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UCL 1684 (dibromide) is a first nanomolar, non-peptidic small conductance calcium-activated potassium (SK) channel blocker. UCL 1684 (dibromide) is effective in preventing the development of atrial fibrillation due to potent atrial-selective inhibition of INa. UCL 1684 (dibromide) causes atrial-selective prolongation of ERP secondary to induction of postrepolarization refractoriness .
Rimtuzalcap (CAD-1883) is a first-in-class selective positive allosteric modulator of small-conductance calcium-activated potassium channels (SK channels). Rimtuzalcap can be used for the research of movement disorders including essential tremor (ET) and spinocerebellar ataxia (SCA) .
Slotoxin, a peptide from Centruroides noxius Hoffmann scorpion venom, blocks high conductance calcium-activatedpotassium channel, with Kd of 1.5 nM[1].
Kobusin is a bisepoxylignan isolated from the Pnonobio biondii Pamp. Kobusin is an activator of CFTR and CaCCgie chloride channels and a inhibitor of ANO1/CaCC (calcium-activated chloride channel) channel .
DFBTA is an orally active, potent and little brain penetrated ANO1 (Calcium-activated chloride channel anoctamin-1) inhibitor, with an IC50 of 24 nM. DFBTA shows analgesic efficacy for inflammatory pain .
Kaliotoxin is a peptidyl inhibitor of neuronal BK-Type. Kaliotoxin can specific inhibit Kv channels and calcium-activated potassium channels. Kaliotoxin can be used for the research of the regulation of membrane potential and neuron excitability .
Noxiustoxin is a toxin from the venom of the Mexican scorpion Centruroides noxius which block voltage-dependent potassium channel (Kv1.3, IC50 = 360 nM), and calcium-activatedpotassium channel. Noxiustoxin plays an important role in neuroinflammatory disease .
E 64c is a derivative of naturally occurring epoxide inhibitor of cysteine proteases, a Calcium-activated neutral protease (CANP) inhibitor and a very weak irreversible cathepsin C inhibitor. E 64c exhibits entry-blocking effect for MERS-CoV.
N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is a broad spectrum Phospholipase A2 (PLA2) inhibitor and TRP channel blocker . N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is also an effective reversible inhibitor of calcium-activated chloride channels, has potential to treat arrhythmia .
T16Ainh-A01, an aminophenylthiazole, is a potent transmembrane protein 16A (TMEM16A) inhibitor, inhibiting TMEM16A-mediated chloride currents with an IC50 value of ~1 µM. TMEM16A (ANO1) functions as a calcium-activated chloride channel (CaCC) .
Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect .
Yoda 1 is a potent and selective Piezo1 agonist. Yoda 1 activates purified Piezo1 channels. Yoda 1 potently inhibits macropinocytosis induced by epidermal growth factor (EGF). Yoda 1 enhances Ca 2+ influx followed by activation of the calcium-activated potassium channel KCa3.1 and inhibition of Rac1activation .
Hydrochlorothiazid-d2 is the deuterium labeled Hydrochlorothiazide. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect[1][2][3].
NS13001 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 .
Hydrochlorothiazide (Standard) is the analytical standard of Hydrochlorothiazide. This product is intended for research and analytical applications. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect .
Hydrochlorothiazide- 13C6 is the 13C labeled Hydrochlorothiazide[1]. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect[2][3][4].
Hydrochlorothiazid- 13C,d2 is the 13C- and deuterium labeled Hydrochlorothiazide. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect[1][2][3].
Niflumic acid is a calcium-activatedchloride channel blocker and COX-2 inhibitor with the IC50 value of 100 nM. Niflumic acid induces apoptosis through caspase-8/Bid/Bax pathway in lung cancer cells. Niflumic acide exhibits anti-tumor activity by affecting the expression of ERK1/2 and the activity of MMP2 and MMP9. Niflumic acid has orally bioactivity. Niflumic acid acts on rheumatoid arthritis .
Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo .
Hydrochlorothiazide- 15N2, 13C,d2 is 15N and deuterated labeled Hydrochlorothiazide (HY-B0252). Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect .
Spiperone hydrochloride (Spiroperidol hydrochloride) is a selective dopamine D2 receptor (Ki values of 0.06 nM, 0.6 nM, 0.08 nM, ~350 nM, ~3500 nM for D2, D3, D4, D1 and D5 receptors, respectively) and 5-HT2A/5-HT1A receptor (Kis of 1 nM/49 nM) antagonist. Spiperone hydrochloride is also a selective α1B-adrenoceptor antagonist. Spiperone hydrochloride activatescalcium-activated chloride channel (CaCC). Antipsychotic and anti-inflammatory activities .
