Inhibitors and Activators

Product #

Description

Biochem/physiol Actions

Add to Cart

SML0085 A-967079 ≥98% (HPLC) A-967079 is a potent and selective antagonist of Transient Receptor Potential Anykrin 1 (TRPA1) with IC50′s of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively, and minimal or no activity at other TRP channels or G-protein-coupled receptors, enzymes, transporters, and ion channels out of 89 tested. A-967079 blocks TRPA1 activation in human and rat cell lines and has been shown to reduce the responses of wide dynamic range (WDR) and nociceptive specific (NS) neurons to high-intensity mechanical stimulation.
343781-M ω-Conotoxin GVIA, Conus geographus - CAS 106375-28-4 - Calbiochem A neurotoxin that acts as an antagonist of voltage-activated N-type Ca2+ channels and of neurotransmitter release at neuronal synapses.  
481981 Nifedipine - CAS 21829-25-4 - Calbiochem Relatively selective blocker of L-type Ca2+ channels.  
482200 Nimodipine - CAS 66085-59-4 - Calbiochem An L-type Ca2+ channel blocker.  
648485-M TrpA1 Antagonist, HC-030031 - CAS 349085-38-7 - Calbiochem The TrpA1 Antagonist, HC-030031, also referenced under CAS 349085-38-7, controls the biological activity of TrpA1. This small molecule/inhibitor is primarily used for Neuroscience applications.  
676777 (±)-Verapamil, Hydrochloride - CAS 152-11-4 - Calbiochem A papaverine derivative that blocks Ca2+ channels (principally the L-type) in smooth and cardiac muscle cells.  
SML0129 AC-265347 ≥98% (HPLC) AC-265347 is a calcimimetic that acts as agonist to calcium-sensing receptor. It reduces serum parathyroid hormone and plasma ionizable calcium.
AC-265347 is a human calcium-sensing receptor (CaSR) allosteric agonist. AC-265347 activates CaSR signaling in cellular proliferation and phosphatidyl inositol (PI) hydrolysis assays.
A7410 Amiloride hydrochloride hydrate ≥98% (TLC), powder Selective T-type calcium channel blocker and blocker of epithelial sodium channel. Selective inhibitor of urokinase plasminogen activator (uPA).
A8423 Amiodarone hydrochloride ≥98% Non-selective ion channel blocker with broad fungicidal activity. Amiodarone induces an immediate influx of Ca2+ in Saccharomyces cerevisiae, followed by mitochondrial fragmentation and cell death.
A5605 Amlodipine besylate ≥98% (HPLC) Amlodipine is an L-type calcium channel blocker. Amlodipine belongs to a class of cardiovascular drugs, which act at the voltage gated calcium channel of the CaV1, or L-type, class. Amlodipine also has antihypertensive and antianginal effects. Its activity resides mainly in the (-)-isomer. Amlodipine inhibits growth of human epidermoid carcinoma A431 cells and has antireproductive effects in male rats.
A8486 N-(p-Amylcinnamoyl)anthranilic acid ≥98% (HPLC) Broad spectrum phospholipase A2 (PLA2) inhibitor and TRP channel blocker.
A7232 AP-18 ≥98% (HPLC), solid AP-18 is a selective TRPA1 channel blocker. Transient receptor potential A1 (TRPA1) plays a central role for chemical sensing in the pain pathway. AP-18 is a novel TRPA1 channel blocker. It reduces cinnamaldehyde-induced nociception in vivo and blocks cold- and mustard oil-induced activation of mouse TRPA1 but not capsaicin-induced activation demonstrating selectivity vs. TRPV11. AP-18 reverses CFA-induced mechanical hyperalgesia in mice.
