Calcium Channel

NKY-722 (HCl), also known as Iganidipine, is a calcium channel blocker potentially for the treatment of glaucoma.

(S)-(-)-Bay-K-8644 ((S)-(-)-Bay K 8644) is an agonist of L-type Ca2+ channel and activates Ba2+ currents with an EC50 of 32 nM.

A 425619 (1-(4-(TRIFLUOROMETHYL)BENZYL)-3-(ISOQUINOLIN-5-YL)UREA) is a potent TRPV1 antagonist

Naltiazem, a calcium channel antagonist, is used potentially for the treatment of arrhythmias, hypertension and myocardial infarction.

Mioflazine suppresses nucleoside uptake. Mioflazine is an orally active nucleoside transport inhibitor. It has the potential for sleep disorders treatment.

HA-1004 dihydrochloride is an inhibitor of PKA, PKC, cGKI, MYLK, and calcium channel protein

N-type calcium channel blocker-1 is an orally active analgesic agent,shows high affinity to functionally block N-type calcium channels.

Mioflazine hydrochloride is a nucleoside transport inhibitor that acts on adenosine to improve sleep.

A selective vascular KCa1.1 channel stimulator with CaV1.2 blocking ability and mild myorelaxant effects.

Budiodarone (ATI-2042) resembles amiodarone, potentially preventing atrial fibrillation.

Cavα2δ1&NET-IN-3 (example 216) is an inhibitor targeting both the α2δ subunit of voltage-gated calcium channels (VGCC) and the noradrenaline transporter (NET).

Piprofurol is used as a Calcium channel blocker.

BBT has anti-hyperglycemic activity, protecting beta cells from cytokine or streptozotocin-induced cell death, and restoring beta cell function.

RS 5773 is a benzothiazepine derivative with antianginal effects.

TMDJ-035 is a selective inhibitor of the RyR2 (ryanodine receptor 2).

TROX-1 is the activation state-dependent Cav2 channel antagonist.

Broad spectrum cation channel blocker

Halofuginone hydrochloride (RU-19110), a derivative of Febrifugine, functions as a competitive inhibitor of prolyl-tRNA synthetase, displaying a Ki value of 18.3 nM. This compound effectively inhibits type-I collagen synthesis, providing therapeutic benefits in osteoarthritis (OA) by impeding TGF-β signaling. Additionally, it serves as a potent pulmonary vasodilator, mainly through the activation of Kv channels and the inhibition of various calcium channels including voltage-gated, receptor-operated, and store-operated ones. Beyond its vascular effects, Halofuginone hydrochloride exhibits a broad spectrum of biological activities, including anti-malarial, anti-inflammatory, anti-cancer, and anti-fibrotic properties, supported by multiple studies.

Coelenterazine H, a Ca2+ sensitive synthetic derivative, is a luminescent biomolecule used to measure Ca2+ changes.

Iganidipine（NKY 722） is a new water-soluble Ca2+ antagonist with antihypertensive activity for research and neurological related diseases.

Darodipine (PY-108068) is a dihydropyridine type Ca+2 antagonist.

Nelutroctiv is a potent activator of cardiac troponin.

RO 23-6152, a new calcium antagonist, can inhibit platelet aggregation in vitro associated with occlusive coronary thrombus formation.

Bupivacaine hydrochloride monohydrate is an NMDA receptor inhibitor that inhibits SCN5A channels and is commonly used in the study of chronic pain.

EMD57033 activates cardiac troponin C, enhances Ca2+ sensitivity to boost heart contraction.

Cis-22a: selective TRPV6 inhibitor (IC50=0.32μM), halts T47D breast cancer cell growth.

Fluspirilene is a long-acting antipsychotic for schizophrenia, inhibiting L-type calcium channels (IC50: 0.03 μM).

Reldesemtiv (CK-2127107) boosts exercise capacity, targeting fast muscle troponin, EC50 3.4 μM.

CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg

Compound 9e is a Cav 2.2/3.2 blocker; IC50: 1.22 μM & 80 μM, respectively; penetrates CNS.

(rel)-Mirogabalin ((rel)-DS5565) is an inhibitor of voltage-dependent calcium channels, specifically targeting the α2δ-1 subunit.

