calcium-activated

TRPM4-IN-1 (4-chloro-2-(2-(2-chlorophenoxy)acetamido)benzoic acid) is a potent and selective inhibitor of TRPM4 with an IC50 of 1.5 μM.

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).

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.

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.

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.

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.

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).

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.

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.

Bufalin is a natural product and a Na⁺/K⁺-ATPase inhibitor (IC50 ≈ 40–45 nM) with favorable cell permeability. By binding to α subunits such as ATP1A1, bufalin induces calcium overload and pyroptosis, and can be used for experimental research and therapeutic exploration in various cancers.

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

VZMC013 is a potent chemical probe targeting the MOR-CCR5 heterodimer, effectively inhibiting HIV-1 entry exacerbated by opioid compounds. It exhibits nanomolar binding affinity to both MOR and CCR5, inhibits CCL5-activated calcium mobilization, and significantly enhances anti-HIV-1BaL activity compared to previously reported bivalent ligands. In TZM-bl cells co-expressing CCR5 and MOR, VZMC013 demonstrates greater inhibition of viral infection than in cells expressing only CCR5. Additionally, VZMC013 blocks HIV-1 entry into peripheral blood mononuclear cells (PBMC) in a concentration-dependent manner and more effectively inhibits opioid-accelerated HIV-1 entry in phytohemagglutinin-activated PBMC than in opioid-free environments.

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.

Ferroptosisinducer-7 is an orally active and selective inducer of ferroptosis, operating through the inositol 1,4,5-trisphosphate receptor (IP3R)/ORAI calcium release-activated calcium channel protein. This compound significantly alleviates anemia, inhibits bone marrow CTL activation, and improves hematopoietic function in immune-mediated bone marrow failure. It is utilized in research on aplastic anemia.

D-myo-Inositol-1,3,4-triphosphate (sodium) is one of the inositol polyphosphate isomers involved in signal transduction. It increases intracellular levels of Ins(3,4,5,6)-P4 by inhibiting the activity of Ins(3,4,5,6)-P4 kinase, which in turn suppresses calcium-activated chloride channels. This compound is regulated by cytoplasmic free calcium levels.

Maxi-K modulator 1 (Example 1) is a modulating agent for the large conductance calcium-activated potassium (Maxi-K) channels. It serves as a potent stimulator of Maxi-K channel activity and is applicable in research on Fragile X syndrome.