SML1467 ASP7663 ≥98% (HPLC) ASP7663 is a selective activator of transient receptor potential ankyrin 1 (TRPA1), known to play a role for chemical sensing in the pain pathway. ASP7663 activated human, rat, and mouse TRPA1 receptors with EC50 values of 510, 540, and 500 nM, respectively, and little or no affinity at more than 60 other related receptors, channels and enzymes. ASP7663 enhanced colonic motility and exerted analgesic effects against abdominal pain in mouse models.
A7106 Azelnidipine ≥98% (HPLC), powder Azelnidipine, a novel dihydropyridine derivative, is a L-type calcium channel blocker and antihypertensive. Unlike other L-type calcium channel blockers, azelnidipine causes minimal stimulation of the sympathetic nervous system despite its significant depressor effect. Azelnidipine may have a protective role in inflammation in atherosclerosis.
B133 (S)-(−)-Bay K8644 ≥98% (HPLC), solid Ca2+ channel activator; enantiomer of Bay K 8644.
B112 (±)-Bay K8644 calcium channel agonist Increases influx of Ca2+ specifically at voltage-gated calcium channels.
B5016 Bepridil hydrochloride powder Non-selective calcium channel blocker and class IV antiarrhythmic agent; inhibits Na+-Ca2+ exchange; inhibits growth of brain tumor cells in vitro.
SML0916 CaCCinh-A01 ≥98% (HPLC) CaCCinh-A01 is a potent calcium-activated chloride channel (CaCC) inhibitor that fully inhibits CaCC current in human bronchial and intestinal cells. CaCCinh-A01 does not inhibit CFTR.
C235 Caged Ca2+ channel antagonist  
SML0408 Carboxyamidotriazole ≥98% (HPLC) Carboxyamidotriazole (L-651582) is an orally active calcium channel blocker. Carboxyamidotriazole blocks intracellular and mitochondrial calcium entry and flux, resulting in inhibition of cell proliferation, calcium-release-activated calcium channel (CRAC) function, and maintenance of mitochondrial membrane potential.
C1493 Cilnidipine ≥98% (HPLC), powder Cilnidipine is a slow-acting Ca2+ channel blocker; antihypertensive; vasodilator; dual blocker of L-type voltage-gated Ca2+ channels in vascular smooth muscle and N-type Ca2+ channels in sympathetic nerve terminals that supply blood vessels. Cilnidipine may offer an advantage over nifedipine as the long term intake of the latter has been linked to increased risk of myocardial infarction and mortality in patients with coronary artery disease. Cilnidipine lowers blood pressure, but has less effect on sympathetic activity. Unlike nifedipine, cilnidipine does not inhibit PKC.
SML1498 Cinepazide maleate ≥98% (HPLC) Cinepazide maleate is a vasodilator used clinically in China used in China for the treatment of cardiovascular and cerebrovascular diseases, and peripheral vascular diseases. Cinepazide maleate is thought to act as a potentiator of adenosine A2 receptors and has also been characterized as a calcium channel blocker. It was withdrawn for agranulocytosis in several countries.
C5270 Cinnarizine powder Ca2+ channel blocker; central and peripheral vasodilator.
SML1447 Clemizole hydrochloride ≥98% (HPLC) Clemizole is a potent and preferring inhibitor of TRPC5 that efficiently blocks heterologously expressed homomeric TRPC5 channels as well as heteromeric TRPC1:TRPC5 channels. Clemizole is a potent and selective H1 histamine receptor antagonist. Clemizole inhibited binding of HCV RNA by NS4B inhibit HCV RNA replication in cell culture.
Clemizole is an antihistamine and an inhibitor of NS4B (nonstructural protein 4B) RNA of HCV (hepatitis C virus). Studies in Scn1α (sodium channel, voltage-gated, type I, α) Zebrafish mutant show that this drug has the potential as a therapeutic agent in Dravet Syndrome treatment.
SML0597 Daurisoline ≥98% (HPLC) Daurisoline alkaloid isolated from the rhizomes of Menispermum dauricum that exhibit varies pharmacological activities including antiplatelet aggregation, anti-inflammatory, neuron-protective properties, and antiarrhythmic effect. It appears that antiarrhythmic effect of daurisoline is maintained through blockade of hERG channels.
