>98%,Standard References

A potent, selective CRAC channel Orai1 blocker with IC50 of 3 uM.

A-1048400(A 1048400) is a novel potent, selective, orally active N-type and T-type calcium channel blocker with IC50 of 1.4 and 1.2 uM, respectively.

ABT-639 is a novel, peripherally acting, selective T-type Ca2+ channel blocker. ABT-639 blocks recombinant human T-type (Cav3.2) Ca2+ channels in a voltage-dependent fashion (IC50 = 2 μM) and attenuates LVA currents in rat DRG neurons (IC50 = 8 μM).

CDN1163 (CDN-1163) is a small molecule, allosteric activator of SERCA2, dose-dependently increases the Vmax of SERCA2 Ca2+-ATPase activity in ER microsomes; increases Ca2+-ATPase activity and significantly enhances Ca2+ uptake into the ER, attenuates H2O2-stimulated cell death in HEK cells; improves glucose homeostasis and metabolic parameters, increases glucose tolerance in ob/ob mice; CDN1163 reduces lipid accumulation and decreases lipogenesis in obese mice livers.

Cilnidipine(FRC8653) is a dual L- and N-type calcium channel blocker and displays antihypertensive, sympatholytic and neuroprotective activity.

Clevidipine(Clevidipine) is a short-acting dihydropyridine calcium channel antagonist (IC50= 7.1 nM, V(H) = -40 mV ) under development for treatment of perioperative hypertension.

Dantrolene sodium hemiheptahydrate is a skeletal muscle relaxant which acts by blocking muscle contraction beyond the neuromuscular junction. Dantrolene sodium hemiheptahydrate is a inhibitor of calcium channel proteins, inhibiting the release of Ca2+ fro

Dantrolene sodium is a inhibitor of calcium channel proteins, inhibiting the release of Ca2+ from the sarcoplasm. Dantrolene sodium is a skeletal muscle relaxant which acts by blocking muscle contraction beyond the neuromuscular junction.

Diltiazem HCl (Tiazac)

Diltiazem hydrochloride is a calcium ion influx inhibitor (slow channel blocker or calcium antagonist).

Efonidipine(NZ-105) Hcl monoethanolate is a dual T-type and L-type calcium channel blocker (CCB).

FPL64176 is a potent L-type Ca++ channel activator with EC50 of 16 nM.

Manidipine 2Hcl (CV-4093) is a dihydropyridine compound and a calcium channel blocker for Ca2+ current with IC50 of 2.6 nM.

Manidipine is a dihydropyridine L- and T-type calcium channel blocker.

Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium-channel complexes in the CNS.

Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium-channel complexes in the CNS.

MK-8998 is a novel bioactive compound for the treament of psychiatric disease.

Nicardipine Hcl(YC-93) is a calcium channel blocker that has been widely used to control blood pressure in severe hypertension following events such as ischemic stroke, traumatic brain injury, and intracerebral hemorrhage.

Nisoldipine(BAY-k 5552; Sular) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC50 of 10 nM.

NS638 is a Ca(2+)-channel blocker.

Pregabalin

Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.

Gallopamil hydrochloride (Methoxyverapamil hydrochloride), a methoxy derivative of Verapamil, is a phenylalkylamine calcium antagonist. Gallopamil hydrochloride inhibits acid secretion in a concentration-dependent manner with an IC50 of 10.9 μM. Gallopamil hydrochloride is a potent antiarrhythmic and vasodilator agent.

(R)-Lercanidipine hydrochloride is the R-enantiomer of Lercanidipine. (R)-lercanidipine hydrochloride is a calcium channel blocker.

(S)-Lercanidipine hydrochloride is the S-enantiomer of Lercanidipine hydrochloride. (S)-lercanidipine hydrochloride is a potent calcium channel blocker.

Methyl homoveratrate, a metabolite of RWJ-26240 in vivo, can be identified in plasma, urine and faecal extract. McN5691 (RWJ-26240) is a voltage-sensitive calcium channel blocker.

