Calcium Channel

Monatepil 2maleate is an orally active Ca2+-channel antagonist and ACAT inhibitor with alpha(1)-adrenergic receptor blocking activity and antiarrhythmic properties that inhibit vasoconstriction.Monatepil 2maleate may be used to study atherosclerosis.

SAK3 is a modulator of nAChR activity and is used to study memory deficits and Alzheimer's disease.

(S)-(-)-Bay-K-8644 ((S)-(-)-Bay K 8644) is an agonist of L-type Ca2+ channel and activates Ba2+ currents with an EC50 of 32 nM.

Lercanidipine (Masnidipine) is a calcium channel blocker of the dihydropyridine class.

Applications Labelled Diltiazem (D460620). A calcium channel blocher 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),

Applications A calcium channel blocker. Antihypertensive; antianginal; antiarrhythmic (class IV). 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 Atlas, D, and Adler, M.: Proc. Natl. Acad. Sci. USA, 78, 1237 (1981), Janis, R., et al.: Adv. Drug. Res., 16, 309 (1987)

Gabapentin enacarbil (XP-13512) is a prodrug for the anticonvulsant and analgesic gabapentin, offering sustained dose-proportional exposure and predictable bioavailability.

Applications Ralfinamide mesylate is a mixed sodium and N-type calcium channel protein inhibitor. Inhibitory activity of Ralfinamide mesylate is voltage dependent, with higher potency towards inactivated channels. Ralfinamide mesylate is useful in preventing, alleviating and curing a wide range of pathologies, including pain, migraine, peripheral diseases, cardiovascular diseases, inflammatory processes affecting all body systems, disorders affecting skin and related tissues, disorders of the respiratory system, disorders of the immune and endocrinol. systems, gastrointestinal, urogenital, metabolic and seizure disorders. References Bayes, M., et al.: Methods. Find. Exp. Clin. Pharmacol., 27, 411 (2005); Pevarello, P., et al.: J. Med. Chem., 41, 579 (1998); Bauer, M., et al.: Pharmacol., 85, 297 (2010);

2-Aminoethyl diphenylborinate (2-APB) is a chemical that acts to inhibit both IP3 receptors and TRP channels.

ABT-639 is a potent and selective T-type calcium channel blocker.

YM-58483 (BTP2) is a specific and effective inhibitor of CRAC channels and subsequent Ca2+ signals.

Mirogabalin (DS5565) is a calcium channel blocker with analgesic effects.

NPS-2143 (SB 262470A) is a novel potent and selective antagonist of Ca(2+) receptor.

Praeruptorin C/E relaxes arteries, reduces heart contractility, acting like calcium blockers. D/E protect mice from acid lung injury by halting PMNs and IL-6.

(±)-Praeruptorin A could exhibit its anti-osteoclastogenic activity by inhibiting p38/Akt-c-Fos-NFATc1 signaling and PLCγ-independent Ca(2+) oscillation.

YM-244769 dihydrochloride is an effective inhibitor of Na+/Ca2+ exchange 3 (NCX3) with an IC50 of 18 nM.

Stability Light Sensitive Applications 5-Ethyl-demethyl Lercanidipine is an impurity of Lercanidipine (L179000), which is a dihydropyridine calcium channel blocker. References Bianchi, G., et al.: Pharmacol. Res., 21, 193 (1989); Rimoldi, E., et al.: Acta Therap., 200, 23 (1994); Argekar, A., et al.: J. Pharm. Biomed. Anal., 21, 1137 (2000);

SQ-31765 is a blocker of benzazepine calcium channel.

Ginsenoside Rd (Gypenoside VIII) may have properties that inhibit or prevent the growth of tumors.

Almorexant hydrochloride (ACT 078573 hydrochloride) is a dual orexin receptor antagonist that induces apoptosis and can be used to study sleep disorders.

Azumolene (EU4093 free base)

DHBP dibromide (1,1'-DI-N-HEPTYL-4,4'-BIPYRIDINIUM DIBRO) is calcium release and a muscle relaxant inhibitor.

Atagabalin HCl is a novel voltage-dependent calcium channel (VDCC) α2δ subunit (1 and 2) ligand that affects slow-wave sleep and can be used to treat insomnia.

Applications Isotope labelled Clindipine (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

Isradipine (PN 200-110), a dihydropyridine, is an antihypertensive calcium channel blocker that dilates arteries and reduces resistance.

Ethyl cinnamate has antifungal, and vasorelaxant effects.

Butamben (Butyl 4-aminobenzoate) is a long-duration local anesthetic used for the treatment of chronic pain.

Impurity Nimodipine EP Impurity A; Nimodipine USP Related Compound A Stability Light Sensitive Applications Dehydro Nimodipine (Nimodipine EP Impurity A; Nimodipine USP Related Compound A) is the dehydrogenated analogue and the major metabolite of the calcium channel blocker Nimodipine (N478200). References Scherling, D. et al.: Arzneim.-Forsch., 41, 392 (1991); Liu, X. et al.: Yaox. Xueb., 35, 257 (2000); Eicher, H. et al.: Arch. Gerontol. Geriat., 14, 309 (1992);

Tamolarizine (Tamolarizine free base) free base is a novel calcium antagonist.

Ethosuximide (Zarontin) is an anticonvulsant, blocks the low voltage-activated T-type calcium channel used in the treatment of absence seizures unaccompanied by

Calcium Channel antagonist 3 is a voltage-gated calcium channel inhibitor (IC50 : 5-20 μM).

Applications A dihydropyridine calcium channel blocker. Antihypertensive. References Safar, M., et al.: Clin. Pharmacol. Ther., 46, 94 (1989), Kharat, V.R., et al.: J. Pharm. Biomed. Anal., 28, 789 (2002), McCormack, A.J., et al.: Drugs, 63, 2327 (2003),

Norverapamil is a blocker of L-type calcium channel and an inhibitor of P-glycoprotein (P-gp) function .

SB-237376 is a calcium and potassium channel antagonist used to treat cardiac arrhythmias.

Trimebutine maleate (Polibutin) is a weak mu-opioid agonist and has antimuscarinic effects.

Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.

N-type calcium channel blocker-1 is an orally active analgesic agent,shows high affinity to functionally block N-type calcium channels.

Barnidipine (YM-09730-5(Free base)) is a calcium channel blocker.

Clevidipine (Clevidipine butyrate) is a dihydropyridine L-type calcium channel blocker that is selective for vascular smooth muscle and is indicated for blood

Catharanthine Tartrate, from Madagascar periwinkle, blocks L-type Ca2+ channels; has anti-cancer and antihypertensive properties.

Taurolithocholic acid sodium salt (Sodium taurolithocholate) is the major human metabolite, a bile acid which inhibits radioligand binding to muscarinic M1, but

Lidoflazine: antianginal, blocks HERG K+ & Ca channels, risks QT prolongation & arrhythmia.