Daurisoline is antiarrythmic, anti-inflammatory, neuron-protective; and blocks hERG channels.
D2521 (+)-cis-Diltiazem hydrochloride ≥99% (HPLC) Blocks slow, or L-type Ca2+ channels; regulates Ca2+ release from intracellular stores in neutrophils; stimulates 1,4-dihydropyridine binding to Ca2+ channels; coronary vasodilator.
E0159 Efonidipine hydrochloride monoethanolate ≥98% (HPLC) Racemic efonidipine has both L-type and T-type calcium channel blocking activity. The R(−)-isomer appears to be very selective for T-type calcium channel. The S(+)-isomer inhibits the expressed Ca(V)1.2, Ca(V)1.3 and Ca(V)3.1 channel currents almost equally.
SML0579 EVP4593 ≥98% (HPLC) EVP4593 is a high affinity partial antagonist of NF-KB pathway activation acting by inhibiting store-operated calcium (Ca2+) entry (SOC). It appears that EVP4593 targets heteromeric channels containing TRPC1 as one of the subunits in HD neurons. EVP4593 exhibits neuroprotective effects from glutamate toxicity in nanomolar concentrations.
F9677 Felodipine solid L-type calcium channel blocker
F7265 Fendiline hydrochloride Coronary vasodilator
F8304 Flavoxate hydrochloride ≥98% (HPLC), solid L-type Ca2+ (Cav1.2) channel inhibitor
F8257 Flunarizine dihydrochloride ≥98% (TLC) Blocks T-type Ca2+/Na+ channels; inhibits K+-induced catecholamine release from chromaffin cells
F100 Fluspirilene Dopamine receptor antagonist; antipsychotic; calcium channel blocker.
F131 FPL 64176 ≥98% (HPLC), powder Potent Ca2+ channel (L-type) activator.
G154 Gabapentin solid Anticonvulsant with unknown mechanism of action; crosses the blood brain barrier; increases GABA concentrations in the brain and reduces excitatory amino acid neurotransmission, perhaps through its effects on voltage-gated calcium channels; exhibits antinociceptive, anxiolytic, neuroprotective and anti-epileptic effects.
SML0942 GSK2193874 ≥98% (HPLC) GSK2193874 is a very potent, specific antagonist of TRPV4 ion channels (IC50 = 50 nM). Lung edema caused by high pulmonary venous pressure (PVP) is driven by TRPV4 activity. GSK2193874 blocks TRPV4-mediated calcium influx in cells expressing native and recombinant TRPV4, and inhibits vascular permeability and lung edema in isolated rodent and canine lungs subjected to high PVP. The compound also resolves pulmonary edema in murine myocardial infarction model.
SML1551 GV-58 ≥97% (HPLC) GV-58 is a roscovitine analog that retains the ability to prolong the open state of calcium channels, but unlike roscovitine, is inactive against Cdk activity. GV-58 is a selective agonist of N-type and P/Q type calcium channels, which are critical to the triggering of neurotransmitter release at the neuromuscular junction. GV-58 has been studied as a possible therapeutic agent in a mouse model of Lambert-Eaton myasthenic syndrome (LEMS). The EC50 values for activation of N-, P/Q- and L- type calcium channels are 6.8, 9.9 and >100 μM, respectively.
H139 HA-1077 dihydrochloride solid, ≥98% (HPLC) Novel vasodilator agent which inhibits vascular smooth muscle contraction by acting as an intracellular Ca2+ antagonist.
H4415 HC-030031 ≥98% (HPLC), powder HC-030031 is a selective TRPA1 channel blocker, antagonizing formalin-evoked calcium influx and formalin-induced pain. IC50 is 5 μM. TRPA1 antagonism is a promising therapeutic target for chronic inflammatory or neurogenic pain.
