Calcium Channel Inhibitor

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.

RyR1-IN-1 (Compound 1) is a RyR1 inhibitor with an IC₅₀ of 12 nM. RyR1-IN-1 blocks Ca²⁺ release and inhibits muscle tetany caused by caffeine and heat stress. RyR1-IN-1 can completely prevent the increase in body temperature and death caused by isoflurane and heat stress. RyR1-IN-1 can be used for the study of heat stroke.

UR 8225 is an orally active ATP-sensitive K⁺ channel activator with vasodilator, smooth muscle relaxant, antihypertensive, and bronchodilator activities. UR 8225 induces membrane hyperpolarization by increasing outward K⁺ conductance and reduces Ca²⁺ influx through voltage-gated L-type Ca²⁺ channels. UR 8225 reduces total peripheral vascular resistance, shortens cardiac action potential duration, inhibits agonist-induced Ca²⁺ influx, and stimulates renin release. UR 8225 induces reflex tachycardia but lacks β-adrenergic receptor blocking activity. UR 8225 is widely applicable to research in fields related to hypertension, myocardial ischemia, ventricular fibrillation, and other conditions.

Cerebellin is a neuromodulatory hexadecapeptide that serves as a marker for Purkinje cell maturation. Cerebellin stimulates norepinephrine release via the adenylate cyclase/PKA-dependent signaling pathway. Cerebellin reduces insulin secretion from pancreatic islets under high-glucose conditions. Cerebellin also regulates synaptic structure formation and controls catecholamine secretion in peripheral tissues. Cerebellin can be used in neurological research.

Diproteverine hydrochloride is an oral activity calcium channel blocker. Diproteverine hydrochloride embryonic toxicity. Diproteverine hydrochloride also shows antianginal properties.

Nicardipine-¹³C,d₃ hydrochloride (YC-93-¹³C,d₃) is the deuterium and ¹³C-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.

ML218-d₉ is the deuterium labeled ML218. ML218 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 inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 has no significant inhibition of L- or N-type calcium channels, KATP or hERG potassium channels. ML218 can penetrate the blood-brain barrier.

Felodipine-d₅ is deuterium labeled 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.

Levamlodipine ((S)-Amlodipine; Levoamlodipin) hydrochloride is an orally active L-type calcium channel blocker and MMP-9 modulator with high permeability and retention properties. Levamlodipine hydrochloride 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 hydrochloride 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 hydrochloride exerts no significant inhibitory effect on abdominal aortic intimal hyperplasia. When excessively accumulated in the epidermis, Levamlodipine hydrochloride 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 hydrochloride can be used in research related to hypertension and atherosclerosis.

CALP3 TFA, a Ca²⁺-like peptide, is a potent Ca²⁺ channel blocker that activates EF hand motifs of Ca²⁺-binding proteins. CALP3 TFA can functionally mimic increased [Ca²⁺]_i by modulating the activity of Calmodulin (CaM), Ca²⁺ channels and pumps. CALP3 TFA has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia.

COX-2-IN-55 (compound 1) is an orally active, Celecoxib (HY-14398)-based analog with broad-spectrum anticancer activity and weak COX-2 inhibition. COX-2-IN-55 specifically inhibits SERCA2, increases caspase-3 cleavage and DR5 levels, thereby activating GRP78 and inhibiting the development of triple-negative breast cancer (TNBC). COX-2-IN-55 can also downregulate the levels of angiogenic markers VEGF-α and IL-8, inhibiting the formation of microvessels.

A-1048400 is an orally active and selective calcium channel inhibitor with an IC₅₀ value of 1.4 μM for N-type channels, 1.2 μM for T-type channel. A-1048400 inhibits neurotransmitter release and reduces membrane hyperexcitability, exerting potent analgesic activity. A-1048400 is promising for research of neuropathic pain (e.g., pain induced by spinal nerve ligation and chronic constriction injury).

Parametadione (Isoethadione) is an antiepileptic agent.

Ibutilide-d₅ (fumarate) is deuterium labeled Ibutilide (fumarate).

trans-AzoTAB is a photoresponsive potassium/sodium/calcium channel modulator and DNA-binding agent. trans-AzoTAB undergoes trans-cis isomerization driven by light, with variable polarity and DNA affinity. trans-AzoTAB also enhances voltage-gated potassium currents and inhibits sodium and calcium currents in cardiomyocytes, thereby reducing spontaneous electrical activity and excitation conduction velocity. In addition, trans-AzoTAB induces compaction and frozen conformation of λ-phage DNA, and non-sequence-dependently inhibits transcription and translation processes in the dark; its activity can be reversed and restored by visible light after activation with ultraviolet irradiation. trans-AzoTAB can serve as a probe for two-photon optical regulation of myocardial excitability, and is used to construct photoresponsive interfacial polymer structures.

Kurtoxin is a selective Cav3 (T-type) voltage-gated Ca²⁺ channel gating inhibitor with a K_d of 15 nM for Cav3.1 (α1G T-type) Ca²⁺ channel. Kurtoxin can interact with high affinity with native neuronal high-threshold L-type, N-type, and P-type Ca²⁺ channels in central and peripheral neurons. Kurtoxin also shows cross-reactivity with voltage-gated Na⁺ channel.

NecroX-5 free base is a derivative of the NecroX, reduces intracellular calcium concentration, and possesses anti-inflammatory and anti-cancer activity.

Calpain Inhibitor-2 (compound 5) is a peptide inhibitor of μ-calpain (Ki=9 nM). Calpain Inhibitor-2 exhibits antiproliferative activity against melanoma cell lines (A-375 and B-16F1) and PC-3 prostate cancer cells in vitro.

Ruthenium Red Staining Solution (0.01%) is a polycationic dye widely used for electron microscopy (EM) of cells, tissues and vegetative bacteria. Ruthenium Red Staining Solution (0.01%) strongly reacts with phospholipids and fatty acids and binds to acidic mucopolysaccharides. Ruthenium Red Staining Solution (0.01%) is a L-type calcium current (I_Ca) blocker. When using Ruthenium Red Staining Solution (0.01%) to stain plant tissue sections affected by pathogens, the breakdown of mucilaginous substances by the pathogens prevents them from taking up the stain, whereas the cell walls of healthy tissue stain red.

Levobunolol (l-Bunolol) is a non-selective β-adrenergic antagonist and vasodilator. By blocking calcium ion influx and reducing the sensitivity of vascular smooth muscle to calcium, Levobunolol effectively dilates the ciliary arteries and increases ocular blood flow, so it is widely used in research on glaucoma and ocular hypertension. Levobunolol inhibits the β-receptor signaling pathway and the expression of related proliferation markers (such as CK3, CK14, CK19, Ki67) in corneal cells. In rabbit models, Levobunolol not only does not inhibit corneal epithelial regeneration, but also accelerates the healing of mechanical injury without adverse effects. Levobunolol also inhibits histamine-induced vasoconstriction and intracellular calcium elevation, exhibiting unique vascular regulatory activity. Levobunolol protects ocular blood flow and promotes corneal repair.