Canal calcique

Crobenetine (BIII 890 CL) Free Base is a selective NaV channel blocker that eliminates VTD-induced [Ca2+] elevation.

R 56865 is a weak potential-operated channel inhibitor that inhibits the late sodium current in human isolated cardiomyocytes.

Upacicalcet (AJT-240) is a calcium mimetic for SHPT in dialysis, reducing PTH by targeting parathyroid receptors.

DS16570511 is a novel, cell-permeable inhibitor targeting the mitochondrial calcium uniporter.

Clopimozide (R-29764), a long-acting oral antischizophrenic, blocks calcium channels and [3H] nilandipine binding.

SERCA2a activator 1 boosts heart function by reducing phospholamban restraint and enhancing cardiac contraction-relaxation cycles.

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

Mioflazine hydrochloride anhydrous 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.

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

MONIRO-1 blocks T/N-type Ca²⁺ channels: hCav2.2 (IC50: 34μM), hCav3.1 (3.3μM), hCav3.2 (1.7μM), hCav3.3 (7.2μM).

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

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

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

ATI-22-107 is a positive cardiac inotropic agent which may affect myocyte calcium cycling and contractility.

5J-4 is a potent a blocker of calcium release-activated calcium (CRAC) channel and store-operated calcium entry (SOCE).

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

Broad spectrum cation channel blocker

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

(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.

8-Bromo NAD+ serves as a prodrug for the cyclic ADP-ribose (cADPR) inhibitor, 8-bromo cADPR, undergoing conversion to its active form by the enzyme CD38.

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.

Nelutroctiv is a potent activator of cardiac troponin.

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.

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

RS 5773 is a benzothiazepine derivative with antianginal effects.

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

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

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

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

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).

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

Cav 3.2 Inhibitor 4 (Compound 21) is a selective and potent inhibitor of the T-type calcium channel (Ca v 3.2), demonstrating peripheral restriction with an

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

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

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

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

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

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

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

Leualacin is a novel calcium blocker from Hapsidospora irregularis.

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].

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

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.

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

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

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).

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

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).

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

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.

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.

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.

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

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

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

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

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

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

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

Ca2+ channel antagonist

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.

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).

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).

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.

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.