Calcium Channel Inhibitor

Fantofarone (Standard) is the analytical standard of Fantofarone. This product is intended for research and analytical applications. Fantofarone is a highly potent Calcium Channel antagonist.

Suvecaltamide (Standard) is the analytical standard of Suvecaltamide (HY-101096). This product is intended for research and analytical applications. Suvecaltamide (MK-8998) is a selective T-type calcium channel inhibitor with oral efficacy. Suvecaltamide exhibits no cytotoxicity in myeloma cell lines and does not affect the antitumor efficacy of Bortezomib (BTZ). Suvecaltamide reverses BTZ-induced peripheral neuropathy (CIPN) in mouse and rat models, and helps inhibit myeloma growth.

Topiramate-¹³C (McN 4853-¹³C) is ¹³C labeled Topiramate. 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.

(2R,3R)-Diltiazem hydrochloride is an isomer of Diltiazem (HY-B0632) hydrochloride. 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.

Bepridil hydrochloride (Standard) (CERM 1978 (Standard);Org 5730 hydrochloride (Standard)) is the analytical standard of Bepridil hydrochloride (HY-103315). This product is intended for research and analytical applications. Bepridil hydrochloride is an orally active non-selective calcium channel antagonist with multi-ion channel blocking activity. Bepridil hydrochloride modulates Calmodulin, the 20S proteasome, T-type/L-type calcium channels, cardiac sodium channels, multiple potassium channels, γ-secretase, β-secretase, and mitoK_ATP/sarcK_ATP channels. Bepridil hydrochloride acts as a hydroxyl radical scavenger, regulates mitochondrial and intracellular calcium handling, and exerts antiarrhythmic, antianginal, and cardioprotective effects. Bepridil hydrochloride alters amyloid precursor protein processing, reduces β-amyloid and thalamic calcium levels, restores seladin-1/DHCR24 expression, and improves sensorimotor recovery after cerebral ischemia. Bepridil hydrochloride also exhibits potent inhibitory effects on SARS-CoV-2 replication. Bepridil hydrochloride is used in studies related to stable angina, arrhythmias, cerebral ischemia, Alzheimer's disease, and SARS-CoV-2 infection.

Efonidipine (NZ-105) hydrochloride is an orally active dual L-type and T-type calcium channel blocker (CCB) with IC₅₀ values of 1.8 and 350 nM, respectively. Efonidipine hydrochloride inhibits SARS-CoV-2 main protease. Efonidipine hydrochloride modulates adrenal steroidogenesis by increasing the expression of steroidogenic acute regulatory protein (StAR), dbcAMP-or angiotensin II-induced StAR mRNA expression and DHEA-S production, while suppressing the biosynthesis of aldosterone and cortisol. Efonidipine hydrochloride reduces plasma aldosterone levels in vivo. Efonidipine hydrochloride improves cardiac function in heart failure models by inhibiting T-type calcium channels (via both tonic and use-dependent blockade), independently of blood pressure reduction. Efonidipine hydrochloride can be used for research in hypertension, heart failure, and disorders involving dysregulated steroid hormone synthesis.

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

trans-Ned 19 (Standard) is the analytical standard of trans-Ned 19 (HY-103316). This product is intended for research and analytical applications. trans-Ned 19 is a NAADP antagonist and TPC blocker. trans-Ned 19 suppresses the calcium signal and the rat aorta relaxation in response to low histamine concentrations. trans-Ned 19 increases the spontaneous acrosome reaction rate, alleviates anti-CD3 mAb-induced intestinal inflammation, and improves kidney damage in mice with nephrotoxic serum nephritis.

Lacidipine (Standard) is the analytical standard of Lacidipine. This product is intended for research and analytical applications. Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI).

Ethaverine hydrobromide is a Papaverine derivative and vasodilator. Ethaverine hydrobromide inhibits Phosphodiesterase, Tyrosine hydroxylase, and MAO-B. Ethaverine hydrobromide blocks L-type Ca²⁺ channels, reduces intracellular Ca²⁺ levels, inhibits platelet adhesion and aggregation, regulates cardiac conduction and heart rate, and increases peripheral and cerebral blood flow. Ethaverine hydrobromide alters cochlear microcirculation, intracochlear Po₂, CM potential, and EP in guinea pigs, and induces transient hypotension. Ethaverine hydrobromide is used in the research of peripheral vascular diseases.

