Canal calcique

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

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).

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

Piprofurol is used as a Calcium channel blocker.

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

RS 5773 is a benzothiazepine derivative with antianginal effects.

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

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

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.

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

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

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

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).

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

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

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).

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 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).

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

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

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.

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

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

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).

Leualacin is a novel calcium blocker from Hapsidospora irregularis.

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.

Ca2+ channel antagonist

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.

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

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.

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

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

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.

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

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

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

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

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

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.

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.