HC-030031 is a selective TRPA1 channel blocker. HC-030031 antagonizes formalin-evoked calcium influx. IC50 is 5 μM.
I6658 Isradipine ≥98% (HPLC), solid L-type calcium channel blocker (also referred to as dihydropyridine-type calcium channel blocker); antihypertensive.
K4144 KB-R7943 ≥98% (HPLC), powder KB-R7943 inhibits the reversed Na(+)/Ca(2+) exchanger, NCX. In cardiomyocytes, Ca2+ is released from intracellular stores during contraction, and sequestered again during relaxation. NCX is the primary mechanism that prevents Ca2+ overload due to influx of calcium across the plasma membrane.
K1514 Kurtoxin Kurtoxin is isolated from the venom of the South African scorpion Parabuthus transvaalicus. It associates with voltage-gated sodium channels and delays their inactivation.
T-type Ca2+ channel blocker; Scorpion toxin
SML0946 Lacidipine ≥98% (HPLC) Lacidipine is a long-acting calcium antagonist that is used in the management of hypertension. Lacidipine is a L-type Ca(2+) channel blocker belonging to 1,4-dihydropyridine class. Also, Lacidipine inhibits ryanodine receptors on the ER membrane that enhances folding, trafficking and lysosomal activity of ERAD (ER-associated degradation) misfolded lysosomal glucocerebrosidase (GS).
L6668 Lercanidipine hydrochloride ≥98% (HPLC) Lercanidipine hydrochloride is a L-type (Cav1.2b) vascular channel antagonist; L-type (Cav1.2a) cardiac channel agonist voltage-dependent and highly lipophylic compound, which exhibits a slower onset and longer duration of action than other calcium channel antagonists; an antihypertensive agent in patients with mild-to-moderate hypertension; more vasoselective than lacidipine and amlodipine.
L9668 Lidoflazine ≥98% (HPLC), powder Lidoflazine is an antianginal calcium channel blocker that carries a significant risk of QT interval prolongation and ventricular arrhythmia. It prolongs QT interval by blocking HERG channel. IC50 < 0.1 μM
L6295 Lomerizine dihydrochloride ≥98% (HPLC), powder Lomerizine dihydrochloride is a voltage-dependent calcium channel blocker and selective cerebral vasodilator. It is one of the most selective calcium channel blockers for the CNS and cerebral arteries. It has been reported to inhibit both T-type and L-type Ca2+ currents in rat hippocampal CA1 pyramidal neurons, to prevent glutamate-induced neurotoxicity in rat hippocampal primary cell cultures, and to exhibit protective effects in animal models of migraine, ischemia and hypoxia. In Japan, lomerizine has been used as the first-line prophylactic drug for migraines.
L4762 Loperamide hydrochloride Loperamide hydrochloride (HCl) is a non-selective Ca2+ channel blocker. At nanomolar concentrations, it binds to μ-opioid receptors. Loperamide HCl does not cross the blood-brain barrier.
SML0893 M8-B hydrochloride ≥98% (HPLC) M8-B is a selective and potent antagonist of the transient receptor potential melastatin-8 (TRPM8) channel. M8-B blocked cold-induced and icilin or methol-induced activation of rat, human, and murine TRPM8 channels with IC50 values in rat ranging from 7.8 nM to 64.3 nM, and it did not block other TRP channels (IC50 values > 20 mM). M8-B decreased deep body temperature in both mice and rats, showing that blockade of TRPM8 receptor might be used to induce therapeutic hypothermia, an effective treatment in cardiac arrest.
M0267 (±)-Methadone hydrochloride powder, ≥98% (TLC) μ opioid receptor agonist that desensitizes both the μ opioid receptor and the δ opioid receptor on chronic exposure; narcotic analgesic, characterized by a gradual onset of action and prolonged, milder withdrawal; may also block L-type calcium channels independently of its effects on opioid receptors.
