Calcium Channel

Psoralenoside: a compound from Psoralea fruit; has estrogenic, osteoblastic, antitumor, and antibacterial properties.

TTA-A8 is an antagonist of T-type calcium channel.

Carboxyamidotriazole Orotate (L-651582 Orotate) is a cytostatic inhibitor of non-voltage-operated calcium channels and calcium channel-mediated signaling

CCT129957 is a novel and potent phospholipase C-γ (PLC-γ) inhibitor with an IC50 of about 3 μM and a GC50 of 15 μM.CCT129957 exhibits anticancer activity and

Applications N-Piperidinyl acetamide derivatives as calcium channel blockers and their use in the treatment of obesity. References Lopez-Rodriguez, et al.: Bioorg. Med. Chem. Lett., 11, 2807 (2001), Yang, et al.: J. Med. Chem., 51, 6471 (2008),

Darodipine (PY-108068) is a dihydropyridine type Ca+2 antagonist.

SB-423557 is an orally active antagonist of calcium-sensing receptor (CaR) with IC50 of 520 nM

(Rac)-PD0299685 is a potent voltage-dependent calcium channel inhibitor for the study of retina-related diseases.

Carboxyamidotriazole is a cytostatic inhibitor of non-voltage-operated calcium channels and calcium channel-mediated signaling pathways.

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),

Gallopamil blocks acid secretion (IC50: 10.9 μM), acts as antiarrhythmic, vasodilator, and is a methoxy Verapamil derivative.

Impurity Nisoldipine Applications Dehydronitrosonisoldipine is an impurity of Nisoldipine (N489125). Nisoldipine is a dihydropyridine calcium channel blocker and it is antihypertensive and antianginal. References Kazda, S., et al.: Arzneimittel-Forsch., 30, 2144 (1980); Pasanisi, F., et al.: Eur. J. Clin. Pharmacol., 29, 21 (1985); Lam, J., et al.: J. Am. Col. Cardiol., 6, 447 (1985)

BTT-266 is a blocker of voltage-gated calcium channel for pain management.

Cronidipine (LF 20254), a calcium channel antagonist, is used potentially for the treatment of hypertension and myocardia ischemia.

Zonisamide (AD 810), a sulfonamide anticonvulsant, is approved for use as an adjunctive treatment in adults with partial-onset seizures.

Tetrandrine (Sinomenine A) is a naturally occurring biphenylisoquinoline alkaloid, a calcium channel inhibitor. Cost-effective and quality-assured.

Applications α-Phenyl-α-[3-(phenyl-2-pyridinylmethylene)-2,4-cyclopentadien-1-yl]-2-pyridinemethanol is an intermediate in the synthesis of Norbormide (N661150), a rodenticide that acts as a vasoconstrictor and calcium channel blocker, but is selectively toxic to rats and has relatively low toxicity to other species, due to a species specific action of opening the permeability transition pores in rat mitochondria. References Rennison, D., et al.: Bioorg. Med. Chem. 15, 2963 (2007);

Stability Light and Moisture Sensitive Applications Isotope Labelled analogue of rac-Kavain (K145490), the main kavalactone found in the roots of the kava plant. Kavain is known to exhibit anticonvulsive properties by attenuating vascular smooth muscle contraction through interactions with voltage-dependent sodium and calcium channels. rac-Kavain was shown in recent research to exhibit protective properties on anaerobic glycolysis, ATP content and intracellular calcium and sodium of anoxic brain vesicles. References Gleitz, J., et al: Neuropharmacol., 35, 1743 (1997); Hashimoto, T., et al.: Phytomedicine, 10, 309 (2003); Mulholland, P.J., et al.: Brain. Res., 945, 106 (2002);

Diltiazem (CRD 401 free base) is an orally available L-type Ca2+ channel blocker with antihypertensive, antiarrhythmic, and cardioprotective properties that prevent post-reperfusion myocardial injury, angina pectoris, and cardiovascular-related diseases.

