Calcium Channel

DS16570511 is a novel, cell-permeable inhibitor targeting the mitochondrial calcium uniporter.

SERCA2a activator 1 boosts heart function by reducing phospholamban restraint and enhancing cardiac contraction-relaxation cycles.

PD 0299685 is a potent α2δ ligand of the Ca2+ channel for the treatment of interstitial cystitis.

Drotaverine hydrochloride is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor,and is an antispasmodic drug, used to enhance cervical dilation

PD 173212 is a blocker that blocks N-type voltage sensitive calcium channel (Cav2.2).

Jamaicin (AnCoA4), an isoflavone derived from the chickweed plant, is an inhibitor of the STIM1-Orai1 channel that blocks calcium ion influx.

SR33805 is a potent antagonist of Ca2+ channel(EC50s of 4.1 nM and 33 nM in depolarized and polarized conditions, respectively)

MRS1845 is a selective inhibitor of store-operated calcium (SOC) channel (IC50 of 1.7 μM).

GSK205 is a selective TRPV4 antagonist (IC50: 4.19 μM) for inhibiting TRPV4-mediated Ca2+ influx.

Fasudil hydrochloride (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively.

Applications (Z)-Methyl 2-(3-Nitrobenzylidene)-3-oxobutanoate is an intermediate in the synthesis of Lercanidipine-d3 Hydrochloride (L179002), a labelled dihydropyridine calcium channel blocker. References Bianchi, G., et al.: Pharmacol. Res., 21, 193 (1989); Rimoldi, E., et al.: Acta Therap., 200, 23 (1994)

Applications rac Atomoxetine-d5 Hydrochloride is labelled rac Atomoxetine Hydrochloride (A791390) which is 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),

CDN1163 is a small molecule activator of sarco/endoplasmic reticulum Ca2+-ATPase (SERCA).

Suvecaltamide (MK-8998) as potent inhibitors of T-type calcium channels.

LY393615 (NCC1048) is a novel blocker of both neuronal Ca²⁺ (calcium) and Na⁺ (sodium) channels, exhibiting half-maximal inhibitory concentrations (IC₅₀) of 1.9

Applications Verapamil-d3 Hydrochloride is the labeled analogue of Verapamil Hydrochloride (V125000), which is a calcium channel blocker, antihypertensive, antianginal, and 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)

Applications Paxilline is a indole-diterpenes and a potent inhibitor of large conductance Ca2+-activated K+ currents in vascular smooth muscle cells 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 Tagami, K., et al.: J. Am. Chem. Soc. 35, 260 (2013); Li, G. and Cheung, W. Eur. J. Pharmacol 372, 103 (1999);

Applications Desacetyl Diltiazem Hydrochloride is 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)

Ruthenium Red (Ammoniated ruthenium oxychloride) is a polycationic dye widely used for electron microscopy (EM) of cells, tissues and vegetative bacteria.

Impurity Flumazenil EP Impurity B Stability Hygroscopic Applications Defluoro Flunarizine (Flumazenil EP Impurity B) Dihydrochloride, is an impurity of Flunarizine(F455200, Dihydrochloride), which is a calcium channel blocker. Flunarizine is a fluorinated derivative of Cinnarizine and a vasodilator (cerebral and peripheral). 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)

HA-1004 dihydrochloride is an inhibitor of PKA, PKC, cGKI, MYLK, and calcium channel protein

Verapamil hydrochloride (Verapamil HCl) is a calcium channel blocker that is a class IV anti-arrhythmia agent.

Penfluridol (TLP-607) is a highly potent antipsychotic.

Upacicalcet (AJT-240) is a calcium mimetic for SHPT in dialysis, reducing PTH by targeting parathyroid receptors.

Gabapentin hydrochloride (Neurontin HCl) is a GABA analogue, used to treat seizures and neuropathic pain.

TTA-A2: T-type calcium channel blocker; anticonvulsant targeting Cav3.1, Cav3.2; IC50 of 89/92 nM; potential for treating neurological conditions.

Lacidipine (SN-305) is a slow-acting, long-duration lipophilic dihydropyridine calcium blocker that prevents reflex tachycardia and lowers blood pressure.

Nisoldipine (BAY-k 5552) is a dihydropyridine calcium channel antagonist that acts as a potent arterial vasodilator and antihypertensive agent.

Ethacrynic acid (Edecrin) 是谷胱甘肽 S-转移酶抑制剂,也是NF-κB 信号传导途径的有效抑制剂,并且还调节白三烯的形成。它还可抑制 L 型电压依赖性和储存操作的钙通道,从而导致气道平滑肌细胞松弛。它是利尿剂,具有抗炎特性,可减轻类维生素 A 诱导的小鼠耳部水肿。

Dantrolene sodium treats spasticity by disrupting muscle contraction; not central in action, grouped with central relaxants.

GSK1016790A (GSK101) (GSK101) is a novel, potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34 nM in choroid plexus epithelial

14-Deoxyandrographolide is a bioactive compound of Andrographis paniculata with hepatoprotective efficacy.

Urolithin C is a gut metabolite of ellagic acid. Urolithin C induces apoptosis in PC12 cells through a mitochondria-mediated pathway.

Dehydronitrosonisoldipine blocks SARM1, slows axon decay & cADPR synthesis; useful in neurodegeneration research.

Applications Felodipine-13C4, d3 is the labeled analogue 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)

Pinocembrin chalcone: tyrosinase inhibitor, antimutagenic, aids in gastric ulcer prevention studies.

MDK-4025 is an inhibitor of the high voltage-activated (HVA) Ca2+ current in pyramidal neurons.

Applications A piperidine derivative as calcium channel blockers. 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 McMahon, R. E. , et al.: J. Med. Chem., 22, 1100 (1979),

Ca2+ channel agonist 1 activates N-type Ca2+ channels and inhibits Cdk2 (EC50: 14.23 μM/3.34 μM) for motor nerve issues.

L-Ascorbic acid sodium salt (Vitamin C sodium salt) is a more bioavailable form of vitamin C that is an alternative to taking ascorbic acid as a supplement.

8-Bromo-cGMP sodium: PKG activator, eases pain, dilates vessels, reduces Ca2+ currents & insulin release.

Fenoverine (Spasmopriv) has antispasmodic activity and can be used to study gastrointestinal spasms.

2,3-Dihydroxy-4-methoxyacetophenone (2',3'-Dihydroxy-4'-methoxyacetophenone) is a natural product,it improves cognitive function and may be helpful for the

Stability Light Sensitive Applications 1R,3R,αR-Deltamethrin is an isomer of Deltamethrin (D230700), a 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),

18:0 LYSO-PE is a compound that induces an increase in [Ca2+]i and can be used as a phospholipid (PL) standard for lipid analysis by electrospray mass spectrometry (ESI-MS)/MS.

TMDJ-035 is a selective inhibitor of the RyR2 (ryanodine receptor 2).

Emopamil, a calcium channel inhibitor, reduces neuronal damage caused by ischemia.

Trimethadione (3,5,5,-Trimethyloxazolidine-2,4-dione) is a dione-type anticonvulsant with antiepileptic activity.