Calcium Channel Inhibitor

Proadrenomedullin (1-20), human is a potent hypotensive and catecholamine release–inhibitory peptide released from chromaffin cells. Proadrenomedullin (1-20) inhibits catecholamine secretion in PC12 pheochromocytoma cells (IC₅₀ ≈ 350 nM) by suppressing Na⁺/Ca²⁺ influx and blocking desensitization. Proadrenomedullin (1-20), human specifically acts on nicotinic cholinergic receptors in a non competitive manner. Proadrenomedullin (1-20), human can be used for research on conditions such as hypertension.

NP118809 is a potent N-type calcium channel blocker, with an IC₅₀ of 0.11 μM; also less potently inhibits L-type calcium channel with an IC₅₀ of 12.2 μM.

Clonixin (SCH-10304) 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.

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

ent-(+)-verticilide is a potent and selective inhibitor of cardiac ryanodine receptor (RyR2) calcium release channels with antiarrhythmic activity. ent-(+)-verticilide inhibits RyR2-mediated diastolic Ca2+ leak and exhibits higher potency and a distinct mechanism of action compared with theDantrolene and Tetracaine. ent-(+)-verticilide is a useful tool to investigate the therapeutic potential of targeting RyR2 hyperactivity in heart and brain pathologies.

Gabapentin-d₄ is the deuterium labeled Gabapentin. Gabapentin (Neurontin) is a pharmaceutical agent, specifically a GABA analog. It was originally developed to treat epilepsy, and currently is also used to relieve neuropathic pain.

Brompheniramine ((±)-Brompheniramine) maleate is a potent and orally active antihistamine of the alkylamine class. Brompheniramine maleate is a selective histamine H1 receptor antagonist with a K_d of 6.06 nM. Brompheniramine maleate can block the hERG channels, calcium channels, and sodium channels with IC₅₀s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine maleate has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research.

ω-Agatoxin IVA is a potent, selective P/Q type Ca²⁺ (Cav2.1) channel blocker with IC₅₀ values of 2 nM and 90 nM. ω-Agatoxin IVA inhibits glutamate exocytosis and calcium influx elicited by high potassium. ω-Agatoxin IVA inhibits Capsaicin (HY-10448)-induced CGRP release and vasodilation. ω-Agatoxin IVA can be used for the research of neurological and cardiovascular disease.

ABT-639 is a novel, peripherally acting, selective T-type Ca²⁺ channel blocker.

Mirogabalin besylate is a selective and orally available ligand for the α2δ subunit of voltage-gated calcium channels, with K_ds of 13.5 nM, 22.7 nM, 27 nM, and 47.6 nM for human α2δ-1, human α2δ-2, rat α2δ-1, and rat α2δ-2, respectively.

(Rac)-Ibrutinib alkyne (Compound 8) is a Btk inhibitor with an IC₅₀ of 0.72 nM. (Rac)-Ibrutinib alkyne can effectively inhibit functions related to the B-cell receptor signaling pathway, with an IC₅₀ of 9 nM for inhibiting Ca flux in Ramos cells. (Rac)-Ibrutinib alkyne can be used in the research of diseases such as rheumatoid arthritis.

Gabapentin enacarbil (XP-13512) is a prodrug of Gabapentin (HY-A0057) designed to be absorbed throughout the intestine by high-capacity nutrient transporters. Gabapentin is a potent, orally active P/Q type Ca²⁺ channel blocker. Gabapentin enacarbil can be used for the study of Restless Legs Syndrome (RLS) and postherpetic neuralgia (PHN).

(±)-Praeruptorin A, a coumarin compound, is the main bioactive component in Peucedani Radix. As a calcium channel blocker, (±)-Praeruptorin A exhibits great antihypertensive effects. In addition, (±)-Praeruptorin A also has the effects of relaxing vascular smooth muscle, inhibiting airway inflammation and airway hyperresponsiveness. (±)-Praeruptorin A can be used for the research of allergic asthma, hypertension and other diseases.

Efonidipine (NZ-105) 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 inhibits SARS-CoV-2 main protease. Efonidipine 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 reduces plasma aldosterone levels in vivo. Efonidipine 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 can be used for research in hypertension, heart failure, and disorders involving dysregulated steroid hormone synthesis.

A-425619 is an orally active and selective transient receptor potential type V1 (TRPV1) antagonist. A-425619 blocks Capsaicin (HY-10448)- and N-arachidonoyl-dopamine (NADA)-induced Ca²⁺ influx in dorsal root ganglia and trigeminal ganglia. A-425619 relieves pathophysiological pain associated with inflammation and tissue injury in rats. A-425619 can be used for the study of pain related to inflammation and tissue injury.

Lidoflazine is a high affinity blocker of the HERG (human ether-a-go-go-related gene) K⁺ channel. Lidoflazine is an antianginal calcium channel blocker that carries a significant risk of QT interval prolongation and ventricular arrhythmia.

VU6032735 is a potent and subtype-selective sperm-specific potassium channel 3 (SLO3) inhibitor with IC₅₀ values of 165 nM (hSLO3) and 730 nM (mSLO3). VU6032735 also inhibits sodium channel and L-type calcium channel VU6032735 can sustain high tissue exposure in the fertilized oviduct. VU6032735 can be used for the research of contraception.

Nemadipine-A is a specific inhibitor of the EGL-19 L-type Ca²⁺ channel. Nemadipine-A, a cell-permeable L-type calcium channel inhibitor, sensitizes TRAIL-resistant cancer cells to this ligand.

BMS-192364 is targeting the G_α-RGS interaction to produce an inactive Gα-RGS complex. BMS-192364 reduces urinary bladder contraction and exert RGS-agonist properties by increasing the action of GAPs on Gq proteins. BMS-192364 inhibits calcium flux.

Bupivacaine (hydrochloride) (Standard) is the analytical standard of Bupivacaine (hydrochloride). This product is intended for research and analytical applications. Bupivacaine hydrochloride is a NMDA receptor inhibitor.Bupivacaine can block sodium, L-calcium, and potassium channels.Bupivacaine potently blocks SCN5A channels with the IC₅₀ of 69.5 μM. Bupivacaine hydrochloride can be used for the research of chronic pain.