NSC-609249 hydrochloride is an impurity of Verapamil (HY-14275). Verapamil is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor[1][2].
Cycleanine is a potent vascular selective Calcium antagonist. Cycleanine has analgesic, muscle relaxant and anti-inflammatory activities. Cycleanine has potential for anti-ovarian cancer acting through the apoptosis pathway[1][2].
Albanin A, a flavonoid, suppresses glutamate release by decreasing Ca2+/calmodulin/adenylate Cyclase 1 (AC1) activation in synaptosomes and exerts neuroprotective effect in vivo. Albanin A has anti-inflflammatory activity[1].
Dopropidil is a novel anti-anginal calcium ion modulating agent, possessing intracellular calcium antagonist activity and anti-ischemic effects in several predictive animal models.
Ned 19 is a selective membrane-permeant non competitive NAADP antagonist and inhibits NAADP-mediated Ca2+ signaling, with an IC50 of 65 nM[1]. Ned 19 strongly inhibits tumor growth and vascularization as well as lung metastases in mice[2].
Lemildipine is a new dihydropyridine calcium entry blocker.
Calcicludine is a protein toxin from the venom of the green mamba Dendroaspis angusticeps that inhibits high-voltage-activated calcium channel, especially L-type calcium channel with the IC50 of 88 nM. Calcicludine has role in excitatory synaptic transmission[1][2].
Drotaverine (hydrochloride) is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor and an L-type voltage-dependent calcium channel (L-VDCC) blocker, blocks the degradation of 3',5'-cyclic adenosine monophosphate. Drotaverine (hydrochloride) exhibits in vivo antispasmodic efficacy without anticholinergic effects.
L-Ascorbic acid-13C-2-4 is the 13C labeled L-Ascorbic acid. L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collag
Ethaverine hydrochloride, a derivative of papaverine, inhibits cardiac L-type calcium channel. Ethaverine hydrochloride is a peripheral vasodilator and antispasmodic agent. Ethaverine hydrochloride can be used for research of peripheral vascular disease[1][2][3].
Cav 2.2 blocker 1 (compound 9) is a N-type calcium channel (Cav 2.2) blocker for the treatment of pain, with an IC50 of 1 nM[1].
GV-58 is a potent, selective N- and P/Q-type Ca2+ channels agonist with EC50 of 7.21/8.81 uM for N-type/P-Q-type Ca2+ channel; 20-fold less potent CDK inhibitor activity.IC50 value: 7.21/8.81 uM (N-type/P-Q-type Ca2+ channel) [1]Target: Ca2+ channel agonistIn comparison with the parent molecule, (R)-roscovitine, GV-58 has a 20-fold less potent cyclin-dependent kinase antagonist effect, a 3- to 4-fold more potent Ca2+ channel agonist effect, and 4-fold higher efficacy as a Ca2+ channel agonist. GV-58 had no agonist activity (up to 100 μm) on the L-type α-subunit we tested (Cav1.3). In summary, GV-58 greatly improved upon (R)-roscovitine in terms of our properties of interest, with a ～4-fold increase in efficacy as an agonist for N- and P/Q-type Ca2+ channels, a ～3- to 4-fold increase in potency as an agonist for N- and P/Q-type Ca2+ channels, and a 20-fold decrease in potency as a Cdk antagonist.
Ethosuximide-d5 is deuterium labeled Ethosuximide. Ethosuximide, a widely prescribed anti-epileptic drug, improves the phenotypes of multiple neurodegenerative disease models and blocks the low voltage activated T-type calcium channel.
Z944 is a T-type calcium channel antagonist that rescues impairments in crossmodal and visual recognition memory.
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[1][2].
ω-Conotoxin CVIA, a 27 amino acid neuropeptide toxin, is an voltage sensitive calcium channels blocker[1].
Nisoldipine-d7 (BAY-k 5552-d7) is the deuterium labeled Nisoldipine. Nisoldipine(BAY-k 5552) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC50 of 10 nM[1][2].
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+ from the sarcoplasm.
Gabapentin enacarbil (XP-13512) is a prodrug for the anticonvulsant and analgesic drug gabapentin.IC50 Value: Target: Calcium ChannelGabapentin enacarbil is an actively transported prodrug of gabapentin that provides sustained dose-proportional exposure to gabapentin and predictable bioavailability.in vitro: The prodrug (XP-13512) demonstrated active apical to basolateral transport across Caco-2 cell monolayers and pH-dependent passive permeability across artificial membranes. XP13512 inhibited uptake of (14)C-lactate by human embryonic kidney cells expressing monocarboxylate transporter type-1, and direct uptake of prodrug by these cells was confirmed using liquid chromatography-tandem mass spectrometry. XP13512 inhibited uptake of (3)H-biotin into Chinese hamster ovary cells overexpressing human sodium-dependent multivitamin transporter (SMVT) [1].in vivo: In 4 studies of healthy volunteers (136 subjects total), the pharmacokinetics of XP13512 immediate- and extended-release formulations were compared with those of oral gabapentin. XP13512 immediate-release (up to 2800 mg single dose and 2100 mg twice daily) was well absorbed (>68%, based on urinary recovery of gabapentin), converted rapidly to gabapentin, and provided dose-proportional exposure, whereas absorption of oral gabapentin declined with increasing doses to <27% at 1200 mg. Compared with 600 mg gabapentin, an equimolar XP13512 extended-release dose provided extended gabapentin exposure (time to maximum concentration, 8.4 vs 2.7 hours) and superior bioavailability (74.5% vs 36.6%) [2].Toxicity: Gabapentin's most common side effects in adult patients include dizziness, fatigue, weight gain, drowsiness, and peripheral edema (swelling of extremities).
Terodiline is an M1-selective muscarinic receptor (mAChR) antagonist with Kbs of 15, 160, 280, and 198 nM in rabbit vas deferens (M1), atria (M2), bladder (M3) and ileal muscle (M3), respectively. Terodiline also is a Ca2+ blocker. Terodiline acts as a treatment for urinary frequency and urge incontinence[1].
TROX-1 is an N-type calcium channel (CaV2.2) inhibitor with an IC50 value of 0.11 μM. TROX-1 can be used in chronic pain research[1].
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.
Prenylamine is a calcium channel blocker of the amphetamine chemical class. Prenylamine can be used as a vasodilator and can be used for the research of angina pectoris[1].
Fluspirilene is a non-competitive antagonist of L-type calcium channels with an IC50 of 0.03 μM. Fluspirileneis a long-acting injectable depot antipsychotic drug used for schizophrenia.
Calcium Channel antagonist 2 (Compound 154) is a calcium channel antagonist (IC50=5-20 μM). Calcium Channel antagonist 2 can be used in study of calcium channel-mediated diseases such as pain and diabetes[1].
Fasudil (HA-1077; AT877) hydrochloride semihydrate 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 hydrochloride semihydrate is also a potent Ca2+ channel antagonist and vasodilator[1][2][3].