Calcium Channel

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.

TPC2-A1-N is a TPC2 small molecule agonist that can be used to detect different functions of TPC2 channels in intact cells.

CRAC intermediate 2 is a intermediate compound for CRAC inhibitor synthesis.

Ionomycin: a calcium ionophore/antibiotic from Streptomyces conglobatus, raises Ca2+ levels, aids in studying Ca2+ transport, and activates PKC.

Oxodipine blocks rabbit aortic contraction and weakens rat cardiac force; reduces Ca currents in myocytes; side effects: mouse constipation, dog gum swelling.

Monatepil maleate (AJ-2615 maleate) is a Ca2+-channel and α1-adrenergic receptor antagonist, and ACAT inhibitor with antihypertensive activity.

Ginsenoside Rf (Panaxoside Rf) is a trace component of ginseng root. Ginsenoside Rf inhibits N-type Ca2+ channel.

Minocycline HCl: tetracycline antibiotic, treats bacterial infections and acne, may cause acute or chronic hepatitis.

Applications A dihydropyridine calcium channel blocker. Enantiomer S 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),

Fantofarone (SR 33557) is a highly potent antagonist of Calcium Channel.

Nimodipine (BAY-e 9736), a 1, 4-dihydropyridine calcium channel blocker, acts primarily on vascular smooth muscle cells.

Glaucine: antitussive, antioxidative, antiviral, may fight arthritis, boosts IL-10, hinders breast cancer cell spread by inhibiting MMP-9 and NF-κB.

Applications Used as an antihypertensive and antianginal. A dihydorpyridine calcium channel blocker. References Ali, S.L., et al.: Anal. Profiles Drug Subs., 18, 221 (1989), Soons, P.A., et al.: J. Pharm. Biomed. Anal., 9, 475 (1991), Brown, M.J., et al.: Lancet, 356, 366 (2000),

GeX-2 is a truncated analogue of αO-conotoxin. It has the ability to activate GABAB receptors and inhibit α9α10nAChR as well as CaV2.2 channels. Additionally, GeX-2 is effective in alleviating pain in a rat model of chronic constriction injury.

Yangambin: selective PAF antagonist, hypotensive, inhibits Ca2+ influx, induces peripheral vasodilation, affects CNS.

Pinaverium bromide is an calcium channel blocker with Antispasmodic and effectively relieves pain, diarrhea and intestinal discomfort.

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. Also useful in cannabis testing kits as a component in pesticide mixes (P698230). 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),

ML-9 suppresses MLCK, PKA, and PKC activity with Ki values of 4, 32, and 54 μM, respectively.

Flosatidil is a small molecule voltage-gated calcium channel complex (VDCCs) blocker for the treatment of neurological disorders and cardiovascular diseases,

cADPR, made from NAD+, boosts calcium in cells via Ryanodine receptors and TRPM2 channels.

Pranidipine (OPC-13340) is a novel, long-acting 1,4-dihydropyridine calcium channel blocker.

N6-(2-Hydroxyethyl)adenosine is a sedative, Ca2+ antagonist, and anti-inflammatory, affecting brain and heart blood flow.