Kadethrin is a synthetic pyrethroid that acts as an insecticide. Kadethrin can affect the binding of [3H] full-histamine toxin ([3H]H12-HTX) to the nicotinic acetylcholine (Ach) receptor/channel binding sites, and it inhibits the Ca²⁺ flux through the receptor ion channels.

Diltiazem-d₄ is deuterium labeled Diltiazem. 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.

Norfluoxetine oxalate is the active metabolite of the antidepressant Fluoxetine (HY-B0102); it is also a TREK-2 K₂P potassium channel inhibitor. Norfluoxetine oxalate exhibits neuroimmunological activity, induces apoptosis in primary microglial cells, and inhibits the release of pro-inflammatory factors. Norfluoxetine oxalate inhibits high-threshold voltage-gated Ca²⁺ currents in neurons with an EC₅₀ of 20.4 μM. Norfluoxetine oxalate can be used in research related to depression, ischemic stroke, and epilepsy.

LY393615 (NCC1048) free base is a novel neuronal Ca²⁺ (calcium channel) and Na ⁺ channel (sodium channel) blocker with IC₅₀s of 1.9 μΜ and 5.2 μΜ for α1A and α1B calcium channel subunits. LY393615 free base has good brain penetration and neuroprotective effects in models of in cerebral ischemia that can be used for neurological disease research.

MRS 1523 (Standard) is the analytical standard of MRS 1523. This product is intended for research and analytical applications. MRS 1523 is a potent and selective adenosine A3 receptor antagonist with Ki values of 18.9 nM and 113 nM for human and rat A3 receptors, respectively. In rat this corresponds to selectivities of 140- and 18-fold vs A1 and A2A receptors, respectively. MRS 1523 can exert antihyperalgesic effect through N-type Ca channel block and action potential inhibition in isolated rat dorsal root ganglion (DRG) neurons.

Bepridil-d₅ hydrochloride (CERM 1978-d₅; Org 5730-d₅ hydrochloride) is the deuterated-labeled Bepridil hydrochloride (HY-103315). Bepridil hydrochloride (CERM 1978; Org 5730 hydrochloride) is an orally active non-selective calcium channel antagonist with multi-ion channel blocking activity. Bepridil hydrochloride modulates Calmodulin, the 20S proteasome, T-type/L-type calcium channels, cardiac sodium channels, multiple potassium channels, γ-secretase, β-secretase, and mitoK_ATP/sarcK_ATP channels. Bepridil hydrochloride acts as a hydroxyl radical scavenger, regulates mitochondrial and intracellular calcium handling, and exerts antiarrhythmic, antianginal, and cardioprotective effects. Bepridil hydrochloride alters amyloid precursor protein processing, reduces β-amyloid and thalamic calcium levels, restores seladin-1/DHCR24 expression, and improves sensorimotor recovery after cerebral ischemia. Bepridil hydrochloride also exhibits potent inhibitory effects on SARS-CoV-2 replication. Bepridil hydrochloride is used in studies related to stable angina, arrhythmias, cerebral ischemia, Alzheimer's disease, and SARS-CoV-2 infection.

Nesapidil is an antiarrhythmic agent and calcium channel blocker. Nesapidil slows calcium channel activity, which in turn causes slowing of atrioventricular conduction and sinus heart rate. Nesapidil alters preload, afterload, contractility, and coronary blood flow. Nesapidil can be used in research related to arrhythmia and hypertension.

Flunarizine (Standard) is the analytical standard of Flunarizine. This product is intended for research and analytical applications. Flunarizine is a potent dual Na⁺/Ca²⁺ channel (T-type) blocker. Flunarizine is a D₂ dopamine receptor antagonist. Flunarizine shows anticonvulsive and antimigraine activity, and peripheral vasodilator effects.

Nisoldipine-d₄ (BAY-k 5552-d₄) is the deuterium labeled Nisoldipine. Nisoldipine(BAY-k 5552) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC₅₀ of 10 nM.

Diproteverine (BRL 40015) is an oral activity calcium channel blocker. Diproteverine embryonic toxicity. Diproteverine also shows antianginal properties.