SML0658 3-MFA ≥97% (HPLC) 3-MFA is a mefenamic acid analog that blocks the transient receptor potential melastatin 2 (TRPM2) channel. Unlike other TRPM2 blockers such as 2-APB and flufenamic acid, 2-APB does not induce release of calcium from intracellular stores.
M5441 Mibefradil dihydrochloride hydrate ≥98% (HPLC), powder Ro 40-5967 is a T-type Ca2+ channel blocker; antihypertensive.
SML1509 MK6-83 ≥98% (HPLC) MK6-83 is a potent activator of wild type and mutant variants F465L and F408D of TRPML1 channel. MK6-83 weakly activates TRPML mutants R403C or V446L. MK6-83 restores channel function and rescue disease associated abnormalities in mucolipidosis type IV (MLIV) patient cells.
SML0400 ML204 ≥98% (HPLC) ML204 is a potent and selective TRPC4 channel inhibitor.
SML0385 ML218 ≥98% (HPLC) ML218 (CID 45115620) is a potent and selective T-Type (Cav3.1, Cav3.2, Cav3.3) calcium channel inhibitor (Cav3.2, IC50 = 150 nM in Ca2+ flux; Cav3.2 IC50 = 310 nM and Cav3.3 IC50 = 270 nM with good Drug metabolism/Pharmacokinetics. In a panel of 68 GPCRs, ion channels and transporters, ML218 was found to bind significantly only two other targets (sodium channel site 2 and sigma 1) and had no significant inhibition of L- or N-type calcium channels, KATP or hERG potassium channels. It showed robust inhibition of calcium current in STN neurons and was orally active in a rodent model of Parkinson’s Disease.
SML0627 ML-SA1 ≥95% (HPLC) ML-SA1 is a potent and selective cell permeable agonist of lysosomal mucolipin transient receptor potential channels (TRPML) 1, 2, 3 that significantly increases [Ca2+]cyt in HEK293 cells stably- or transiently-expressing mutant TRPML1 channels ML1-4A.
M1692 MRS 1845 ≥95% (HPLC), solid Store-operated calcium (SOC) channel inhibitor.
SML1623 MSP-3 ≥98% (HPLC) MSP-3 is a Transient Receptor Potential Vanilloid Type-1 (TRPV1) channel agonist with antioxidant and neuroprotective activity. MSP-3 activated TRPV1 channels with similar efficacy as compared to capsaicin (EC50 = 870 nM). It protected a keratinocyte cell line from oxidative stress damage with more efficacy than capsaicin and prevented the damage caused by H2O2 in differentiated human neuroblastoma cell lines as well as in rat cortical slices.
N3538 Nateglinide ≥98% (HPLC), solid Nateglinide is a Kir6.2/SUR1 channel inhibitor and antidiabetic. It is selective for the SUR1 subtype, which is found on pancreatic islet cells. Nateglinide evokes KATP channel-dependent insulin secretion (50-200 μM) in the absence and presence of insulin.
N1876 Neomycin trisulfate salt hydrate powder Mode of action: This product acts by binding to the 30S and 50S subunits, causing miscoding and inhibiting initiation and elongation during protein synthesis. Neomycin also blocks voltage-sensitive Ca2+ channels without affecting the Na+/Ca2+ antiporter in neurons.

Antimicrobial spectrum: Neomycin acts against both gram-positive and gram-negative bacteria.
N7510 Nicardipine hydrochloride powder, ≥98% Blocks L-type voltage-dependent calcium channels; antihypertensive.
N7634 Nifedipine ≥98% (HPLC), powder L-type Ca2+ channel blocker; induces apoptosis in human glioblastoma cells.
SML1372 Nifetepimine ≥95% (HPLC) Nifetepimine is a dihydropyrimidone calcium channel blocker that down-modulates SERCA3 (sarco/endoplasmic reticulum Ca2+ -ATPase 3) pump, and protects of the CD4+ T cells from tumor-induced apoptosis. Nifetepimine induces apoptotic cell death in triple negative breast cancer (TNBC) cells by stimulation of cross-talk between ER stress and the MEK/ERK pathway.
