Calcium Channel

Ned 19 inhibits tumor growth, vascularization, lung metastases in mice, and is a selective NAADP antagonist.

NecroX-5, a derivative of NecroX, exhibits anti-inflammatory and anti-cancer activities. NecroX-5 reduces intracellular calcium concentration.

ORM-10103 is a novel potent and selective inhibitor of the Na+/Ca2+ exchanger (NCX).ORM-10103 inhibited NCX currents with estimated IC50 values of 55 and 67 nM

Applications Inhibits the catalytic activities of several protein kinases competitively with respect to ATP and exhibited different Ki values toward each protein kinase. Also found to be a new type of vascular relaxant. References Hidaka, H., et al.: J. Biol. Chem., 262, 16, 7796 (1987)

Vatanidipine (AE0047) is a novel dihydropyridine (DHP)-type calcium channel blocker with slow-onset pharmacological actions.A slow-onset and long-lasting

1-Octanol is a saturated fatty alcohol, inhibits T-type Ca²⁺ channels with a 4 μM IC50, and is a potential diesel-like biofuel.

Manidipine dihydrochloride (Manidipine 2HCl) is a potent calcium channel blocker for Ca2+ current(IC50=2.6 nM).

Linoleic Acid Amide (Linoleamide) is derived from linoleic acid and regulates Ca2+ flux by inhibiting the sarco/endoplasmic reticulum Ca2+-ATPase.

Nicardipine hydrochloride is a potent calcium channel blocker used to dilate cerebral and coronary vessels.

Applications Synthetic pyrethroid insecticide, which acts as a potent inhibitor of calcineurin (protein phosphatase 2B) and has an IC50 of about 100pM. This inhibition action results in cellular hyperexcitability by causing non-mutated calcium channels to remain open for an extended period of time allowing an abundance of Ca2+ to enter the cell. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Kavlock, R., et al.: J. Environ. Pathol. Toxicol., 2, 751 (1979), Enan, E., et al.: Biochem. Pharmacol., 43, 1777 (1992), Tan, J., et al.: Mol. Biol., 32, 445 (2002),

Applications tert-Butyl 3-Aminopropyl(methyl) Carbamate acts as a reagent for dihydroquinazoline derivatives preparation and antitumor activities, induction of apoptosis in human lung adenocarcinoma A549 cells by T-type calcium channel antagonist. References Choi, D. L., et al.: Bioorg. Med. Chem. Lett. 24, 1565 (2014); Byun, J. S., et al.: Bioorg. Med. Chem. Lett., 26, 1073 (2016);

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Mibefradil is a calcium channel blocker with moderate selectivity for T-type Ca2+ channels (IC50s: 2.7 μM and 18.6 μM for T-type and L-type currents).

Nicardipine (Cardene), a calcium channel blockers belonging to the dihydropyridine class, is a drug used to treat angina and high blood pressure.

Maresin 1 is biosynthesized by macrophages (MΦ) and possesses significant anti-inflammatory activity that attenuates LPS-induced lung injury in mice.

Opc 8490 is a cardiotonic agent and a positive inotropic vasodilator, which prolongs the atrial action potential in a concentration-dependent manner.

Catharanthine ((+)-3,4-Didehydrocoronaridine) suppresses nicotinic receptor-mediated diaphragm contractions (IC50=59.6 μM).

Teludipine hydrochloride is a blocker of lipophilic calcium channel.

McN5691 is a voltage sensitive calcium channel blocker.

Nilvadipine (FK235), a calcium channel blocker (CCB), is utilized for treatment of hypertension.

Applications Dihydrocinnamyl Cilnidipine is a metabolite of Cilnidipine (C441375); a dihydropyridine calcium channel blocker. References Ikeda, K., et al.: Oyo Yakuri, 44, 433 (1992); Hosono, M., et al.: J. Pharmacobio-Dyn., 15, 547, (1992); Ishii, M.: Japan Pharmacol. Ther., 21, 59 (1993)

CP-060 is a potent Ca2+ antagonist and inhibits Ca2+ overload with antioxidant and cardioprotective activities.

TTA-Q6 is a T-type Ca2+ channel antagonist that inhibits the uptake of extracellular calcium ions by tumour cells for the treatment of neurological diseases.

PptT-IN-4 (Compound 3a) is a PptT inhibitor exhibiting an IC50 of 0.71 μM.