TTA-A2 is a potent, selective and orally active t-type voltage gated calcium?channel antagonist with reduced pregnane X receptor (PXR) activation. TTA-A2 is equally potent against the Cav3.1 (a1G) and Cav3.2 (a1H) channels with IC50 values of 89 nM and 92 nM, respectively, at -80 and -100 mV holding potentials. TTA-A2 can be used for the research of a variety of human neurological diseases, including sleep disorders and epilepsy.

Isotachysterol 3 is an analog of 1,25-dihydrox Vitamin D3. Isotachysterol 3 stimulates intestinal calcium transport and bone calcium mobilization in anephric rats.

Ned-K is a nicotinic acid adenine dinucleotide phosphate (NAADP) antagonist. Ned-K is effective at dampening simulated ischaemia and reperfusion (sIR)-induced Ca2+ oscillations in cardiomyocytes.

TPC2-A1-N is a novel, lipophilic, membrane permeable isoform-selective small molecule agonist of two-pore channel 2 (TPC2). TPC2-A1-N plays its role by mimicking the physiological actions of NAADP and PI(3,5)P2?through independent binding sites. TPC2-A1-N has inverse effects on key lysosomal activities and increases the pH in the lysosomal lumen in a TPC2-dependent manner.

Urolithin C, a gut-microbial metabolite of Ellagic acid, is a glucose-dependent activator of insulin secretion. Urolithin C is a L-type Ca2+ channel opener and enhances Ca2+ influx. Urolithin C induces cell apoptosis through a mitochondria-mediated pathway and also stimulates reactive oxygen species (ROS) formation.

Calcium ionophore I (ETH 1001) is a selective Ca2+ ionophore for biological membranes. Calcium ionophore I can be used in Ca2+-selective microelectrodes that can be used for quantitative intracellular measurements of resting Ca2+-activities and of slowly changing Ca2+-levels.

NSC-609249 hydrochloride is an impurity of Verapamil. Verapamil is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor.

SR33805 is a potent Ca2+ channel antagonist, with EC50s of 4.1 nM and 33 nM in depolarized and polarized conditions, respectively. SR33805 blocks L-type but not T-type Ca2+ channels. SR33805 can be used for the research of acute or chronic failing hearts.

Bepridil hydrochloride hydrate ((±)-Bepridil hydrochloride hydrate) is a non-selective, long-acting Ca+ channel antagonist and Na+, K+ channel inhibitor, with antianginal and type I antiarrhythmic effects. Bepridil hydrochloride hydrate also acts as a cardiac Na+/Ca2+ exchange (NCX1) inhibitor. Bepridil hydrochloride hydrate can be used for the research of cardiovascular disorders.

β-Cyfluthrin (beta-Cyfluthrin) is a type II synthetic pyrethroid and also an active ingredient of many insecticide products used for pestsin agriculture. β-Cyfluthrin is a neurotoxicant and affects calcium concentration in nervous tissue by inhibiting Ca2+ ATPase involved in calcium transport.

ω-Conotoxin MVIIC is a N- and P/Q-type Ca2+ channel blocker, significantly suppresses the 11-keto-βboswellic acid-mediated inhibition of glutamate release.

ω-Conotoxin MVIIC TFA is a N- and P/Q-type Ca2+ channel blocker, significantly suppresses the 11-keto-βboswellic acid-mediated inhibition of glutamate release.

ω-Conotoxin GVIA is an inhibitor of the N-type Ca2+ channel.

ω-Conotoxin GVIA TFA is an inhibitor of the N-type Ca2+ channel.

ProTx-I, a venom toxin of the tarantula Thrixopelma pruriens, is a potent, selective CaV3.1 channel blocker with IC50 values of 0.2 μM and 31.8 μM for hCaV3.1 and hCaV3.2 respectively. ProTx-I is also a potent blocker for voltage-gated Na+ channels and inhibits KV 2.1 channels.

SNX-482, a peptidyl toxin of the spider Hysterocrates gigas, is a potent, high affinity, selective and voltage-dependent R-type CaV2.3 channel blocker with an IC50 of 30 nM. SNX-482 has antinociceptive effect.

CALP2 is a calmodulin (CaM) antagonist ( (Kd of 7.9 μM)) with high affinity for binding to the CaM EF-hand/Ca2+-binding site. CALP2 inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca2+ concentrations. CALP2 potently inhibits of adhesion and degranulation. CALP2 is also a strong activator of alveolar macrophages.

