Calcium Channel

Applications Calcium channel blocker with antiallergic and anti-vasoconstricting activity. Antihistaminic. References Barber, J.H., et al.: Pharmatherapeutica, 2, 401 (1980), Spedding, M., et al.: Arch. Pharmacol., 318, 234 (1982), Morad, et al.: Pharmacol. Res., 35, 177 (1997)

Applications 1-EBIO stimulates Cl- secretion in secretory epithelia through direct activation of clacium potassium channels. References Devor, D.C., et. al.: 271, L775 (1996)

Menthol (DL-Menthol) is an organic compound made synthetically or obtained from peppermint or mint oils with flavoring and local anesthetic properties.

Norverapamil HCl, a Verapamil metabolite, blocks L-type calcium channels and inhibits P-gp function.

Nifedipine (Procardia) is a dihydropyridine calcium channel blocking agent.

CAD204520 functions as an inhibitor of SERCA (IC50 = 0.34 μM), specifically targeting mutations in the wild-type NOTCH1 protein associated with T-cell acute lymphoblastic leukemia (T-ALL) and mantle cell lymphoma (MCL).

Praeruptorin C: an antioxidant, calcium antagonist, protects neurons, reduces vascular hypertrophy, affects cellular signals.

RWJ 22108 is a bronchial-selective calcium channel (calcium channel) blocker that exhibits an IC50 of 5.7 nM in dog bronchial smooth muscle calcium-dependent contractions.

Acetylcholine Chloride is the chloride salt form of acetylcholine, a synthetic, quaternary amino alcohol with cholinergic properties.

GSK-7975A is a potent and orally available inhibitor of CRAC channel.

Mesaconitine: anti-inflammatory, relieves pain by boosting cAMP and central β-adrenergic system.

Barnidipine HCl is a potent dihydropyridine Ca²⁺ blocker with 0.35 nM IC50 in pig coronary artery.

Devapamil (Devapamilo) is a phenylalkylamine that blocks L-type calcium currents from the inner side of membrane cells in a use-dependent manner.

Ionomycin calcium (SQ23377 calcium) is an effective and selective calcium ionophore, exhibiting high specificity for calcium ions. Cost-effective and quality-assured.

Benidipine hydrochloride (Coniel) , a hydrochloride salt form of benidipine, is used as a blocker of dihydropyridine calcium channel.

Bupivacaine hydrochloride (Vivacaine) is a long-lasting, amide local anesthetic that blocks sodium channels, inhibiting nerve impulses and sensation.

Applications O-Des[2-aminoethyl]-O-carboxymethyl-dehydroamlodipine is the metablolite of Amlodipine (A633495), a long-acting calcium channel blocker that is commonly used as an anti-hypertensive in the treatment of cardiovascular conditions. 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),

Impurity Flunarizine EP Impurity D Applications (Z)-Flunarizine is Z-isomer of Flunarizine(F455200, Dihydrochloride), which is a calcium channel blocker. Flunarizine is a fluorinated derivative of Cinnarizine and a vasodilator (cerebral and peripheral). EP Impurity C References 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),

Palonidipine is an antagonist of calcium, is potential for the therapy of angina-pectoris and hypertension.

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),

Ophiopogonin D is a natural product,and is a CYP2J3 inducer that significantly inhibits Ang II induced NF-κB nuclear translocation.

Gomisin J is a natural product and have vasodilatory activity.

Calcium Channel antagonist 2 is a calcium channel antagonist (IC50=5-20 μM) that can be used to study diseases due to Ca2+ channels like pain and diabetes.

Crobenetine (BIII 890 CL) Free Base is a selective NaV channel blocker that eliminates VTD-induced [Ca2+] elevation.

Stability Light and Temperature Sensitive Applications 3-Desethyl-3-(2-phthalimidoethyl) Phthaloyl Amlodipine is a derivative of Amlodipine (A633495); a dihydropyridine calcium channel blocker where activity mainly resides in the (-)-isomer. 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)

Synta66 is a store-operated calcium entry channel Orai inhibitor, and used for the research of neurological disease.

Nitrendipine is a vasodilating calcium channel blocker and antihypertensive that preserves kidney function and promotes sodium excretion.

Catharanthine tartrate (Catharanthine hemitartrate) is an alkaloid from periwinkle that inhibits voltage-gated L-type calcium channels and has antitumor effect.

AE0047 Hydrochloride is a blocker of calcium, and used in the research of the hypertensive disease.

Diltiazem hydrochloride (RG 83606 HCl) is a benzothiazepine calcium channel blocking agent with vasodilating action.

Applications (+)-Muscarine Chloride modulates calcium channel currents in rats. References Stewart, A. E., et al.: J. Neurophysiol., 81, 72-84 (1999);

Cyclopiazonic acid (CPA) is a neurotoxic secondary metabolite (SM) made by A.

CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg

Applications Falipamil is a specific bradycardic agent and a calcium channel blocker. References Boucher, M., et al.: Eur. J. Pharmacol., 306, 93 (1996), Mubagwa, K., et al.: Arch. Int. Pharmacodyn. Ther., 286, 71 (1987), Chaudhry, A., et al.: Development Cardiovascular Medicine, 46, 196 (1985), Ogiwara, Y., et al.: Jpn Heart J., 29, (1988)

PD0176078 () is a newly blocker of N-type Calcium channel.

Efonidipine (NZ-105)(NZ-105) is a dihydropyridine calcium channel blocker, blocking both T-type and L-type calcium channels.

BMS-195270 is a bio-active chemical.

Manidipine (Iperten), a calcium channel blocker, which is dihydropyridine type. It is utilized

ethyl 4-chloro-2-oxo-1,2-dihydroquinoline-3-carboxylate inhibits NAD(P)H: quinone oxidoreductase 1.

Otilonium bromide (SP63) , an antimuscarinic, is utilized as a spasmolytic agent.

(2R/S)-6-PNG (6-Prenylnaringenin) from hops is a natural histone deacetylase inhibitor that blocks T-type calcium channels reducing neurogenicity in mice.

5J-4 is a potent a blocker of calcium release-activated calcium (CRAC) channel and store-operated calcium entry (SOCE).

Applications Labelled Diltiazem (D460620). A calcium channel blocker with vasodilating activity. Antianginal; antihypertensive; antiarrhythmic (class IV). References Sato, et al.: Arzneim.-Forsch., 21, 1338 (1971), Smirnov, S.R.: Eur. J. Pharmacol., 360, 81 (1998), Hansson, L., et al.: Lancet, 356, 359 (2000),

Levamlodipine besylate, or S-amlodipine (CAS 103129-82-4), is the active enantiomer of amlodipine, used to treat hypertension and angina.

SN 6 (SN6) is a selective Na+/Ca2+ exchanger (NCX) inhibitor (IC50s of NCX1: 2.9 μM , NCX2: 16 μM ,NCX3: 8.6 μM)

Impurity Clevidipine Butyrate Impurity A Applications Desethyl Felodipine is an impurity in the synthesis of Felodipine (F232375), a dihydropyridine calcium channel blocker. 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),

FPL64176 is a L-type calcium channels activator.

Equilin (7-Dehydroestrone) is a neurotrophic estrogenic steroid with vasodilatory activity used in the study of hypertension.

Applications Desacetyl Diltiazem-d4 Hydrochloride is the labeled analogue of Desacetyl Diltiazem Hydrochloride (D289335), a metabolite of Diltiazem Hydrochloride (D460620), a calcium channel blocher with vasodilating activity. Antianginal; antihypertensive; antiarrhythmic (class IV). References Shallcross, H., et al.: Br. Med. J., 295, 1236 (1987); Yeung, P.K.F., et al.: Drug Metab. Dispos., 18, 1055 (1990); Cashman, J.R., et al.: J. Med. Chem., 34,2049 (1991); Sato, et al.: Arzneim.-Forsch., 21, 1338 (1971); Smirnov, S.R.: Eur. J. Pharmacol., 360, 81 (1998); Hansson, L., et al.: Lancet, 356, 359 (2000)

(S)-Verapamil hydrochloride is an inhibitor of leukotriene C4 (LTC4) and calcein transport by MRP1,and leads to the death of potentially resistant tumor cells.

Fluspirilene is a long-acting antipsychotic for schizophrenia, inhibiting L-type calcium channels (IC50: 0.03 μM).

Nexopamil (LU-49938) is a dual calcium channel and 5-HT2A receptor antagonist that inhibits cell contraction and growth.

Impurity Nimodipine EP Impurity C; Nimodipine USP Related Compound B Applications O-Desisopropyl-O-methoxyethyl Nimodipine (Nimodipine EP Impurity C) is an impurity in the synthesis of Nimodipine (A dihydropyridine calcium channel blocker. It is used as a vasodilator (cerebral). Nimodipine USP Related Compound B. References Allen, G.S., et al.: N. Engl. J. Med., 308, 619 (1983), Schluter, H.: Arzneim.-Forsch., 36, 1733 (1986), Deyo, R.A., et al.: Science, 243, 809 (1989),

Applications TRAM-34 blocks intermediate conductance calcium-activated potassium channel IKCa1 with a Kd of 20nM and exhibits exquisite selectivity for the channel. Clotrimazole impurity. References Wulff, H., et al.: J. of Biological Chemistry, 276, 34, 32040 (2001)

Stability Light Sensitive Applications Ethyl Palmitoleate-d5 is the isotope analog of Ethyl Palmitoleate. Ethyl Palmitoleate is used in biological studies for calcium relase-activated calcium channel blockade as a potential tool in antipancreatitis therapy. References Gerasimenko, J.V., et al.: Proc. Natl. Acad. Sci. U.S.A., 110, 13186 (2013)

D-myo-Inositol-1,4,5-triphosphate trisodium (Inositol 1,4,5-trisphosphate trisodium) is a second messenger produced in cells by phospholipase C-mediated

Ibutilide Fumarate is a class III antiarrhythmic, prolonging action potentials by enhancing sodium influx, and can extend QT interval.