TRPM4-IN-1 (CBA) is a potent and selective inhibitor of the cation channel TRPM4, with an IC50 of 1.5 μM. TRPM4-IN-1 can be used for the research of cardiac diseases and prostate cancer .
Potassium channels are the most widely distributed type of ion channel and are found in virtually all living organisms. There are four major classes of K channels: voltage-gated potassium channel, calcium-activated potassium channel, inwardly rectifying potassium channel and tandem pore domain potassium channel. There is growing evidence that dysfunction in potassium channels correlates with several diseases, such as chronic hypertension, diabetes, hypercholesterolemia and atherosclerosis, etc.
MCE Potassium Channel Compound Library consists of 215 potassium channel inhibitor and activators, which is a useful tool to discover drugs for cardiovascular diseases and potassium channel research.
Slotoxin, a peptide from Centruroides noxius Hoffmann scorpion venom, blocks high conductance calcium-activatedpotassium channel, with Kd of 1.5 nM[1].
Kaliotoxin is a peptidyl inhibitor of neuronal BK-Type. Kaliotoxin can specific inhibit Kv channels and calcium-activated potassium channels. Kaliotoxin can be used for the research of the regulation of membrane potential and neuron excitability .
Noxiustoxin is a toxin from the venom of the Mexican scorpion Centruroides noxius which block voltage-dependent potassium channel (Kv1.3, IC50 = 360 nM), and calcium-activatedpotassium channel. Noxiustoxin plays an important role in neuroinflammatory disease .
Kobusin is a bisepoxylignan isolated from the Pnonobio biondii Pamp. Kobusin is an activator of CFTR and CaCCgie chloride channels and a inhibitor of ANO1/CaCC (calcium-activated chloride channel) channel .
CAPN2 (Calpain-2) is a calcium-regulated, non-lysosomal thiol protease known for catalyzing the limited proteolysis of substrates critical for cytoskeletal remodeling and signaling. Notably, CAPN2 proteolytically cleaves MYOC at “Arg-226,” suggesting its involvement in regulating the function of this protein. CAPN2 Protein, Human (His) is the recombinant human-derived CAPN2 protein, expressed by E. coli , with N-6*His labeled tag. The total length of CAPN2 Protein, Human (His) is 681 a.a., with molecular weight of ~82.1 kDa.
CAPN1 (Calpain-1) is a calcium-regulated non-lysosomal thiol protease that plays a critical role in the limited proteolysis of substrates involved in cytoskeletal remodeling and signal transduction. This protease catalyzes specific cleavage events, including CTBP1 cleavage at "Asn-375," "Gly-387," and "His-409," and activation of caspase-7 (CASP7). CAPN1 Protein, Human (His) is the recombinant human-derived CAPN1 protein, expressed by E. coli , with N-6*His labeled tag. The total length of CAPN1 Protein, Human (His) is 714 a.a., with molecular weight of ~85.9 kDa.
CAPN1 protein, a calcium-regulated non-lysosomal thiol-protease, facilitates cytoskeletal remodeling and signal transduction. It selectively cleaves substrates involved in these processes, including CTBP1 at 'Asn-375', 'Gly-388', and 'His-410'. CAPN1 also activates caspase-7 (CASP7), highlighting its role in regulating cellular functions. CAPN1 Protein, Mouse (His) is the recombinant mouse-derived CAPN1 protein, expressed by E. coli , with N-6*His labeled tag. The total length of CAPN1 Protein, Mouse (His) is 713 a.a., with molecular weight of ~86.1 kDa.
CANT1, a calcium-dependent nucleotidase, exhibits a pronounced preference for UDP, showcasing its enzymatic activity order as UDP > GDP > UTP > GTP. Notably, its activity towards ADP is minimal, and even lower towards ATP, while it does not hydrolyze AMP and GMP. This substrate specificity has been well-documented in various studies. Beyond its nucleotidase function, CANT1 is implicated in proteoglycan synthesis, underscoring its role in cellular processes related to the production of these essential macromolecules. The distinct substrate preferences and involvement in proteoglycan synthesis highlight the nuanced and specialized functions of CANT1 in cellular metabolism. CANT1 Protein, Human (HEK293, His) is the recombinant human-derived CANT1 protein, expressed by HEK293 , with N-His labeled tag. The total length of CANT1 Protein, Human (HEK293, His) is 322 a.a., with molecular weight of ~40 kDa.