Mibefradil dihydrochloride (Ro 40-5967 (dihydrochloride)) is an blocker of calcium channel with moderate selectivity for T-type Ca2+ channels (T-type and L-type

(+)-Kavain ((R)-KAWAIN) is one of the six major kavalactones found in the Piper methysticum (kava) plant; reversible inhibitor of MAO-B.

Applications 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)

(R)-Lercanidipine hydrochloride is the R-enantiomer of Lercanidipine. (R)-lercanidipine hydrochloride is a blocker of calcium channel.

Dantrolene depresses excitation-contraction coupling in skeletal muscle by binding to the ryanodine receptor 1 and decreasing intracellular calcium

UK51656 is an antagonist of calcium (IC50: 4 nM).

Temiverine hydrochloride is a potential calcium channel antagonist with anticholinergic effects that inhibits some of the functions of atropine.

5,5-Dimethyloxazolidine-2,4-dione (Dimethadione) is an anticonvulsant that is the active metabolite of TRIMETHADIONE.

Strontium ranelate (S12911), a strontium (II) salt of the ranelic acid, is a medication for osteoporosis and can slow the course of osteoarthritis of the knee.

Thapsigargin is a natural product, an inhibitor of sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA) and an endoplasmic reticulum stress inducer.

Applications A labelled 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),

EMD57033 activates cardiac troponin C, enhances Ca2+ sensitivity to boost heart contraction.

Bepridil hydrochloride (CERM 1978) is a calcium channel blocker and also inhibits Na+/Ca2+ exchange (NCX), sodium channels and cardiac sarcolemmal KATP channels

Sesamodil (SD 3211) is a novel calcium antagonist that can be used to study hypertension.

Zegocractin (CM-4620) is a calcium-release activated calcium-channel (CRAC channel) inhibitor.

Ser-Ala-alloresact acetate is a sperm-activating peptide (SAP) that is released by marine invertebrate eggs and plays an important role in fertilization.

Pyridaben is a METI acaricide that inhibits mitochondrial electron transport at complex I (METI; Ki = 0.36 nmol/mg protein in rat brain mitochondria).

Applications A labelled dihydropyridine calcium channel blocker. It is used as a vasodilator (cerebral). 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),

Halofuginone specifically inhibits collagen type I and MMP-2 gene expression, which may result in the suppression of angiogenesis and tumor cell growth.

Applications 1,3-Dihydroxyacetone Dimer is used in the synthesis of dihydropyrimidine calcium channel blockers. Also used in the preparation of a new antineoplastic and antifilarial agents as anticancer agents. References Atwal, K. et al., J. Med. Chem., 33, 1510 (1990); Ram, S. et al.: J. Med. Chem., 35, 539 (1992);

Tetracaine HCl (Pontocaine), a potent local anesthetic and antipruritic, is used in eye care and for surface/spinal anesthesia.

CRAC intermediate 1 (5-(S)-Fluorowillardiine) is a key intermediate in the chemical synthesis of a series of CRAC channel inhibitors.

NS-638 is a Ca2+-channel blocker. It can block K+-stimulated intracellular Ca2+-elevation (IC50: 3.4 μM).

Cinepazide maleate (MD-67350), a maleate salt form of cinepazide, is a vasodilator.

Bevantolol hydrochloride (NC-1400 hydrochloride) is a β1-adrenoceptor antagonist that treatment angina pectoris and hypertension.

Propiverine is a widely used antimuscarinic drug with a mixed mode of action in the treatment of symptoms associated with overactive bladder (OAB).

β-Amino Acid Imagabalin Hydrochloride is the voltage-dependent calcium channel ligand for the α2δ subunit.

Ebselen is a selenium compound with anti-inflammatory and antioxidant properties, mimicking glutathione peroxidase to protect against ROS damage.

Clopimozide (R-29764), a long-acting oral antischizophrenic, blocks calcium channels and [3H] nilandipine binding.