CALP2 TFA is a calmodulin (CaM) antagonist (Kd of 7.9 μM) with high affinity for binding to the CaM EF-hand/Ca2+-binding site. CALP2 TFA inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca2+ concentrations. CALP2 TFA potently inhibits of adhesion and degranulation. CALP2 TFA is also a strong activator of alveolar macrophages.

CALP1 is a calmodulin (CaM) agonist (Kd of 88 μM) with binding to the CaM EF-hand/Ca2+-binding site. CALP1 blocks calcium influx and apoptosis (IC50 of 44.78 μM) through inhibition of calcium channel opening. CALP1 blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 activates CaM-dependent phosphodiesterase activity.

CALP1 TFA is a calmodulin (CaM) agonist (Kd of 88 μM) with binding to the CaM EF-hand/Ca2+-binding site. CALP1 TFA blocks calcium influx and apoptosis (IC50 of 44.78 μM) through inhibition of calcium channel opening. CALP1 TFA blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 TFA activates CaM-dependent phosphodiesterase activity.

Huwentoxin XVI, an analgesic, is a highly reversible and selective mammalian N-type calcium channel (IC50 of ~60 nM) antagonist from Chinese tarantula Ornithoctonus huwena. Huwentoxin XVI has no effect on voltagegated T-type calcium channels, potassium channels or sodium channels.

Huwentoxin XVI TFA, an analgesic, is a highly reversible and selective mammalian N-type calcium channel (IC50 of ~60 nM) antagonist from Chinese tarantula Ornithoctonus huwena. Huwentoxin XVI TFA has no effect on voltagegated T-type calcium channels, potassium channels or sodium channels.

ω-Agatoxin TK, a peptidyl toxin of the venom of Agelenopsis aperta, is a potent and selective P/Q type Ca2+ channel blocker. ω-Agatoxin TK inhibits the high K+ depolarisation-induced rise in internal Ca2+ in cerebral isolated nerve endings with an IC50 of of 60 nM. ω-Agatoxin TK has no effect on L-type, N-type, or T-type calcium channels.

ω-Agatoxin IVA is a potent, selective P/Q type Ca2+ channel blocker with IC50s of 2 nM and 90 nM for P-type and Q-type Ca2+ channels, respectively. ω-Agatoxin IVA (IC50, 30-225 nM) inhibits glutamate exocytosis and calcium influx elicited by high potassium. ω-Agatoxin IVA also blocks the high potassium-induced release of serotonin and norepinephrine. ω-Agatoxin IVA has no effect on L-type or N-type calcium channels.

Azumolene (EU4093 free base), a Dantrolene analog, is a muscle relaxant. Azumolene is a ryanodine receptor (RyR) modulator and inhibits the calcium-release through ryanodine receptor. Azumolene can be used for malignant hyperthermia research.

sFTX-3.3 is a Ca2+ channel antagonist with IC50s of approximately 0.24 mM and 0.70 mM against P-type and N-type channels.

Cyclic ADP-ribose ammonium (cADPR ammonium) is a potent second messenger for calcium mobilization that is synthesized from NAD+ by an ADP-ribosyl cyclase. Cyclic ADP-ribose ammonium increases cytosolic calcium mainly by Ryanodine receptor-mediated release from endoplasmic reticulum and also by extracellular influx through the opening of TRPM2 channels.

Ruthenium red (Ammoniated ruthenium oxychloride) is a polycationic dye widely used for electron microscopy (EM) of cells, tissues and vegetative bacteria. Ruthenium red strongly reacts with phospholipids and fatty acids and binds to acidic mucopolysaccharides. Ruthenium red is a L-type calcium current (ICa) blocker.

(Rac)-MEM 1003 is the racemate of MEM 1003. MEM 1003, a dihydropyridine compound, is a potent L-type Ca2+ channel antagonist and has the potential for Alzheimer’s disease research.

1,2,4-Trihydroxybenzene (Hydroxyhydroquinone), a by-product of coffee bean roasting, increases intracellular Ca2+ concentration in rat thymic lymphocytes.

