Calcium Channel

<p>Gallopamil, (-)- is an L-type calcium channel blocker. It is used in the treatment of abnormal heart rhythms.</p>

<p>AK-2-38 is a nifedipine analogue with potent smooth muscle calcium antagonist action and partial agonist effects on isolated guinea pig left atrium.</p>

<p>Falipamil, a verapamil derivative, is a calcium channel blocker with antitachycardic and potential antianginal effects.</p>

<p>Tiropramide is an antispasmodic drug. It also useful to inhibit the contractile response of the urinary bladder and in managing abdominal pain in IBS.</p>

<p>Bms 188107 is a calcium antagonist, it has cardioprotective effects.</p>

<p>AZD 2066 is a selective, orally active, and brain-penetrant mGluR5 antagonist with analgesic activity.</p>

<p>BBR 2160: a calcium-antagonist dihydropyridine derivative, reduces heart tissue contractility and shortens action potentials.</p>

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

<p>Tamolarizine (Tamolarizine free base) free base is a novel calcium antagonist.</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>R 56865 is a weak potential-operated channel inhibitor that inhibits the late sodium current in human isolated cardiomyocytes.</p>

<p>Enecadin is a neuroprotective agent.</p>

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

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

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

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

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

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

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

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

<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>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>

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

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

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

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

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

<p>Terflavoxate is a novel, orally active, semisynthetic statin microtubule inhibitor commonly used in combination with capecitabine.</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>Fenoverine (Spasmopriv) has antispasmodic activity and can be used to study gastrointestinal spasms.</p>

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

<p>Diproteverine HCl is a novel calcium antagonist with antianginal properties, antispasmodic and vasoactive.</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>Lifarizine (RS-87476), a calcium-sodium channel antagonist, shows neuroprotective activity in a simplified rat survival model of double vessel occlusion.</p>

<p>AZD-1305: novel anti-arrhythmic blocking IKr, Ca, Na currents; useful in arrhythmia research.</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>Crobenetine (BIII 890 CL) Free Base is a selective NaV channel blocker that eliminates VTD-induced [Ca2+] elevation.</p>

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

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

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

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

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

<p>TROX-1 is the activation state-dependent Cav2 channel antagonist.</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>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>N-type calcium channel blocker-1 is an orally active analgesic agent,shows high affinity to functionally block N-type calcium channels.</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>A selective vascular KCa1.1 channel stimulator with CaV1.2 blocking ability and mild myorelaxant effects.</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>Darodipine (PY-108068) is a dihydropyridine type Ca+2 antagonist.</p>

<p>HA-1004 dihydrochloride is an inhibitor of PKA, PKC, cGKI, MYLK, and calcium channel protein</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>TMDJ-035 is a selective inhibitor of the RyR2 (ryanodine receptor 2).</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>

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

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

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

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

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

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

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

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

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

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

<p>Ca2+ channel antagonist</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>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>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>NNC 55-0396: Selective T-type calcium channel blocker, IC50 6.8 μM, inhibits human ovarian cancer cell growth.</p>

<p>SB-423557 is an orally active antagonist of calcium-sensing receptor (CaR) with IC50 of 520 nM</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>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>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>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>PD-217014 is an α2δ ligand that exhibits visceral analgesic activity and can suppress visceral hypersensitivity. Its antihyperalgesic effects are dose-dependent.</p>

<p>Emopamil, a calcium channel inhibitor, reduces neuronal damage caused by ischemia.</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>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>Mibefradil dihydrochloride hydrate is a long-acting antihypertensive blocking high-voltage L calcium channels.</p>

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

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

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

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

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