Calcium Channel Inhibitor

Manidipine (dihydrochloride) (Standard) is the analytical standard of Manidipine (dihydrochloride). This product is intended for research and analytical applications. 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.

Levamlodipine besylate Hemipentahydrate is an orally active L-type calcium channel blocker and MMP-9 modulator with high permeability and retention properties. Levamlodipine besylate Hemipentahydrate significantly enhances plaque stability and improves lipid profiles by reducing blood pressure, decreasing systolic blood pressure variability, and inhibiting MMP-9 expression in atherosclerotic plaques. Levamlodipine besylate Hemipentahydrate not only alleviates cardiac and aortic hypertrophy and prevents renal atrophy, but also produces synergistic effects in blood pressure reduction and organ protection when combined with bisoprolol (HY-129029). Levamlodipine besylate Hemipentahydrate exerts no significant inhibitory effect on abdominal aortic intimal hyperplasia. When excessively accumulated in the epidermis, Levamlodipine besylate Hemipentahydrate may induce changes in keratin structure, impair the skin barrier and trigger inflammation; long-term use further exacerbates skin irritation caused by local administration. Levamlodipine besylate Hemipentahydrate can be used in research related to hypertension and atherosclerosis.

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

Cilnidipine-d₄ (FRC-8653-d₄) is deuterium labeled Cilnidipine. Cilnidipine is a long-acting, second-generation dihydropyridine Ca²⁺-channel blocker on L and N-type Ca²⁺ channel. Antihypertensive effects.

Almorexant (Standard) is the analytical standard of Almorexant. This product is intended for research and analytical applications. Almorexant (ACT 078573) is an orally active, potent and competitive dual orexin receptor antagonist, with Kd 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 .

(-)-SA2572 is an orally active Ca²⁺ inward channel inhibitor. (-)-SA2572 inhibits the slow Ca²⁺ inward channel and the fast Na⁺ inward channel. (-)-SA2572 inhibits depolarization-induced contraction of gastrointestinal smooth muscle and vascular smooth muscle, prolongs atrioventricular nodal conduction time, and inhibits His bundle-ventricular conduction time. (-)-SA2572 reduces systolic blood pressure in spontaneously hypertensive rats. (-)-SA2572 can be used in the research of hypertension.

Dronedarone (Standard) is the analytical standard of Dronedarone. This product is intended for research and analytical applications. Dronedarone (SR 33589), a derivative of amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone is a substrate for and a moderate inhibitor of CYP3A4.

HA-1004 dihydrochloride is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 dihydrochloride is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 dihydrochloride is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models.

Gabapentin (hydrochloride) (Standard) is the analytical standard of Gabapentin (hydrochloride). This product is intended for research and analytical applications. Gabapentin hydrochloride is a potent, orally active P/Q type Ca2+ channel blocker. Gabapentin hydrochloride inhibits neuronal Ca2+ influx and reduction of neurotransmitter release. Gabapentin hydrochloride is a GABA analog that can be used to relieve neuropathic pain.

PD 122860 is a calcium channel blocker. PD 122860 also can stimulate sodium channel. PD 122860 can be used for the research of cardiovascular and cerebrovascular diseases.

Nicardipine (Standard) is the analytical standard of Nicardipine. This product is intended for research and analytical applications. Nicardipine (YC-93 free base) is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine acts as an agent for chronic stable angina and for controlling blood pressure.

Psoralenoside is a benzofuran glycoside from Psoralea corylifolia. Psoralenoside exhibits high binding affinities against histaminergic H1, calmodulin, and voltage-gated L-type calcium channels (E-value≥-6.5 Kcal/mol). Psoralenoside shows estrogen-like activity, osteoblastic proliferation accelerating activity, antitumor effects and antibacterial activity.

Diltiazem (Standard) is the analytical standard of Diltiazem. This product is intended for research and analytical applications. 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.

NAADP receptor modulator-1 is a cell-permeable NAADP receptor modulator. NAADP receptor modulator-1 competes with NAADP for binding sites and inhibits NAADP-induced Ca²⁺ release.

Verticilide is a ryanodine-binding inhibitor and inhibits ryanodine binding to ryanodine receptors in the cockroach at an IC₅₀ value of 4.2 μM (whereas inhibition against mouse ryanodine receptors was weak (IC₅₀=53.9 μM)).

1-Octanol-d₂-1 is deuterated labeled 1-Octanol (HY-W032013). 1-Octanol (Octanol), a saturated fatty alcohol, is a T-type calcium channels (T-channels) inhibitor with an IC50 of 4 μM for native T-currents. 1-Octanol is a highly attractive biofuel with diesel-like properties.

Triphenylethylene is an aromatic hydrocarbon that possesses weak estrogenic activity. Triphenylethylene antiestrogens relax duodenal intestinal muscle via a mechanism that involves inhibition of L-type Ca²⁺ channels but not activation of K⁺ channels.

Manidipine-d₄ is the deuterium labeled Manidipine (HY-B0419). Manidipine is an orally active calcium channel antagonist. Manidipine regulates the expression of cytokines (IL-1β, IL-6). Manidipine has a hypotensive effect. Manidipine can be used in the study of cardiovascular diseases (such as hypertension, myocardial ischemia-reperfusion injury, ventricular hypertrophy), kidney diseases (such as glomerular diseases), and epilepsy.

Clonixin (SCH-10304) (Standard) is the analytical standard of Clonixin. This product is intended for research and analytical applications. Clonixin is an orally active non-steroidal anti-inflammatory agent (NSAID) that inhibits COX synthesis. Clonixin acts as a voltage-gated L-type calcium channel blocker, exerts vasodilatory effects by antagonizing Ca²⁺ in vascular smooth muscle. Clonixin inhibits TGF-β, reduces lung coefficient, immune cell infiltration level, oxidative stress response, airway resistance, hydroxyproline content and collagen deposition. Clonixin can be used in research related to inflammation such as idiopathic pulmonary fibrosis and moderate to severe pain.

Isradipine (Standard) is the analytical standard of Isradipine. This product is intended for research and analytical applications. Isradipine (PN 200-110) is an orally active 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.