BER-5 is a potent MrgX2 antagonist, demonstrating broad-spectrum antagonistic activity against various MrgX2 agonists. It can inhibit Substance P(SP)-induced degranulation in LAD2 cells and alleviate SP-induced allergic reactions in mice. BER-5 is useful for researching mechanisms related to allergic reactions.

Cav 3.2 inhibitor 3 is a potent inhibitor of the Cav3.2 T-type Ca2+channel (IC50: 0.1534 μM) and has a low binding affinity for D2 receptors.

RWJ 22108 is a bronchial-selective calcium channel (calcium channel) blocker that exhibits an IC50 of 5.7 nM in dog bronchial smooth muscle calcium-dependent contractions.

CAD204520 functions as an inhibitor of SERCA (IC50 = 0.34 μM), specifically targeting mutations in the wild-type NOTCH1 protein associated with T-cell acute lymphoblastic leukemia (T-ALL) and mantle cell lymphoma (MCL).

NNC 55-0396: Selective T-type calcium channel blocker, IC50 6.8 μM, inhibits human ovarian cancer cell growth.

Mibefradil is a calcium channel blocker with moderate selectivity for T-type Ca2+ channels (IC50s: 2.7 μM and 18.6 μM for T-type and L-type currents).

SB-423557 is an orally active antagonist of calcium-sensing receptor (CaR) with IC50 of 520 nM

Emopamil, a calcium channel inhibitor, reduces neuronal damage caused by ischemia.

Leualacin is a novel calcium blocker from Hapsidospora irregularis.

PD-217014 is an α2δ ligand that exhibits visceral analgesic activity and can suppress visceral hypersensitivity. Its antihyperalgesic effects are dose-dependent.

Sesamodil (SD 3211) is a novel calcium antagonist that can be used to study hypertension.

PDE1-IN-4: inhibits PDE1C/A/B with IC50s 10/145/354 nM, may help study idiopathic pulmonary fibrosis.

MP-010 is an FKBP12 ligand that regulates cytosolic calcium by stabilizing RyR channel activity. It facilitates functional improvement in SOD1G93A mice with amyotrophic lateral sclerosis (ALS), evidenced by enhanced motor coordination, increased integrity of neuromuscular junctions, and significantly higher spinal motor neuron survival rates. MP-010 is applicable for research in the field of neurological disorders.

Mibefradil dihydrochloride hydrate is a long-acting antihypertensive blocking high-voltage L calcium channels.

Cav 3.1 blocker 1 (compound 12) is a T-type calcium channel inhibitor with an IC50 value of 160 nM for Cav3.1. It exhibits weaker inhibition on Cav 3.2 with an IC50 of 5000 nM and shows no inhibitory effect on Cav 3.3 and Cav 1.2 (IC50 > 10000 nM).

Cav 3.2 inhibitor 2 blocks T-type Ca2+ channels (IC50=0.09339 μM) and reduces mouse somatic/visceral pain. Used for intractable pain studies.

Compound 6g inhibits T-type Ca channels (IC50: Cav3.1-31μM, Cav3.2-83μM), cytotoxic to A549 (IC50: 5μM) & HCT-116 cells (IC50: 6.4μM).

AZD 2066 hydrate is a selective, orally active, and brain-penetrant antagonist of mGluR5. It exhibits antinociceptive effects [1].

Calpain Inhibitor-2: Lipophilic, moderates growth of A-375, B-16F1, PC-3 cancers, and hinders 80% DU-145 cell invasion.

TTA-P1: potent T-type calcium channel inhibitor; impacts neuron firing, hormone secretion, cell growth; potential in absence epilepsy research.

IAB15 is a potent inhibitor of T-type calcium channel that can be used in the research of epilepsy [1].

Cav 3.2 inhibitor 1 targets T-type calcium channels, weakly binds D2 receptors, and aids physical and visceral pain research.

Ca2+ channel antagonist

IAA65 is a potent inhibitor of T-type calcium channels, exhibiting an IC50 value of 18.9 μM, and holds potential for use in epilepsy research [1].

NSC-609249 hydrochloride, an impurity of Verapamil, is a calcium channel blocker with potent orally active properties. It also functions as a first-generation P-glycoprotein (P-gp) inhibitor.

Fostedil enhances heart function, maintains blood flow during partial/total coronary occlusions, and lowers aortic pressure.