SML0945 Nilvadipine ≥98% (HPLC) Nilvadipine is a potent calcium channel blocker that is used for treatment of hypertension. Nilvadipine, as other dihydropyridine calcium antagonists, decreases intracellular calcium concentration causing dilation of the coronary and systemic arteries. Nilvadipine acutely reduced brain Aβ levels in a transgenic mouse model of Alzheimer′s disease (AD).
N149 Nimodipine Nimodipine is a potent L-type Ca2+ channel antagonist.
N0165 Nisoldipine ≥98% (HPLC) L-type (CaV1.2) calcium channel blocker; dihydropyridine-type calcium channel blocker with selectivity for smooth muscle (CaV1.2b) over cardiac muscle (CaV1.2a). Arterial vasodilator and antihypertensive agent.
N144 Nitrendipine >95%, powder Ca2+ channel blocker; anti-hypertensive.
N0287 NNC 55-0396 hydrate ≥98% (HPLC) Selective T-type calcium channel inhibitor
SML0972 ORM-10103 ≥98% (HPLC) ORM-10103 is a potent, specific inhibitor of the Na(+)/Ca(2+) exchanger, NCX. The compound ORM-10103 inhibits both inward and outward NCX currents with IC50 values of 780 nM, and 960 nM, respectively. ORM-10103 blocks induced arrhythmias in canine cardiac tissue.
P3371 Penfluridol ≥97% (HPLC), powder T-type Ca2+ channel blocker; antipsychotic
PZ0245 PF-05105679 ≥98% (HPLC) PF-05105679 is an antagonist of the TRP (transient receptor potential) channel, also known as the cold and menthol receptor 1 (CMR1), with an IC50 value of 103 nM. PF-05105679 is in clinical trials for neuropathic pain. Participants taking PF-05105679 could hold their hands in a bucket of ice water for a long time before feeling pain, and pain-alleviating effects matched those of oxycodone for about one hour after administration.
P7912 Phloretin ≥99% Blocks L-type Ca2+ channels; activates Ca2+-activated K+ channels in amphibian myelinated nerve fibers. Monocarboxylate transporter inhibitor.
Reacts with vic-dicarbonyl compounds such as glyoxal and methylglyoxal, preventing cytotoxic conjugation with biological macromolecules.
SML0049 Polygodial ≥97% (HPLC) Polygodial is a selective activator of Transient Receptor Potential Anykrin 1 (TRPA1) channels. Initially painful, polygodial acts as an analgesic by desensitizing sensory neuron. Polygodial also has broad antifungal properties, and is cytotoxic against bacteria and algae.
SML1596 PPZ2 ≥98% (HPLC) PPZ2 selectively activates DAG-activated TRPC3/TRPC6/TRPC7 channels. PPZ2 activates native TRPC6-like channels in smooth muscle cells isolated from the rabbit portal vein. PPZ2 induces BDNF-like neurite growth and neuroprotection in cultured neurons.
TRPCs are cation channels, mainly permeable to Ca2+ ions. TRPC6 plays a crucial role in tumor development. TRPC3 controls fibronectin expression, thereby regulating wound healing process. TRPC7 is involved in the proliferation of osteoblasts.
PZ0010 Pregabalin ≥97% (NMR) Pregabalin is a lipophilic GABA analog/ligand at α2δ subunit of voltage-dependent Ca2+ channels. Pregabalin is an anticonvulsant, anxiolytic analgesic used to treat peripheral neuropathic pain and fibromyalgia.
P8489 Protopine hydrochloride ≥98%, solid Protopine hydrochloride is a Ca2+ channel blocker and antiplatelet agent.
