Inhibitors and Activators

Product #

Description

Biochem/physiol Actions

Add to Cart
SML0129 AC-265347 ≥98% (HPLC) 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.1
    • 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.
    • 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.
    • 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.
    • C235 Caged Ca2+ channel antagonist  
    • LO2221 Calcium Channel Modulators Ligand Set ligand set for calcium channel, TRP channel, and HCN channel modulators  
    • 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.
    • C5270 Cinnarizine powder Ca2+ channel blocker; central and peripheral 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.1
    • SML0579 EVP4593 ≥98% (HPLC) New 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.
    • 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.1
    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 T-type Ca2+ channel blocker; Scorpion toxin
    • L6668 Lercanidipine hydrochloride hemihydrate ≥98% (HPLC), powder 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 Non-selective Ca2+ channel blocker. At nanomolar concentrations, binds to μ opioid receptors; does not cross blood brain barrier.
    • M5441 Mibefradil dihydrochloride hydrate ≥98% (HPLC), powder Ro 40-5967 is a T-type Ca2+ channel blocker; antihypertensive.
    • 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) New 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.
    • 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: binds to the 30S and in some cases the 50S subunit causing miscoding; inhibits initiation and elongation during protein synthesis. Antimicrobial spectrum: Gram-negative and Gram-positive bacteria. Neomycin blocks voltage-sensitive Ca2+ channels without affecting the Na+/Ca2+ antiporter in neurons.
    Mode of action: binds to the 30S and in some cases the 50S subunit causing miscoding; inhibits initiation and elongation during protein synthesis.
    Antimicrobial spectrum: Gram-negative and Gram-positive 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.
    • N149 Nimodipine solid 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
    • P3371 Penfluridol ≥98% (HPLC), powder T-type Ca2+ channel blocker; antipsychotic
    • P4243 S-Petasin >98% (HPLC), powder L-type voltage-dependent calcium channel blocker.
    • 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.1
    • 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.
    • 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.
    Pyr3 is a selectively inhibitor of TRPC3. It acts 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 Ca2+ ion channels that are activated by membrane receptor-mediated stimulation of phospholipase C (PLC). However, TRPC3 and other family members are also activated by membrane-independent diacylglycerol (DAG). This channel is implicated in various processes, including B cell receptor (BCR)-mediated Ca2+ oscillations, activation of nuclear factor of activated T cells (NFAT), and promotion of cardiac hypertrophy.
    • R2751 Ruthenium Red Technical grade  
    • S6444 N-Salicyloyltryptamine ≥98% (HPLC), solid 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,1 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.
    • T7645 Tetracaine hydrochloride Sigma Reference Standard Blocks voltage-sensitive release of Ca2+ from sarcoplasmic reticulum.
    • 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 Inhibitor of calcium release-activated calcium (CRAC) channels (see Dennis et al.)
    Selective inhibitor of PDGF receptor tyrosine kinase.
    • 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.
    • Y4895 YM-58483 ≥98% (HPLC), solid 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.
    • 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.
    • 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.1
    • 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.
    • 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.