| 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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