NFAT Inhibitor-2 is a compound used as a molecular building block.

Applications 4-(2-Chlorophenyl)-2-methyl-5-oxo-4,4a,5,7,8,10-hexahydro-1H-pyrido[2',3':2,3]azeto[2,1-c][1,4]oxazine-3-carboxylic Acid is an intermediate in the synthesis of 3-O-Desethyl-5-O-desmethyl Amlodipine (D291305). 3-O-Desethyl-5-O-desmethyl Amlodipine is an impurity of Amlodipine (A633495), which is a dihydropyridine calcium channel blocker. References Arrowsmith, J.E., et al.: J. Med. Chem., 29, 1696 (1986); Burges, R.A., et al.: J. Cardiovasc. Pharmacol., 9, 110 (1987); Haria, M., et al.: Drugs, 50, 560 (1995)

2,5-Di-tert-butylhydroquinone (BHQ) is an effective and selective endoplasmic reticulum Ca2+-ATPase inhibitor.

Applications Darodipine, is a calcium channel antagonist. References Matucci, R., et al.: British J. Pharmacol., 122, 1353 (1997);

1-(aminomethyl)cyclopropanecarboxylic acid hydrochloride inhibits L amino acid transporter proteins and the α2δ subunit of voltage-gated calcium channels.1-(

L-Ascorbic acid (Vitamin C) is a natural product that is a potent reducing agent and antioxidant.

Calcium channel-modulator-1 is a calcium channel-modulator (IC50:0.8 μM) with specialisation to block aortic constriction.

Iganidipine(NKY 722) is a new water-soluble Ca2+ antagonist with antihypertensive activity for research and neurological related diseases.

1,4-Dihydropyridine acts as an antagonist for calcium channels (calcium channel), specifically blocking the L-type calcium channels. This action reduces the influx of calcium ions into cardiac and vascular smooth muscle cells, consequently decreasing cardiac contractility and heart rate, dilating blood vessels, and lowering blood pressure.

Applications Carboxyamidotriazole is an orally active calcium channel blocker. Carboxyamidotriazole also exhibits inhibition of pro-inflammatory cytokines in tumor associated macrophages as potential anti-cancer mechanism. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Ju, R., et al.: Euro. J. Cancer., 48, 1085 (2012); Corrado, C., et al.: Cancer. lett., 300, 205 (2011);

Praziquantel (Droncit) is an anthelmintic that paralyzes worms by increasing calcium in muscle cells, causing tegument damage and immune response.

Nexopamil racemate((Rac)-Nexopamil) is a racemate of Nexopamil. The Nexopamil racemate has potential anti-asthmatic and anti-ulcer activity.

1-EBIO (1-EBIO) is a calium channel agonist.

Applications A23187 is calcium channel modulator; Highly selective Ca2+ ionophore. References Khin, P. P., et al.: Pharmacol., 99, 216-225 (2017); Han, N., et al.: Chin. Exp. Pharmacol. Physiol., 44, 257-265 (2017)

Applications Ruthenium Red is an inhibitor of ryanodine receptor (RyR) channels (1). It is also an inhibitor of mitochondrial ETC complexes I and III (2). Dyes and metabolites. References (1) Lukyanenko, V., et al.: Biophys J. 79, 1273 (2000) (2) Theodossiou, T. et al.: Photochem. Photobio., 88, 1016 (2012)

Flavoxate hydrochloride (DW61) , a muscarinic AChR antagonist, is used in the therapy of various urinary syndromes and as an antispasmodic.

Levamlodipine (S-amlodipine) belongs to the dihydropyridine group of calcium channel blockers.

Dronedarone (SR 33589) is an amiodarone analogue which has an effective and promising treatment for Atrial fibrillation.

Applications A dihydropyridine calcium channel blocker. Enantiomer R of Felodipine. References Berntsson, P.B., et al.: Acta Pharm. Suec., 18, 221 (1981), Kratochwil, N., et al.: Biochem. Pharmacol., 64, 1355 (2002), O'Brien, S., et al.: J. Med. Chem., 48, 1287 (2005), Castilho, M., et al.: Bioorg. Med. Chem., 14, 516 (2006),

Cis-22a: selective TRPV6 inhibitor (IC50=0.32μM), halts T47D breast cancer cell growth.

ISX-9 (Isoxazole 9) is necessary to activate neuron-specific genes as neurogenesis inducer.