Calcium Channel Inhibitor

Diltiazem is an orally active L-type Ca²⁺ channel blocker. Diltiazem shows antihypertensive and antiarrhythmic effects. Diltiazem can be used for the research of cardiac arrhythmia, hypertension, and angina pectoris.

GluN1 (356-385) is a polypeptide targeting NMDAR GluN1. GluN1 (356-385) induces the production of autoantibodies, which reduce the density of cell surface NMDAR clusters, impair long-term potentiation, and decrease NMDAR-mediated Ca²⁺ influx. As an immunogen, GluN1 (356-385) induces symptoms similar to anti-NMDAR encephalitis, including memory loss, in mice. GluN1 (356-385) can be used to establish a mouse model that mimics the pathogenesis of anti-NMDAR encephalitis. GluN1 (356-385) is applicable to research related to anti-NMDAR encephalitis.

Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca²⁺ channels, modulating non-selective cation channels (NSC), activating K⁺ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.

NNC 55-0396 (NNC 55-0396 dihydrochloride) is a blood-brain-barrier-permeable T-type Ca²⁺ channel inhibitor and pan-P450 inhibitor. NNC 55-0396 selectively inhibits T-type Ca²⁺ channels, suppresses HIF-1α expression and stability and inhibits Kv currents. NNC 55-0396 reduces brain infarct and attenuates neurological dysfunction. NNC 55-0396 inhibits the activity of multiple P450 enzymes. NNC 55-0396 (free base) can be used for the research of brain injury, hypertension, and glioblastoma.

Isradipine (PN 200-110) is an orally active and blood-brain barrier permeability L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease.

L-Ascorbic acid (Standard) is the analytical standard of L-Ascorbic acid. This product is intended for research and analytical applications. L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Ca_v3.2 channels with an IC₅₀ of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor. L-Ascorbic acid exhibits anti-cancer effects through the generation of reactive oxygen species (ROS) and selective damage to cancer cells.

GSK-7975A is a potent and orally available CRAC channel inhibitor.

Bupivacaine is a NMDA receptor inhibitor. Bupivacaine can block sodium, L-calcium, and potassium channels.Bupivacaine potently blocks SCN5A channels with the IC₅₀ of 69.5 μM. Bupivacaine can be used for the research of chronic pain.

Topiramate (McN 4853) is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase.

Tris(2-chloroethyl) phosphate (TCEP) is a widely used organic phosphorus flame retardant, mainly used as a plasticizer. Tris(2-chloroethyl) phosphate has orally active hepatotoxicity, inducing an increase in reactive oxygen species (ROS) and calcium ions (Ca²⁺) influx, a decrease in mitochondrial membrane potential (△Ψm), and causing DNA damage and cell apoptosis. Tris(2-chloroethyl) phosphate directly binds to FXR, inducing obesity and the formation of fatty liver in mice. Chloroethyl) phosphate activates the TLR4/NF-κB pathway, triggering liver inflammation.

Cilnidipine is a long-acting, second-generation dihydropyridine Ca²⁺-channel blocker on L and N-type Ca²⁺ channel. Antihypertensive effects.

Argireline (Acetyl hexapeptide-3) is a non-toxic, skin-permeable, antiwrinkle peptide. Argireline significantly inhibits Ca²⁺ dependent neurotransmitter release (acetylcholine) at the neuromuscular junction. Argireline has antiwrinkle and anti-aging activity.

Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier.

Ranolazine (CVT 303) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (I_Na and I_Kr with IC₅₀ values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP). Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor. Antianginal agent.

Eloralintide sodium is an Amylin Receptor agonist. Eloralintide sodium selectively activates AMY1R and AMY3R in cells expressing human or rat AMY1R, AMY3R or CTR. Eloralintide sodium activates AMYRs and CTR in rats, inducing a sustained decrease in plasma Ca²⁺ levels. Eloralintide sodium reduces appetite and body weight in both lean and obese rats. Eloralintide sodium can be used for research related to obesity.

TPC2-A1-N is a powerful and Ca²⁺-permeable agonist of two pore channel 2 (TPC2), which plays its role by mimicking the physiological actions of NAADP. TPC2-A1-P reproducibly evokes significant Ca²⁺ responses from TPC2 (EC₅₀=7.8 μM), and the effect can be blocked by several TPC blockers. TPC2-A1-N can be used to probe different functions of TPC2 channels in intact cells.

SG-094 is a potent TPC2 inhibitor with antiproliferative effects. SG-094 can be used for the research of cancer.

Paxilline is an indole alkaloid mycotoxin derived from Penicillium paxilli, which effectively inhibits the BK channel through a channel-blocking mechanism. Paxilline also inhibits sarco/endoplasmic reticulum Ca²⁺-stimulated ATPase (SERCA), with IC₅₀ values ranging from 5 μM to 50 μM for different SERCA isoforms. Paxilline exhibits significant anticonvulsant and neuroprotective effects, as well as certain antioxidant activity.

Almorexant (ACT 078573) is an orally active, potent and competitive dual orexin receptor antagonist, with K_d values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant totally blocked the intracellular Ca²⁺ signal pathway. Almorexant stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis.

Manidipine dihydrochloride is a third-generation, lipophilic, orally active and highly vasoselective calcium channel antagonist (IC₅₀ = 2.6 nM in guinea-pig ventricular cells) and acts as an antihypertensive agent. Manidipine effectively reduces blood pressure as well as improving insulin sensitivity, renal protection, and antiatherosclerotic activity. Manidipine also exerts anti-inflammatory activity mediated by NF-κB and antiviral activity against many flavivirus and negative-strand RNA viruses through the inhibition of calcium channel. Manidipine is widely applied to research of cardiovascular, metabolic disease and infection.