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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) .
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 .
Dehydrosoyasaponin I (Soyasaponin Be;DHS-I), a triterpene glycoside, is a potent and reversible calcium-activated potassium (maxi-K) channelsactivator .
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 .
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.
Crofelemer (Provir) is an orally active antidiarrheal agent. Crofelemer acts on 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 can be used in the research of diarrheal diseases .
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 .
(E/Z)-BML264 (N-(p-amylcinnamoyl) Anthranilic Acid) is a broad spectrum Phospholipase A2 (PLA2) inhibitor and TRP channel blocker . (E/Z)-BML264 (N-(p-amylcinnamoyl) Anthranilic Acid) is also an effective reversible inhibitor of calcium-activated chloride channels, has potential to treat arrhythmia .
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].
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 .
AP14145 is an inhibitor for small conductance calcium-activated potassium channel, inhibits KCa2.2 channel and KCa channel with IC50 of 1.1 μM and 1.1 μM. AP14145 prolongs atrial effective refractory period (AERP) in rats, causes the conversion of atrial fibrillation to sinus rhythum in porcine left ventricular dysfunction models, and exhibits antiarrhythmic effect .
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 .
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- 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].
ANO1-IN-4 (Compound 10bm) is a reversible inhibitor for calcium-activated chloride channel transmembrane protein 16A (TMEM16A, also known as ANO1) with an IC50 of 0.030 µM. ANO1-IN-4 exhibits good metabolic stability in rat liver microsomes. ANO1-IN-4 inhibits spontaneous contraction in mouse isolated ileum .
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].
BKCa activator-1 (Compound 51b) is the orally active activator for the calcium-activated potassium channel BKCa with an EC50 of 2.82 μM. BKCa activator-1 increases K+ efflux, leads to cell membrane hyperpolarization, thereby inhibiting smooth muscle contraction. BKCa activator-1 alleviates urinary incontinence in spontaneously hypertensive rat (SHR) model, exhibits antitussive effect in puinea pig cough model .
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 .
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 .
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 .
NS4591 is a modulator of calcium-activated potassium channels with activity that enhances small (SK) and intermediate (IK) conductivity. NS4591 doubled IK-mediated currents in whole-cell patch-clamp experiments at a concentration of 45 +/- 6 nM, and doubled SK3-mediated currents at a concentration of 530 +/- 100 nM. NS4591 inhibits the number of action potentials generated by suprathreshold depolarizing pulses in acutely isolated bladder primary afferent neurons. NS4591 also reduced carbakol-induced detrusor ring contraction in the rat bladder, demonstrating sensitivity to apamin .
Niflumic acid (Standard) is the analytical standard of Niflumic acid. This product is intended for research and analytical applications. 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 .
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 .
NS 11021 is a potent and specific Ca 2+-activated big-conductance K + Channels (KCa1.1 channels)activator. NS 11021 at concentrations above 0.3 μM activates KCa1.1 in a concentration-dependent manner by parallelshifting the channel activation curves to more negative potentials .
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 .
Tertiapin (reduced) is a kind of synthesis of melittin, its Cys3-Cys14 and Cys5-Cys18 between containing a disulfide bond. Tertiapin (reduced) is a kind of inward rectifier potassium channels blockers, can block the activity of calcium activates large conductance potassium channels. Tertiapin (reduced) can be used for research in diseases such as rheumatoid arthritis and multiple sclerosis .
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 263 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 .
Tertiapin (reduced) is a kind of synthesis of melittin, its Cys3-Cys14 and Cys5-Cys18 between containing a disulfide bond. Tertiapin (reduced) is a kind of inward rectifier potassium channels blockers, can block the activity of calcium activates large conductance potassium channels. Tertiapin (reduced) can be used for research in diseases such as rheumatoid arthritis and multiple sclerosis .
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 .
Dehydrosoyasaponin I (Soyasaponin Be;DHS-I), a triterpene glycoside, is a potent and reversible calcium-activated potassium (maxi-K) channelsactivator .
CANT1 is a calcium-dependent nucleotidase that shows a clear preference for UDP, and the order of its enzymatic activity is UDP > GDP > UTP > GTP. It is worth noting that it has little activity on ADP and even less activity on ATP, but it does not hydrolyze AMP and GMP. CANT1 Protein, Human (HEK293, His) is the recombinant human-derived CANT1 protein, expressed by HEK293 , with N-His labeled tag.
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.
ANO1/Anoctamin-1 protein, a calcium-activated chloride channel (CaCC), is involved in ion transport, smooth muscle contraction, and mucus secretion. 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.
CANT1 is a calcium-dependent nucleotidase that shows a clear preference for UDP, and the order of its enzymatic activity is UDP > GDP > UTP > GTP. It is worth noting that it has little activity on ADP and even less activity on ATP, but it does not hydrolyze AMP and GMP. CANT1 Protein, Human (HEK293, Fc) is the recombinant human-derived CANT1 protein, expressed by HEK293 , with N-hFc labeled tag.
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.
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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