Calcium Channel Inhibitor

CPU-228 is a complex class III antiarrhythmic agent. CPU-228 concentration-dependently blocks the activities of the rapid component 50 of the delayed rectifier potassium channel (I_Kr) and the L-type calcium channel (I_Ca,L), with an IC₅₀ value of 0.909 μM for I_Ca,L current. CPU-228 produces negative inotropic effects and induces mild, non-frequency-dependent prolongation of the effective refractory period (ERP) in isolated left atria. CPU-228 reduces the incidence of torsades de pointes (TDP) in anesthetized rabbits and inhibits ischemia/reperfusion-induced arrhythmias in rats. CPU-228 can be used in studies related to torsades de pointes.

Levomepromazine (Methotrimeprazine) hydrochloride is an orally active antipsychotic compound and Ca²⁺ release inducer. Levomepromazine inhibits SERCA pump and induces an increase in cytoplasmic Ca²⁺ levels. Levomepromazine hydrochloride has antagonistic effects on a variety of neurotransmitter receptors, including dopamine, cholinergic, serotonin, and histamine receptors. Levomepromazine hydrochloride can induce adaptive ER stress and autophagy. In addition, Levomepromazine hydrochloride has antiviral, anti-inflammatory, neuroprotective and analgesic, sedative and anti-injurious activities. Levomepromazine hydrochloride can be used in the study psychiatric disorders and relieving nausea and vomiting.

Ancitabine (hydrochloride) (Standard) is the analytical standard of Ancitabine (hydrochloride). This product is intended for research and analytical applications. 0

SQ-31765 is a benzazepine calcium channel blocker.

Tamolarizine is a calcium channel blocker. Tamolarizine crosses the blood-brain barrier and antagonizes the effects of calcium on neurons. Tamolarizine can be used in nervous system research.

Dantrolene (Standard) is the analytical standard of Dantrolene. This product is intended for research and analytical applications. Dantrolene is an orally active, non-competitive glutathione reductase inhibitor with a Ki of 111.6 μM and an IC₅₀ of 52.3 μM. Dantrolene is a ryanodine receptor (RyR) antagonist and Ca2+ signaling stabilizer. Dantrolene is a direct-acting skeletal muscle relaxant. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome.

Thapsigargin (Standard) is the analytical standard of Thapsigargin (HY-13433). This product is intended for research and analytical applications. Thapsigargin, an endoplasmic reticulum (ER) stress inducer, is an inhibitor of microsomal Ca²⁺-ATPase. Thapsigargin efficiently inhibits coronavirus (HCoV-229E, MERS-CoV, SARS-CoV-2) replication in different cell types.

Nicardipine-d₄ hydrochloride is deuterated labeled Nicardipine hydrochloride (HY-12515A). Nicardipine hydrochloride (YC-93) is a calcium channel blocker with an IC₅₀ of 1 μM for blocking cardiac calcium channels. Nicardipine hydrochloride acts as an agent for chronic stable angina and for controlling blood pressure.

(-)-Denudatin B is an antiplatelet agent. (-)-Denudatin B relaxed vascular smooth muscle by inhibiting the Ca2+ influx through voltage-gated and receptor-operated Ca2+ channels. And (-)-Denudatin B has nonspecific antiplatelet action

Ranolazine-d₅ is the deuterium labeled Ranolazine. Ranolazine (CVT 303) is an anti-angina drug 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.

Pincainide is a calcium channel inhibitor. Pincainide inhibits voltage-gated calcium channel-mediated calcium influx in smooth muscle. Pincainide inhibits norepinephrine- and high potassium-induced contractile responses. Pincainide can be used in the research of heart diseases.

(R)-lercanidipine D₃ hydrochloride is a deuterium labeled (R)-Lercanidipine hydrochloride. (R)-Lercanidipine-d₃ (hydrochloride), the R-enantiomer of Lercanidipine, is a calcium channel blocker.

Cavα2δ1&NET-IN-3 (example 216) is an inhibitor of the subunit α2δ of voltage-gated calcium channels (VGCC) and noradrenaline transporter (NET). Cavα2δ1&NET-IN-3 has K_is of 100-500 nM for human α2δ-1 subunit of Ca_v2.2 calcium channel and NET, respectively.

PptT-IN-4 (Compound 3a) is a PptT inhibitor (IC₅₀: 0.71 μM). PptT-IN-4 inhibits Mtb H37Rv with a MIC value of 42 μM. PptT-IN-4 also inhibits hERG, hCav1.2, and hNav1.5 channels with IC₅₀s of 11 μM, 8.1 μM, 6.9 μM respectively.

RWJ 22108 is a bronchoselective calcium channel blocker, with the IC₅₀ of 5.7 nM in calcium-dependent contraction of canine bronchiolar smooth muscle.

14-Deoxyandrographolide (Standard) is the analytical standard of 14-Deoxyandrographolide. 14-Deoxyandrographolide is a diterpene with calcium channel blocking activity and acts as a uterine smooth muscle relaxant. 14-Deoxyandrographolide stimulates the release of nitric oxide (NO) in endothelial cells. 14-Deoxyandrographolide gradually desensitizes liver cells to TNF-α mediated apoptosis by inducing the release of TNFRSF1A.

Halofuginone hydrochloride (Standard) (RU-19110 hydrochloride (Standard)) is the analytical standard of Halofuginone hydrochloride (HY-N1584B). This product is intended for research and analytical applications. 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.

α-Obscurine derivative-1 (Compound 7) is a α-Obscurine (HY-134036) derivative. α-Obscurine derivative-1 inhibits Ca_V3.1 ion channel current with an IC₅₀ of 0.19 μM. α-Obscurine derivative-1 can be used in the research of neurological disorders.

BGC-201259 (RS-1259) is an orally active inhibitor that simultaneously targets acetylcholinesterase (AChE) (IC₅₀ = 101 nM) and serotonin transporter (SERT) (IC₅₀ = 42 nM). BGC-201259 inhibits 5-HT receptor with an IC₅₀ of 90 nM. BGC-201259 exhibits strong weak activity against the NA transporter (IC₅₀ = 7.7 μM), L-type calcium channel (IC₅₀ = 3.6 μM), σ receptor (IC₅₀ = 2 μM), and sodium channel (IC₅₀ = 5.1 μM). BGC-201259 demonstrates synergistic potential in improving cognitive and emotional symptoms by balancing the inhibition of these two targets. BGC-201259 can be used in research on Alzheimer's disease.

ATI22-107 is a dual-pharmacophore compound designed to simultaneously inhibit cardiac phosphodiesterase (PDE-III) and L-type calcium channels (LTCC), with activity that has specific effects on calcium cycling and contractility in cat ventricular myocytes and trabeculae.