SML1243 Pyr10 ≥98% (HPLC) Pyr10 is a novel, selective inhibitor of the transient receptor potential channel TRPC3. Pyr10 blocks carbachol-induced calcium entry into TRPC3-transfected HEK293 cells (IC50 = 0.72 μM), with significantly lower activity against STIM1/Orai1 mediated release of calcium from endoplasmic reticulum (store operated calcium entry) in BRL-2H3 cells (IC50 = 13.08 μM).
P0032 Pyr3 ≥98% (HPLC) Pyr3 is a pyrazole compound that potently and selectively antagonizes TRPC3. Pyr3 inhibits TRPC3 by binding to the extracellular side of the receptor, resulting in suppression of B cell activation and cardiac hypertrophy.

Members of the canonical transient receptor potential (TRPC) channel family are ion channels which conduct Ca+2 and are activated by membrane receptor-mediated stimulation of phospholipase C (PLC) activity. However, TRPC3 and other family members are also activated by membrane-independent diacylglycerol (DAG). BTP1 and BTP2 are pyrazoles that block TRPC channels, but they are not specific for TRPC subtypes. This channel is implicated in various processes, including B cell receptor (BCR)-mediated Ca+2 oscillations, activation of nuclear factor of activated T cells (NFAT), and promotion of cardiac hypertrophy.
SML1241 Pyr6 ≥98% (HPLC) Pyr6 is a selective inhibitor of calcium release from the endoplasmic reticulum via STIM1/Orai1 mediated, store operated calcium entry (SOCE). Pyr6 blocks SOCE in thapsigargin treated, calcium depleted BRL-2H3 cells (IC50 = 0.49 μM), but has poor activity against carbachol-induced, TRPC3-mediated calcium entry in TRPC3-transfected HEK293 cells (IC50 = 18.46 μM).
SML1547 RN-9893 ≥98% (HPLC) RN-9893 is a potent and selective antagonist of the Transient Receptor Potential ion channel TRPV4. RN-9893 has IC50 values of 420 nM, 660 nM, and 320 nM for human, rat and mouse TRPV4 receptors, respectively. RN-9893 shows excellent selectivity over related TRP receptors with no inhibition of TRPV1 at a concentration of 10 μM, an IC50 >30 μM against TRPV3, an IC50 of approximately 30 μM against TRPM8, and also good selectivity using 54 binding assays against common biological targets.
SML1602 RQ-00203078 ≥98% (HPLC) RQ-00203078 is an orally available potent and selective TRPM8 antagonist that potently reduces cation currents induced by menthol and other TRPM8 agonists. RQ-00203078 inhibits HSC3 and HSC4 oral squamous carcinoma cell migration and invasion in vitro.
R2751 Ruthenium Red Technical grade  
S6444 N-Salicyloyltryptamine ≥98% (HPLC), solid N-Salicyloyltryptamine (STP) is a central nervous system depressant that inhibits the transient outward and sustained K+ current in neuroendocrine cells. This decreases the ability of neuronal cells to generate action potential.1,3 STP is has immunomodulatory effects as it inhibits the activation of ERK 1/2 and NF-κB.4
Activator of calcium-activated K+ channels; anticonvulsant and neuroprotectant.
S5576 SKA-31 ≥98% (HPLC) SKA-31 is an activator of KCa2 and KCa3.1 calcium-activated potassium channels. Its EC50 is almost identical at 2-3 μM for all KCa2 subtypes, and about 10-fold lower (260 nM) at KCa3.1 channels. It has significant blood-pressure reducing activity in experimentally hypertensive mice, suggesting potassium channel activation as a therapeutic target for hypertension.
SKA31 is an activator of KCa2 and KCa3.1 Potassium Channels, Potentiates the EDHF Response and Lowers Blood Pressure.
