Canale del calcio

ML218 is an inhibitor of T-type Ca2+ channels (Cav3.1, Cav3.2, Cav3.3).ML218 inhibits the synaptic activity of subthalamic nucleus (STN) neurons.

β-Amino Acid Imagabalin Hydrochloride is the voltage-dependent calcium channel ligand for the α2δ subunit.

<p>Ethacrynate Sodium, a sodium salt, blocks chloride, potassium, and sodium transport mainly in Henle's loop.</p>

Lidoflazine: antianginal, blocks HERG K+ & Ca channels, risks QT prolongation & arrhythmia.

Semotiadil recemate fumarate is the recemate of Semotiadil fumarate. Semotiadil fumarate is a novel antagonist of vasoselective Ca2+ channel.

<p>JTV-519 hemifumarate: Ca2+ blocker, SERCA inhibitor, ryanodine receptor partial agonist; antiarrhythmic, cardioprotective.</p>

<p>UK-52831, a calcium channel antagonist, is used potentially for the treatment of hypertension and myocardia ischemia.</p>

<p>SB-237376 HCl (SB-237376 hydrochloride) is a calcium and potassium channel antagonist used in the treatment of cardiac arrhythmias.</p>

<p>Carboxyamidotriazole is a cytostatic inhibitor of non-voltage-operated calcium channels and calcium channel-mediated signaling pathways.</p>

<p>NecroX-5, a derivative of NecroX, exhibits anti-inflammatory and anti-cancer activities. NecroX-5 reduces intracellular calcium concentration.</p>

<p>DS16570511 is a novel, cell-permeable inhibitor targeting the mitochondrial calcium uniporter.</p>

<p>Lifarizine (RS-87476), a calcium-sodium channel antagonist, shows neuroprotective activity in a simplified rat survival model of double vessel occlusion.</p>

<p>Tiapamil hydrochloride (Ro 11-1781 hydrochloride) is a calcium channel blocker with antihypertensive activity used in the study of angina pectoris.</p>

<p>Opc 8490 is a cardiotonic agent and a positive inotropic vasodilator, which prolongs the atrial action potential in a concentration-dependent manner.</p>

<p>Cerebrocrast (IOS-11212) has anti-inflammatory and hypoglycemic activity, blocks human platelet activation, and is used in the study of diabetes.</p>

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

<p>Ticolubant: Oral LTB4 antagonist, Ki=0.78 nM; blocks Ca2+ migration, IC50=6.6 nM; anti-inflammatory in mice.</p>

<p>N106 is an activator of the SUMO-activating enzyme, E1 ligase, and triggers intrinsic sumoylation of SERCA2a. N106 can be used in studies about heart failure.</p>

<p>Vatanidipine (AE0047) is a novel dihydropyridine (DHP)-type calcium channel blocker with slow-onset pharmacological actions.A slow-onset and long-lasting</p>

VU 0240551 is a selective antagonist of neuronal K-Cl cotransporter KCC2 inhibitor with an IC50 of 560 nM. VU 0240551 inhibits L-type calcium channels and hERG.

<p>O-1602 is a novel GPR55 agonist, an atypical cannabinoid associated with the central nervous system and obesity, and is a candidate compound for the treatment</p>

<p>Sulcardine sulfate (B-87823) is a multi-ion channel blocker with antiarrhythmic activity that inhibits Na+, K+, and Ca2+ channels.</p>

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

<p>CP-060 is a potent Ca2+ antagonist and inhibits Ca2+ overload with antioxidant and cardioprotective activities.</p>

Gallopamil blocks acid secretion (IC50: 10.9 μM), acts as antiarrhythmic, vasodilator, and is a methoxy Verapamil derivative.

<p>AZD-1305: novel anti-arrhythmic blocking IKr, Ca, Na currents; useful in arrhythmia research.</p>

<p>PD 173212 is a blocker that blocks N-type voltage sensitive calcium channel (Cav2.2).</p>

<p>8-Bromo-cGMP sodium: PKG activator, eases pain, dilates vessels, reduces Ca2+ currents &amp; insulin release.</p>

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

<p>Terflavoxate is a novel, orally active, semisynthetic statin microtubule inhibitor commonly used in combination with capecitabine.</p>

GSK205 is a selective TRPV4 antagonist (IC50: 4.19 μM) for inhibiting TRPV4-mediated Ca2+ influx.

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

Enecadin is a neuroprotective agent.

<p>SAK3 is a modulator of nAChR activity and is used to study memory deficits and Alzheimer's disease.</p>

<p>Diproteverine HCl is a novel calcium antagonist with antianginal properties, antispasmodic and vasoactive.</p>

<p>Tamolarizine (Tamolarizine free base) free base is a novel calcium antagonist.</p>

<p>Pelretin (BASF 43915) is a potential protein inhibitor for the study of dermatologic diseases.</p>

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

<p>Fenoverine (Spasmopriv) has antispasmodic activity and can be used to study gastrointestinal spasms.</p>

<p>Cronidipine (LF 20254), a calcium channel antagonist, is used potentially for the treatment of hypertension and myocardia ischemia.</p>

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

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

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

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

<p>Budiodarone (ATI-2042) resembles amiodarone, potentially preventing atrial fibrillation.</p>

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

<p>Darodipine (PY-108068) is a dihydropyridine type Ca+2 antagonist.</p>

<p>(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.</p>

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

<p>Broad spectrum cation channel blocker</p>

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

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

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

<p>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</p>

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

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

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

<p>TROX-1 is the activation state-dependent Cav2 channel antagonist.</p>

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

<p>RS 5773 is a benzothiazepine derivative with antianginal effects.</p>

<p>Piprofurol is used as a Calcium channel blocker.</p>

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

<p>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.</p>

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

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

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

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

<p>Calcium channel-modulator-1 is a calcium channel-modulator (IC50:0.8 μM) with specialisation to block aortic constriction.</p>

<p>EMD57033 activates cardiac troponin C, enhances Ca2+ sensitivity to boost heart contraction.</p>

<p>AY 77: Potent, selective PAR2 agonist, favors Ca2+ (ec50=40nM) &amp; ERK1/2 (ec50=2μM), boosts breast cancer cell migration.</p>

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

<p>Leualacin is a novel calcium blocker from Hapsidospora irregularis.</p>

<p>Emopamil, a calcium channel inhibitor, reduces neuronal damage caused by ischemia.</p>

<p>Ca2+ channel antagonist</p>

<p>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.</p>

<p>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.</p>

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

<p>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).</p>

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

<p>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].</p>

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

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

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

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

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

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

<p>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).</p>

<p>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.</p>

<p>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.</p>

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

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

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

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

<p>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.</p>

<p>(Rac)-PD0299685 is a potent voltage-dependent calcium channel inhibitor for the study of retina-related diseases.</p>

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