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.

Applications 2-[(3-Nitrophenyl)methylene]-3-oxo-butanoic Acid 2-[(3,3-Diphenylpropyl)methylamino]-1,1-dimethylethyl Ester Hydrochloride is an intermediate in synthesizing 5-Ethyl-demethyl Lercanidipine (E913200), which is an impurity of Lercanidipine (L179000), 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);

Stability Hygroscopic Applications 4-Defluoro 2-Fluoro Flunarizine 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)

Amlodipine (UK-48340) is a synthetic dihydropyridine and a calcium channel blocker with antihypertensive and antianginal properties.

Brompheniramine maleate (Dimotane) is an antagonist against histamine H1 receptors.

Hexadecylphosphoserine is a type of phospholipid molecule that incorporates a long-chain alkyl group (hexadecyl) and a phosphatidylserine group, granting it high affinity for cell membranes. This compound exhibits antitumor activity by modulating [Ca++]i and related signaling pathways, making it useful for breast cancer research.

AChE/BChE-IN-21 is an antagonist of the histamine H3 receptor, a calcium channel blocker, and an acetylcholinesterase inhibitor. It exhibits neuroprotective activities against H2O2 and Aβ1-40, and can restore cognitive functions in AD mice.

Bay K 8644 (SQ 28,873) is a potent, selective activator of L-type Ca2+ channel with IC50 of 17.3 nM.

Norfluoxetine Hydrochloride (Norfluoxetine HCl) is an active metabolite of fluoxetine. Fluoxetine is an antidepressant drug.

Applications A novel calcium channel antagonist; cardiovascular agent. References Matsumori, A., et al.: Circulation, 66, 355 (1982), Roberts, W., et al.: Am. J. Cardiol., 60, 1340 (1987), Uehara, Y., et al.: J. Cardiovasc. Pharmacol., 23, 970 (1994), Kim, C., et al.: Cardiovasc. Drugs Ther., 13, 455 (1999), Watanabe, K., et al.: Br. J. Pharmacol., 130, 1489 (2000),

Cinnarizine is a piperazine, blocks H1-receptor & Ca-channels, has vasodilating & antiemetic effects, may cause Parkinson-like symptoms.

Stability Light Sensitive Applications Z-Isomer of Lacidipine; 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),

Lifarizine (RS-87476), a calcium-sodium channel antagonist, shows neuroprotective activity in a simplified rat survival model of double vessel occlusion.

Ranolazine (RS 43285-003) inhibits calcium uptake, treats chronic angina by targeting sodium/calcium channels to modulate intracellular sodium.

Applications 1-[(2-Chlorophenyl)phenylmethyl]piperazine is a novel compound derived from the previously reported N-type calcium channel blocker NP118809 (1-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one). References Maggi, C., et al.: Neuroscience, 34, 243 (1990), Evans, A., et al.: Brain Res., 712, 265 (1996), Kerr, L., et al.: Eur. J. Pharmacol., 146, 181 (1998), Hu, L., et al.: Bioorg. Med. Chem. Lett., 9, 907 (1999),

ML218 is an inhibitor of T-type Ca2+ channels (Cav3.1, Cav3.2, Cav3.3).ML218 inhibits the synaptic activity of subthalamic nucleus (STN) neurons.

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

Verapamil (CP-16533-1), an oral calcium channel blocker, inhibits P-gp and CYP3A4, used for hypertension, arrhythmias, and angina research.

Cromolyn sodium (FPL-670) is a chromone complex that acts by inhibiting the release of chemical mediators from sensitized mast cells.

MP-010 is an FKBP12 ligand that regulates cytosolic calcium by stabilizing RyR channel activity. It facilitates functional improvement in SOD1G93A mice with amyotrophic lateral sclerosis (ALS), evidenced by enhanced motor coordination, increased integrity of neuromuscular junctions, and significantly higher spinal motor neuron survival rates. MP-010 is applicable for research in the field of neurological disorders.

Topiramate (RWJ 17021) is a unique antiseizure medication that is used in the treatment of partial and generalized seizures.

Applications Dehydro Amlodipine Besylate is an impurity of Amlodipine (A633495), a dihydropyridine calcium channel blocker; activity resides mainly in the (-)-isomer. References Arrowsmith, J.E., et al.: J. Med. Chem., 29, 1696 (1986); Burges, R.A., et al.: J. Cardiovasc. Pharmacol., 9, 110 (1987); Haria, M., et al.: Drugs, 50, 560 (1995)

Nepetin (6-Methoxyluteolin) has antioxidant activity, it is a potent inhibitor of histamine release and calcium influx via down-regulation of the FcεRI α chain.

Gabapentin (Neurontin) is an Anti-epileptic Agent.

TPC2-A1-P is a TPC2 agonist that can differentially activate two-pore channel 2 (TPC2) and mimic the activation of TPC2 with NAADP and PIP (2).

VU 0240551 is a selective antagonist of neuronal K-Cl cotransporter KCC2 inhibitor with an IC50 of 560 nM. VU 0240551 inhibits L-type calcium channels and hERG.