UK-59811 hydrochloride, a Br-dihydropyridine derivative, is a potent bacterial homotetrameric model voltage-gated Ca2+ (CaV) channel CaVAb inhibitor with an IC50 of 194 nM.

MCU-i4 is a negative modulator of the mitochondrial calcium uniporter (MCU) complex that directly binds a specific cleft in MICU1 and decreases mitochondrial Ca2+ influx.,MCU-i4 decreases mitochondrial Ca2+ influx. Docking simulations reveal that MCU-i4 directly binds a specific cleft in MICU1, a key element of the MCU complex that controls channel gating. Accordingly, in MICU1-silenced or deleted cells, the inhibitory effect of MCU-i4 is lost. Moreover, MCU-i4 fails to inhibit mitochondrial Ca2+ uptake in cells expressing a MICU1 mutated in the critical amino acids that forge the predicted binding cleft.[1]

Taurolithocholic acid sodium salt, a potent cholestatic agent, is a potent Ca2+ agonist.

Cav 2.2 blocker 2 is a Cav2.2 calcium channel blocker extracted from patent WO2017046581A1, compound 1. Cav 2.2 blocker 2 can reverses hyperalgesia associated with an injury or inflammation in conjunction with the opioid.

CALP3 TFA, a Ca2+-like peptide, is a potent Ca2+ channel blocker that activates EF hand motifs of Ca2+-binding proteins. CALP3 TFA can functionally mimic increased [Ca2+]i by modulating the activity of Calmodulin (CaM), Ca2+ channels and pumps. CALP3 TFA has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia.

Norverapamil D7 ((±)-Norverapamil D7) hydrochloride is a deuterium labeled Norverapamil. Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.

Ziconotide acetate (SNX-111 acetate), a peptide, is a potent and selective block of N-type calcium channels antagonist. Ziconotide acetate reduces synaptic transmission, and can be used for chronic pain research.

(-)-Denudatin B is an antiplatelet agent. (-)-Denudatin B relaxed vascular smooth muscle by inhibiting the Ca2+ influx through voltage-gated and receptor-operated Ca2+ channels. And (-)-Denudatin B has nonspecific antiplatelet action

Nemadipine-A is a specific inhibitor of the EGL-19 L-type Ca2+ channel. Nemadipine-A, a cell-permeable L-type calcium channel inhibitor, sensitizes TRAIL-resistant cancer cells to this ligand.

HSK16149 is a novel ligand of voltage-gated calcium channel (VGCC) α 2 δ subunit.

Xestospongin C ((-)-Xestospongin C) is a selective, reversible inositol 1,4,5-trisphosphate receptor (IP3R) inhibitor. Xestospongin C acts as an inhibitor of the sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA) pump of internal stores. Xestospongin C blocks IP3-induced Ca2+ release from cerebellar microsomes with an IC50 of 358 nM. Xestospongin C is a valuable tool for investigating the structure and function of IP3Rs and Ca2+ signaling in neuronal and nonneuronal cells.

L-Phenylalanine-13C9,15N ((S)-2-Amino-3-phenylpropionic acid-13C9,15N) is the 13C- and 15N-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals.

L-Phenylalanine-13C9 ((S)-2-Amino-3-phenylpropionic acid-13C9) is the 13C-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals.

L-Phenylalanine-13C6 ((S)-2-Amino-3-phenylpropionic acid-13C6) is the 13C-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals.

L-Phenylalanine-3-13C ((S)-2-Amino-3-phenylpropionic acid-3-13C) is the 13C-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals.

T-Type calcium channel inhibitor is a potent inhibitor of T-Type calcium channel. T-Type calcium channel inhibitor penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. T-Type calcium channel inhibitor has the potential for the research of neurology disease.

TTA-P1 is a potent state-independent compound inhibiting human T-type calcium channel. T-type calcium channels play a role in diverse physiological responses including neuronal burst firing, hormone secretion, and cell growth. TTA-P1 has the potential for the research of absence epilepsy.

Efonidipine (NZ-105) is a potent, dual T-type and L-type calcium channel blocker, exhibits antihypertensive effect through vasodilatation; increases coronary blood flow by blocking L & T-type calcium channels and attenuates myocardial ischaemia, lowers blood pressure in cerebral resistance vessels and prevents hypertension induced brain damage; increases glomerular filtration rate without increasing intra-glomerular pressure and filtration fraction.

