (Lemazide) is used in the therapy of edema and hypertension. Like other thiazides, benzthiazide accelerates water loss from the body (diuretics). They inhibit Na+ Cl- reabsorption from the distal convoluted tubules in the kidneys. Thiazides also cause loss of potassium and an increase in serum uric acid. Thiazides are often used to treat hypertension, but their hypotensive effects are not necessarily due to their diuretic activity. Thiazides have been shown to prevent hypertension-related morbidity and mortality although the mechanism is not fully understood. Thiazides cause vasodilation by activating calcium-activated potassium channels (large conductance) in vascular smooth muscles and inhibiting various carbonic anhydrases in vascular tissue.

GSK-7975A is a potent, orally available inhibitor of the Calcium Release-Activated Calcium (CRAC) channel.

NS13001 (N-(4-Chlorophenyl)-2-(3,5-dimethyl-1H-pyrazol-1-yl)-9-methyl-9H-purin-6-amine) is a potent, selective, orally active allosteric positive modulator of SK channels (small conductance calcium-activated potassium channels). The EC50s are 1.8 and 0.14 μM for SK2 and SK3, respectively. NS13001 holds promise as a potential therapeutic agent for treatment of spinocerebellar ataxia type 2 (SCA2) and possibly other cerebellar ataxias.

Tetrahydropalmatine is a compound that inhibits voltage-activated L-type calcium channels and active potassium channels.

Calcium influx inducer compound 634 is an agent that stimulates calcium entry. At a concentration of 10 µM, it can enhance the release of extracellular vesicles (EVs) from mouse bone marrow-derived dendritic cells (mBMDCs). Furthermore, Calcium influx inducer compound 634 (10 µM) increases the levels of surface CD86 and CD80 on mBMDCs, an effect that can be blocked by the calcium release-activated calcium channel inhibitor YM-58483.

ANO1-IN-4 (Compound 10bm) is a reversible inhibitor of the calcium-activated chloride channel transmembrane protein 16A (TMEM16A, also known as ANO1), with an IC50 of 0.030 µM. It demonstrates good metabolic stability in rat liver microsomes and can inhibit spontaneous contractions in isolated mouse ileum.

Crofelemer (Provir) is an orally active antidiarrheal agent. It targets the cystic fibrosis transmembrane conductance regulator (CFTR) and calcium-activated chloride channels (CACC), which are responsible for chloride and fluid secretion in the gastrointestinal tract. Crofelemer is applicable for research in diarrhea-related conditions.

BKCa activator-1 (Compound 51b) is an orally active activator of BKCa calcium-activated potassium channels with an EC50 of 2.82 μM. It promotes K+ efflux, leading to cell membrane hyperpolarization and inhibition of smooth muscle contraction. In a spontaneous hypertensive rat (SHR) model, it alleviates urinary incontinence and exhibits antitussive effects in a guinea pig cough model.

8-CPT-2Me-cAMP sodium is a sodium salt compound that selectively activates exchange proteins activated by cAMP (Epac), which are cAMP-sensitive guanine nucleotide exchange factors (GEFs) responsible for activating small GTPases Rap1 and Rap2. It specifically activates Epac1 with an EC50 value of 2.2 μM, while showing no activation of PKA with an EC50 value greater than 10 μM [1]. Additionally, 8-CPT-2Me-cAMP sodium stimulates the Epac-mediated release of calcium ions (Ca2+) in vitro in pancreatic β-cells [2].