Calcium Channel Inhibitor

ML218 hydrochloride is a potent, selective and orally active T-type Ca²⁺ channels (Cav3.1, Cav3.2, Cav3.3) inhibitor with IC₅₀s of 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively. ML218 hydrochloride inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 hydrochloride has no significant inhibition of L- or N-type calcium channels, K_ATP or hERG potassium channels. ML218 hydrochloride can penetrate the blood-brain barrier.

CHF-6366 is a potent M3 muscarinic antagonist and β2-adrenergic receptors agonist with pK_i values of 10.4 and 11.4, respectively. CHF-6366 is also a weak calcium channel inhibitor (IC₅₀~50 μM). CHF-6366 inhibits bronchoconstriction in guinea pigs. CHF-6366 can be used to research chronic obstructive pulmonary disease (COPD).

Halofuginone hydrochloride (RU-19110 hydrochloride), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a K_i of 18.3 nM. Halofuginone hydrochloride is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone hydrochloride is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca²⁺ channels. Halofuginone hydrochloride has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.

(R)-(-)-Felodipine-d₅ is the deuterium labeled (R)-(-)-Felodipine. (R)-(-)-Felodipine is the S enantiomer of Felodipine. 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.

Norfluoxetine-d5 is the d₅-labeled Norfluoxetine (HY-135556). Norfluoxetine is the active metabolite of the antidepressant Fluoxetine (HY-B0102); it is also a TREK-2 K₂P potassium channel inhibitor. Norfluoxetine exhibits neuroimmunological activity, induces apoptosis in primary microglial cells, and inhibits the release of pro-inflammatory factors. Norfluoxetine inhibits high-threshold voltage-gated Ca²⁺ currents in neurons with an EC₅₀ of 20.4 μM. Norfluoxetine can be used in research related to depression, ischemic stroke, and epilepsy.

Nimodipine-d₇ is the deuterium labeled Nimodipine. Nimodipine (BAY-e 9736) is an orally active, well-tolerated and light-sensitive dihydropyridine calcium antagonist. Nimodipine can be used for the research of cerebrovascular disorders.

Ranolazine-d₃ is the deuterium labeled Ranolazine. Ranolazine (CVT 303) is an anti-angina agent that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr 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.

Ethaverine hydrochloride (Standard) is the analytical standard of Ethaverine hydrochloride (HY-B1440). This product is intended for research and analytical applications. Ethaverine hydrochloride is a Papaverine derivative and vasodilator. Ethaverine hydrochloride inhibits Phosphodiesterase, Tyrosine hydroxylase, and MAO-B. Ethaverine hydrochloride 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 hydrochloride alters cochlear microcirculation, intracochlear Po₂, CM potential, and EP in guinea pigs, and induces transient hypotension. Ethaverine hydrochloride is used in the research of peripheral vascular diseases.

Etripamil (MSP-2017) hydrochloride is a short-acting, L-type calcium channel antagonist that can be used in the study of paroxysmal supraventricular tachycardia (PSVT). Etripamil hydrochloride inhibits calcium influx through slow calcium channels, thereby slowing atrioventricular node conduction and prolonging the atrioventricular node refractory period.

Decumbensine ((+)-Egenine) is a phthalideisoquinoline hemiacetal alkaloid present in Corydalis decumbens. Decumbensine significantly inhibits spontaneous calcium oscillations in primary cultured neocortical neurons, reducing oscillation frequency and amplitude. Decumbensine can be used in studies related to central nervous system diseases, epilepsy and pain.

(-)-Gallopamil (hydrochloride) exerts a selective modulation of the fast voltage-dependent inactivation. (-)-Gallopamil (hydrochloride) inhibits efficiently Cav1.2 constructs formed by β-subunits (promoting fast voltage-dependent inactivation). (-)-Gallopamil (hydrochloride) also accelerates the voltage-dependent phase of I_Ca decay (as well as the voltage-dependent decay of Ba²⁺ currents). (-)-Gallopamil (hydrochloride) is promising for research of antiarrhythmics.

Boldine hydrochloride is an aporphine alkaloid telomerase (telomerase) inhibitor (IC₅₀ of 0.17 μM for TERT) and a pannexin/connexin hemichannel blocker, with oral activity and blood-brain barrier permeability. Boldine hydrochloride inhibits telomerase activity through direct interaction with the telomerase ribonucleoprotein and non-competitive binding near the TERT active site, and downregulates hTERT mRNA while shifting alternative splicing toward non-functional transcripts. Boldine hydrochloride blocks Panx1, Cx43, Cx26, and Cx30 hemichannels as well as P2X7 receptor-mediated calcium influx. Boldine hydrochloride exhibits antioxidant, anti-inflammatory, antiproliferative, and cytotoxic activities by scavenging ROS, inhibiting NFκB, dephosphorylating SGK1, and reducing TNF-alpha levels. Boldine hydrochloride can be used in research on breast cancer, Alzheimer's disease, glioblastoma, diabetes, and spinal cord injury.

Topiramate (McN 4853) lithium is a broad-spectrum antiepileptic agent. Topiramate lithium 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.

Lacidipine-¹³C₄ is ¹³C labeled Lacidipine (HY-B0347). 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).

JNJ-26489112, a CNS-active agent, exhibits broad-spectrum anticonvulsant activity in rodents against audiogenic, electrically-induced, and chemically-induced seizures. JNJ-26489112 inhibits voltage-gated Na⁺ channels and N-type Ca²⁺ channels, and is effective as a K⁺ channel opener. JNJ-26489112 has very weak inhibition of CA-II (IC₅₀=35 μM) and CA-I (18 μM).

UK-59811 hydrochloride, a Br-dihydropyridine derivative, is a potent bacterial homotetrameric model voltage-gated Ca²⁺ (Ca_V) channel Ca_VAb inhibitor with an IC₅₀ of 194 nM.

IAA65 is a potent T-type calcium channel inhibitor with a IC₅₀ value of 18.9 µM. IAA65 can be used for epilepsy research.

RCC-36 hydrochloride is an L-type calcium channel inhibitor and competitive muscarinic receptor antagonist. RCC-36 hydrochloride inhibits L-type calcium currents in voltage- and concentration-dependent fashion with no effect on cardiac K⁺ currents. RCC-36 hydrochloride suppresses maximum acetylcholine-induced contractile responses, inhibits detrusor muscle contractions induced by potassium chloride, calcium chloride, and electric field stimulation, including atropine-resistant contractions. RCC-36 hydrochloride can be used for the research of urinary frequency, urinary incontinence, and bladder overactivity.

CTP-amiodarone is a cell-penetrating conjugate of cardiomyocyte targeting peptide and Amiodarone (HY-14187). CTP-amiodarone exhibits antiarrhythmic efficacy through block of Na+, K+, Ca2+ channels and β-adrenergic receptors.

Niludipine (Bay a 7168) is an orally active calcium channel blocker and vasodilator with antihypertensive effects. Niludipine can improve early fatal ventricular arrhythmias induced by acute myocardial ischemia in rats. Niludipine can reduce left ventricular systolic and diastolic loads during pacing-induced angina pectoris. Niludipine can be used in the research of cardiovascular diseases such as coronary heart disease and myocardial ischemia.