Etripamil (MSP-2017) is a novel intranasal non-dihydropyridine calcium channel blocker that has begun phase III clinical trials for the treatment of paroxysmal supraventricular tachycardias.

USP5-Cav3.2 inhibitor II-1 is a small molecule inhibitor of USP5-Cav3.2 interaction, without affecting the enzymatic activity of USP5.II-1 inhibited both phases of formalin-induced nocifensive behaviors in mice.Cav3.2 is required for the action of II-1.II-1 also mediated a robust inhibition of mechanical allodynia induced by injury to the sciatic nerve.

VK-II-86 is a carvedilol analogue lacking antagonist activity at β-adrenoceptors, effectively suppresses SOICR by directly reducing the open duration of the cardiac ryanodine receptor (RyR2).VK-II-86 exhibited >2,000-fold lower beta-AR binding affinity than carvedilol.VK-II-86 prevented stress-induced ventricular tachyarrhythmias in RyR2-mutant mice and did so more effectively when combined with either of the selective beta blockers metoprolol or bisoprolol.VK-II-86 prevented hypokalaemia-induced AP prolongation and depolarization but did not alter AP parameters in normokalaemia.

Fenoverine is an antispasmodic drug and inhibits calcium channel currents. Fenoverine induces rhabdomyolysis.

Cav 2.2/3.2 blocker 1 (Compound 9e) is a neuronal calcium channel blocker with IC50 values of 78 μM and 80 μM against Cav2.2 and Cav3.2, respectively. Cav 2.2/3.2 blocker 1 can penetrate the CNS.

MONIRO-1 is a T-type and N-type calcium channel blocker with IC50 values of 34, 3.3, 1.7 and 7.2 µM against hCav2.2, hCav3.1, hCav3.2 and hCav3.3, respectively.

CXL-1020 is a hydroxylamine-based nitroxyl (HNO) donor. CXL-1020 improves cardiac inotropy/lusitropy and Ca2+ cycling in rats with abnormal relaxation. CXL-1020 induces vasorelaxation and improves cardiac function in canine models. CXL-1020 has been used to research systolic heart failure and stable heart failure.

IAA65 is a potent T-type calcium channel inhibitor with a IC50 value of 18.9 µM. IAA65 can be used for epilepsy research.

IAB15 is a potent T-type calcium channel inhibitor. IAB15 can be used for epilepsy research.

Fasudil (HA-1077; AT877) dihydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil dihydrochloride is also a potent Ca2+ channel antagonist and vasodilator.

SG094 is a potent TPC2 inhibitor with antiproliferative effects. SG-094 can be used for the research of cancer.

2E151 is a small molecule calcium channel activator, increases murine antigen-specific antibody responses when used as a co-adjuvant with LPS.

2D216 is a small molecule calcium channel activator, increases murine antigen-specific antibody responses when used as a co-adjuvant with LPS.

Efonidipine (NZ-105) is a potent, dual T-type and L-type calcium channel blocker, exhibits antihypertensive effect through vasodilatation.

Extracellular vesicle enhancer 634 (Compound 634) is a small molecule enhancer of extracellular vesicle (EV) release with immunostimulatory potency via induction of Ca2+ influx, which is mediated by store-operated Ca2+ entry (SOCE).

IPPQ is a small molecule that selectively target the interface between the N-type calcium (CaV2.2) channel and CaVβ, specifically binds to CaVβ2a and inhibits CaVβ2's interaction with CaV.2-AID (alpha interacting domain).

PST3093 (PST 3093) is the main Istaroxime metabolite and a selective SERCA2a activator, reduces the SERCA2a KdCa value by about 20% at 100 nM.

TMDJ-035 is the first highly potent and selective ryanodine receptor 2 (RyR2) inhibitor with EC50 of 13 nM, shows no effect on RyR1 and RyR3.

TTA-Q6 is a potent, selective T-type Ca2+ channel antagonist with IC50 of 14 nM and 590 nM in FLIPR depolarized assaay and FLIPR hyperpolarized assay, respectively.