Calcium Channel

Calcium Channel antagonist5 (compound 32) is a calcium channel antagonist with a pIC50 of 5.50.

Applications A compound active at novel site on receptor-operated calcium channels useful for treatment of neurological disorders and diseases. References Farid, N.A., et al.: J. Clin. Pharmacol., 25, 296 (1985), Gehlert, D.R., et al.: J. Neurochem., 64, 2792 (1995), Hwamg. et al.: Neurosci. Lett., 265, 151 (1999), Ring, B.J., et al.: Drug Metab. Dispos., 30, 319 (2002),

NP118809 (39-1B4) is a potent N-type calcium channel blocker(IC50 : 0.11 μM).

O-Desmethylcarvedilol (Desmethylcarvedilol) is an active metabolite of Carvedilol, a non-selective β-adrenergic receptor (β-AR) antagonist. This compound inhibits store overload-induced calcium release in HEK293 cells expressing the RyR2 R4496C mutation (IC50= 7.62 µM). Additionally, O-Desmethylcarvedilol slows the increase in heart rate and prevents diastolic pressure reduction induced by Isoproterenol in conscious rabbits (ED50s = 32 and 5 µg/kg).

Dopropidil: anti-angina calcium regulator with anti-ischemic properties in animal models.

Cinacalcet metabolite M4 (Rarechem AL BW 1078) is a metabolite of Cinacalcet. Cinacalcet is an allosteric agonist of Ca receptor.

Applications JTV 519 Fumarate is a useful intermediate. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package

Tiapamil hydrochloride (Ro 11-1781 hydrochloride) is a calcium channel blocker with antihypertensive activity used in the study of angina pectoris.

Calcium Channel antagonist 4 is a voltage-gated calcium channel inhibitor (IC50 : 5-20 μM).

Lanthanum(III) chloride blocks divalent cation channels, useful for biochemical research.

Applications A new lipophilic calcium channel blocker; a new dihydropyridine derivative, on cell lines displaying the multidrug resistant phenotype. References Tolomeo M., et al.: Haematologica, 79, 328 (1994),

Methyl homoveratrate, a McN5691 (RWJ-26240) metabolite detected in vivo in plasma, urine, and fecal extracts, functions as a voltage-sensitive calcium channel

Applications 1-Bis(4-fluorophenyl)methyl Piperzaine-d8 is a labelled analogue of 1-Bis(4-fluorophenyl)methyl Piperzaine (B434875), which is a chemical reagent used in the synthesis of novel tubulin polymerization inhibitors. Also used in the synthesis of novel benzhydrylpiperazine carboxamide derivatives. Impurity of F455200. It is also an intermediate in synthesizing Flunarizine-d8 Dihydrochloride (F455202), which is a calcium channel blocker; fluorinated derivative of Cinnarizine. Vasodilator (cerebral and peripheral). 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 Yin, Y. et al.: Bioorg. Med. Chem., 22, 2409 (2014); Gurdal, E. et al.: J. Enz. Inhib. Med. Chem., 29, 205 (2014); Desmedt, L.K., et al.: Arzneim.-Forsch., 25, 1408 (1975); Godfraind, T., et al.: Eur. J. Pharmacol., 53, 273 (1979); Nihard, P., et al.: Angiology, 33, 37 (1982); Holmes, B., et al.: Drugs, 27, 6 (1984);

KT-362 is a calcium channel blocker with antihypertensive properties that can be used in the study of cardiovascular disease.

Ranolazine 2HCl, an antianginal, treats arrhythmia by inhibiting sodium current without changing blood pressure or heart rate.

Rhynchophylline (Mitrinermine) is an alkaloid isolated from Crocus sativus and is widely used in anti-inflammatory and neuroprotective studies.

Pelretin (BASF 43915) is a potential protein inhibitor for the study of dermatologic diseases.

Applications 1,4-Dibromobenzene is used in the synthesis of triarylamines as well as trans-stilbenes. Also used in the synthesis of calcium channel blockers for inhibition of TRPV6-mediated calcium transport. 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 Corriu, R. et al.: J. Chem. Soc. Chem. Comm., 3, 144 (1972); Lambert, C. et al.: J. Am. Chem. Soc., 121, 8434 (1999); Hofer, A. et al.: Bioorg. Med. Chem., 21, 3202 (2013);

YM-244769 (3-Pyridinecarboxamide, N-[(3-aminophenyl)methyl]-6-[4-[(3-fluorophenyl)methoxy]phenoxy]-) is an effective inhibitor of Na+/Ca2+ exchange 3 (NCX3)

Applications Labelled 2,5-Dimethoxy-4-bromoamphetamine (DOB) is one of the potent hallucinogenic phenylalkylamines with neurotoxic properties. References Monte, A., et al.: J. Med. Chem., 39, 2953 (1996), Pedersen, W., et al.: Addiction, 94, 1695 (1999), Kanamori, T., et al.: J. Anal. Toxicol., 26, 61 (2002),