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You are here:Home-Inhibitors & Agonists-Membrane Transporter/Ion Channel-Calcium Channel

Request The Product List ofCalcium Channel Calcium Channel

Calcium channel is an ion channel which displays selective permeability to calcium ions. It is sometimes synonymous as voltage-dependent calcium channel, although there are also ligand-gated calcium channels. Voltage-gated calcium (CaV) channels catalyse rapid, highly selective influx of Ca2+ into cells despite a 70-fold higher extracellular concentration of Na+. Some calcium channel blockers have the added benefit of slowing your heart rate, which can further reduce blood pressure, relieve chest pain (angina) and control an irregular heartbeat.

Cat. No. Product Name CAS No. Information
GY04417

NS-638

150493-34-8

A nonpeptide calcium channel blocker that dose dependently inhibits AMPA-stimulated [3H]GABA-release from cultured cortical neurons with IC50 of 4.3 uM; blocks K(+)-stimulated intracellular Ca(2+)-elevation in cultured cerebellar granule cells with IC50 of 3.4 uM, reversibly blocks N- and L-type Ca(2+)-channels in cultured chick dorsal root ganglion cells (1-30 uM); exhibits anti-ischemic properties in vivo.

GY07130

Synta-66

835904-51-3

Synta-66 is a potent, selective CRAC channel Orai1 blocker with IC50 of 3 uM; does not impair other plasma membrane ion transporters; inhibits antigen-evoked Ca2+ influx in Fura-2-loaded cells at 10 uM, prevents the increase in Syk activity triggered by Ca2+ entry; reduces FcεRI-dependent Ca(2+) influx and the release of histamine, leukotriene C4, and cytokines (IL-5/-8/-13 and TNFα) by up to 50% at 3 uM in HLMCs.

GY10142

BTT-266

BTT-266 (BTT266) is a voltage-gated CaV2.2 calcium channel inhibitor that disrupts the CaVα·CaVβ3 protein-protein interaction, directly binds to CaVβ3 with Kd of 3.6 uM; decreases surface presentation of the CaV2.2α1 subunit, significantly reduces trafficking of CaV2.2 to the plasma membrane at 50 uM, does not affect CaV2.2 currents in either in HEK-CaV2.2 cells or rat dorsal root ganglion (DRG) neurons.

GY10143

BTT-369

BTT-369 (BTT369) is a voltage-gated CaV2.2 calcium channel inhibitor that disrupts the CaVα·CaVβ3 protein-protein interaction with Ki of 2.0 uM in FP assays; decreases trafficking of CaV2.2 channels to the plasma membrane and modulates the functions of the channel, suppresses pain responses in rodent neuropathic pain models; BTT-369 (BTT369) is a cell-permeable derivative of BTT-266.

GY10444

SAK3

1256269-87-0

SAK3 (T-VGCC enhancer SAK3) is a potent, orally acitve enhancer of T-type voltage-gated Ca2+ channel (T-VGCC), enhances CaV3.1 and CaV3.3, but not CaV3.2 activity at concentrations of 0.01-10 nM in neuro2A cells in vitro; significantly enhanced acetylcholine (ACh) release in the hippocampal CA1 region of na?ve mice (0.5 mg/kg, p.o.); significantly enhanced hippocampal ACh levels in olfactory-bulbectomized (OBX) mice, rescuing impaired memory-related behaviors.

GY05238

RU1968

171336-24-6

RU1968 is a potent, cross-species sperm-specific Ca2+ channel CatSper inhibitor that is selective for CatSper over Slo3; suppresses progesterone- and prostaglandin-induced Ca2+ signals in human sperm (IC50=4 and 3.8 uM), potently abolishes CatSper-mediated Ca2+ signals in mouse, human, and sea urchin sperm.

GY05225

ACT 709478

1838651-58-3

ACT 709478 is a potent, selective, orally-bioavailable, brain penetrant T-type calcium channel blocker with IC50 of 6.4, 18, and 7.5 nM for Cav3.1, Cav3.2, and Cav3.3 channels respectively; displays >100-fold selectivity over Cav1.2 channels; shows a significant decrease of the seizure severity in vivo (100 mg/kg, p.o.).

GY05219

JTV-519 fumarate

1883549-36-7

JTV-519 (K201) is a Ca2+-dependent blocker of SERCA and a partial agonist of ryanodine receptors (RyRs); displays Ca(2+)-dependent inhibition of SERCA-dependent ATPase activity with IC50 of 9 uM at 0.25 Ca2+ in cardiac muscle; may prevent abnormal Ca(2+) leak from the sarcoplasmic reticulum (SR) in the ischemic heart and skeletal muscle (SkM) by stabilizing the ryanodine receptors (RyRs; RyR1 and RyR2, respectively).

GY05374

JTV-519 HCl

1038410-88-6

JTV-519 (K201) is a Ca2+-dependent blocker of SERCA and a partial agonist of ryanodine receptors (RyRs); displays Ca(2+)-dependent inhibition of SERCA-dependent ATPase activity with IC50 of 9 uM at 0.25 Ca2+ in cardiac muscle; may prevent abnormal Ca(2+) leak from the sarcoplasmic reticulum (SR) in the ischemic heart and skeletal muscle (SkM) by stabilizing the ryanodine receptors (RyRs; RyR1 and RyR2, respectively).

GY05339

FPL64176

120934-96-5

FPL64176 (ARC-64176) is a potent L-type Ca++ channel activator with EC50 of 16 nM; prolongs action potential duration and enhances contractility in guinea pig papillary muscle, induces contractile response with EC50 of 0.2 uM; produces biexponential tail current decays at -50 mV with fast and slow time constants of 4.30 +/- 0.30 and 44.52 +/- 4.56 msec, respectively; produces large increases in cardiac contractile force and diastolic blood pressure in anesthetized dogs (100 mg/kg, i.v.).

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