S7809 SKF-96365 ≥98% (HPLC), solid SKF-96365 is a selective inhibitor of receptor-mediated Ca2+ entry and voltage-gated Ca2+ entry. In circular smooth muscle bundles isolated from the guinea-pig stomach antrum, the effects of quinidine, Ni2+, flufenamic acid, niflumic acid, La3+, SKF-96365 and 4′-diisothiocyanatostilbene-2,2′-disulphonic acid (DIDS) on acetylcholine (ACh)-induced depolarization were investigated. SKF-96365 (3-50 μM) depolarized the membrane in a concentration-dependent manner, but did not change the level of ACh-induced depolarization. These results provide evidence that ACh-induced depolarization is not inhibited by chemicals known to inhibit non-selective cation channels.
S1818 SNX-482 synthetic >98% (HPLC), lyophilized powder Specifically blocks Cav2.3 (α1E, R-type) calcium channels in a voltage dependent manner.
T9025 Thioridazine hydrochloride ≥99% D2 dopamine receptor antagonist; phenothazine antipsychotic with reduced extrapyramidal side effects; Ca2+ channel blocker.
T2955 γ6 TM1a trifluoroacetate salt ≥95% (HPLC) The calcium channel γ family is a subgroup of the tetraspanin proteins. There are the eight γ subunits that have been identified to date. Among these γ1 subunit acts as an endogenous antagonist of the skeletal HVA calcium current, and γ6 inhibits the low voltage-activated (LVA) Cav3.1 calcium current. A GxxxA motif in the first transmembrane domain (TM1) of γ6 was identified as critical for inhibiting the Cav3.1 current. γ6 TM1a is an octapeptide contains residues 41 through 48 of the native γ6 protein. The peptide inhibits the Cav3.1 calcium current in a dose-dependent manner. The reduction of channel current is mostly due to the inhibition of both resting and inactivated channels relatively independent of membrane potential. Thus γ6 TM1might function as a pore blocker. Also γ6 TM1a peptide inhibits Cav1.2 current with reduced efficacy. The γ6 TM1a peptide has the potential of being further developed as a novel therapeutic agent targeting Cav3.1 and possibly Cav1.2 calcium current.
T182 Tyrphostin A9 solid Tyrphostin A9 is a PDGF receptor tyrosine kinase inhibitor that can induce apoptosis in cancer cells, inhibit the growth of vascular smooth cells and block calcium release-dependent phosphorylations.
SML0782 (-)-Umbellulone ≥98% (HPLC) (-)-Umbellulone, isolated from the"headache tree" Umbellularia californica Nutt, is a selective activator of Transient Receptor Potential Anykrin 1 (TRPA1) channels. (-)-Umbellulone activates TRPA1 channels on nociceptive trigeminal afferents, resulting in release of CGRP and CGRP-mediated neurogenic vasodilatation, causing a painful cold sensation and headache/migraine.
V5754 Veratridine ≥90% (HPLC), powder Opens voltage-dependent Na+ channels and prevents their inactivation. This, in turn, opens voltage-activated calcium channels, thus increasing intracellular calcium content and inducing neurotransmitter release. Alkaloid neurotoxin which depolarizes excitable tissue; used to increase membrane sodium permeability. Veratridine is cytotoxic to chromaffin cells in vitro.
SML1336 VUAA1 ≥98% (HPLC) VUAA1 is an agonist of the highly conserved insect odorant receptor co-receptor ion channel Orco. VUAA1 is able to activate both heteromeric and homomeric Orco-containing channels, acting as an insect repellant by over-activating an insect′s olfactory senses causing a repellent effect.
Y4895 YM-58483 ≥98% (HPLC) YM-58483 is a selective Ca++ release-activated Ca++ (CRAC) [a.k.a. store-operated Ca++ (SOC) channels] that mediate Ca++ influx in T cells and other inflammatory cells. CRAC channel inhibitors have potential clinical applications in autoimmune disease, transplant rejection, allergic airway inflammation and bronchial asthma. YM-58483 is also promoted as a tool for CRAC studies; may be used as a gold standard.