CANT1, a calcium-dependent nucleotidase, exhibits a pronounced preference for UDP, showcasing its enzymatic activity order as UDP > GDP > UTP > GTP. Notably, its activity towards ADP is minimal, and even lower towards ATP, while it does not hydrolyze AMP and GMP. This substrate specificity has been well-documented in various studies. Beyond its nucleotidase function, CANT1 is implicated in proteoglycan synthesis, underscoring its role in cellular processes related to the production of these essential macromolecules. The distinct substrate preferences and involvement in proteoglycan synthesis highlight the nuanced and specialized functions of CANT1 in cellular metabolism. CANT1 Protein, Human (HEK293, Fc) is the recombinant human-derived CANT1 protein, expressed by HEK293 , with N-hFc labeled tag. The total length of CANT1 Protein, Human (HEK293, Fc) is 322 a.a., with molecular weight of ~65 kDa.
KCNN2 is a voltage-dependent potassium channel that is activated by intracellular calcium, leading to membrane hyperpolarization. This channel is thought to regulate neuronal excitability by promoting a slow component of postsynaptic hyperpolarization. KCNN2 Protein, Rat (Cell-Free, His) is the recombinant rat-derived KCNN2 protein, expressed by E. coli Cell-free , with N-10*His labeled tag. The total length of KCNN2 Protein, Rat (Cell-Free, His) is 580 a.a., with molecular weight of 69.9 kDa.
KCNN4 is a voltage-dependent potassium channel that is activated by intracellular calcium, leading to membrane hyperpolarization and subsequent calcium influx. This channel is critical for the reactivation of naive T cells, helping to maximize calcium influx and promote T cell proliferation. KCNN4 Protein, Human (Cell-Free, His) is the recombinant human-derived KCNN4 protein, expressed by E. coli Cell-free , with N-10*His labeled tag. The total length of KCNN4 Protein, Human (Cell-Free, His) is 427 a.a., with molecular weight of 59.1 kDa.
ANO1/Anoctamin-1 protein, a calcium-activated chloride channel (CaCC), plays diverse roles in cellular functions. It serves as a major contributor to basal and stimulated chloride conductance in airway epithelial cells, impacting tracheal cartilage development and contributing to airway mucus expression induced by interleukins IL3 and IL8, as well as by the asthma-associated protein CLCA1. ANO1 is indispensable for normal functioning of the interstitial cells of Cajal (ICCs), crucial for electrical pacemaker activity in gastrointestinal smooth muscles, and is involved in transepithelial anion transport and smooth muscle contraction. It is also required for CFTR activation and membrane expression, modulating endoplasmic reticulum Ca(2+) store release. Additionally, ANO1 participates in calcium-activated chloride secretion in human sweat gland epithelial cells, showing increased basal chloride permeability and decreased Ca(2+)-induced chloride permeability. In sensory neurons, ANO1 acts as a heat sensor and modulates spontaneous firing patterns, contributing to calcium-activated chloride channel activity in taste cells and mediating non-histaminergic Mas-related G-protein coupled receptor (MRGPR)-dependent itching in dorsal root ganglion neurons. In the developing brain, ANO1 is essential for the Ca(2+)-dependent process extension of radial glial cells. ANO1/Anoctamin-1 Protein, Human (N-His, C-Myc) is the recombinant human-derived ANO1/Anoctamin-1 protein, expressed by E. coli , with C-Myc, N-10*His labeled tag. The total length of ANO1/Anoctamin-1 Protein, Human (N-His, C-Myc) is 87 a.a., with molecular weight of ~17.6 kDa.
Hydrochlorothiazid-d2 is the deuterium labeled Hydrochlorothiazide. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect[1][2][3].
Hydrochlorothiazide- 13C6 is the 13C labeled Hydrochlorothiazide[1]. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect[2][3][4].
Hydrochlorothiazid- 13C,d2 is the 13C- and deuterium labeled Hydrochlorothiazide. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect[1][2][3].
Hydrochlorothiazide- 15N2, 13C,d2 is 15N and deuterated labeled Hydrochlorothiazide (HY-B0252). Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect .
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