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.

Ned 19 inhibits tumor growth, vascularization, lung metastases in mice, and is a selective NAADP antagonist.

NecroX-5, a derivative of NecroX, exhibits anti-inflammatory and anti-cancer activities. NecroX-5 reduces intracellular calcium concentration.

ORM-10103 is a novel potent and selective inhibitor of the Na+/Ca2+ exchanger (NCX).ORM-10103 inhibited NCX currents with estimated IC50 values of 55 and 67 nM

Applications Inhibits the catalytic activities of several protein kinases competitively with respect to ATP and exhibited different Ki values toward each protein kinase. Also found to be a new type of vascular relaxant. References Hidaka, H., et al.: J. Biol. Chem., 262, 16, 7796 (1987)

Vatanidipine (AE0047) is a novel dihydropyridine (DHP)-type calcium channel blocker with slow-onset pharmacological actions.A slow-onset and long-lasting

1-Octanol is a saturated fatty alcohol, inhibits T-type Ca²⁺ channels with a 4 μM IC50, and is a potential diesel-like biofuel.

Manidipine dihydrochloride (Manidipine 2HCl) is a potent calcium channel blocker for Ca2+ current(IC50=2.6 nM).

Linoleic Acid Amide (Linoleamide) is derived from linoleic acid and regulates Ca2+ flux by inhibiting the sarco/endoplasmic reticulum Ca2+-ATPase.

Nicardipine hydrochloride is a potent calcium channel blocker used to dilate cerebral and coronary vessels.

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. 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),

Applications tert-Butyl 3-Aminopropyl(methyl) Carbamate acts as a reagent for dihydroquinazoline derivatives preparation and antitumor activities, induction of apoptosis in human lung adenocarcinoma A549 cells by T-type calcium channel antagonist. References Choi, D. L., et al.: Bioorg. Med. Chem. Lett. 24, 1565 (2014); Byun, J. S., et al.: Bioorg. Med. Chem. Lett., 26, 1073 (2016);

1.

Mibefradil is a calcium channel blocker with moderate selectivity for T-type Ca2+ channels (IC50s: 2.7 μM and 18.6 μM for T-type and L-type currents).

Nicardipine (Cardene), a calcium channel blockers belonging to the dihydropyridine class, is a drug used to treat angina and high blood pressure.

Maresin 1 is biosynthesized by macrophages (MΦ) and possesses significant anti-inflammatory activity that attenuates LPS-induced lung injury in mice.

Opc 8490 is a cardiotonic agent and a positive inotropic vasodilator, which prolongs the atrial action potential in a concentration-dependent manner.

Catharanthine ((+)-3,4-Didehydrocoronaridine) suppresses nicotinic receptor-mediated diaphragm contractions (IC50=59.6 μM).

Teludipine hydrochloride is a blocker of lipophilic calcium channel.

McN5691 is a voltage sensitive calcium channel blocker.

Nilvadipine (FK235), a calcium channel blocker (CCB), is utilized for treatment of hypertension.

Applications Dihydrocinnamyl Cilnidipine is a metabolite of Cilnidipine (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)

CP-060 is a potent Ca2+ antagonist and inhibits Ca2+ overload with antioxidant and cardioprotective activities.

TTA-Q6 is a T-type Ca2+ channel antagonist that inhibits the uptake of extracellular calcium ions by tumour cells for the treatment of neurological diseases.

PptT-IN-4 (Compound 3a) is a PptT inhibitor exhibiting an IC50 of 0.71 μM.