Calcium Channel Modulator

Mito-TEMPO is a mitochondria-targeted antioxidant. Mito-TEMPO induces mitophagy by activating the PINK1/Parkin pathway, inhibits NLRP3 inflammasome activation, restores mitochondrial membrane potential, and improves renal function and podocyte injury. Mito-TEMPO regulates Ca²⁺ homeostasis, inhibits Bnip3 overexpression, shortens action potential duration, and exerts antiarrhythmic effects. Mito-TEMPO reverses premature senescence, reduces trabecular bone loss, and decreases cell apoptosis. Mito-TEMPO can be used in studies of chronic kidney disease, age-related cardiac dysfunction, postmenopausal osteoporosis, and ischemic stroke.

Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca²⁺ levels by activating Ca²⁺-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin dicyclohexylammonium salt modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model.

MitoTEMPO hydrate is a mitochondria-targeted antioxidant. MitoTEMPO hydrate induces mitophagy by activating the PINK1/Parkin pathway, inhibits NLRP3 inflammasome activation, restores mitochondrial membrane potential, and improves renal function and podocyte injury. MitoTEMPO hydrate regulates Ca²⁺ homeostasis, inhibits Bnip3 overexpression, shortens action potential duration, and exerts antiarrhythmic effects. MitoTEMPO hydrate reverses premature senescence, reduces trabecular bone loss, and decreases cell apoptosis. MitoTEMPO hydrate can be used in studies of chronic kidney disease, age-related cardiac dysfunction, postmenopausal osteoporosis, and ischemic stroke.

Nesiritide (Brain Natriuretic Peptide-32 human) is a recombinant human B-type natriuretic peptide. Nesiritide is a NPRs agonist, with K_d values of 7.3 and 13 pM for NPR-A and NPR-C, respectively. Nesiritide regulates V_1/2 activation/inactivation of the L-type calcium channel. Nesiritide shows vasodilatory, diuretic, and natriuretic activities. Nesiritide is used in cardiovascular diseases such as heart failure and vascular remodeling after arterial injury.

Diacerein (Diacerhein), an orally active anthraquinone, reduces production of IL-1 converting enzyme then inhibits the activation of IL-1β by related downstream signaling. Diacerein is an anti-inflammatory and anti-rheumatic drug. Diacerein can relieve bronchospasm and control airway inflammation in asthmatic mice. Diacerein has the potential for slow acting drug in osteoarthritis (SYSADOA) research.

Pulegone is a monoterpene ketone compound widely present in the essential oils of many plants. Pulegone can also be used as a bird repellent. Pulegone has multiple activities such as anti-inflammatory, antibacterial, antifungal, and anti-hyperalgesic effects. Pulegone is particularly effective against bacteria of the Salmonella species.

Tetracaine (Amethocaine) is a sodium channel inhibitor and ryanodine receptor (RyR) inhibitor. Tetracaine blocks sodium conduction across nerve cell membranes, preventing rapid sodium ion influx and depolarization. Tetracaine exhibits biphasic effects on spontaneous sarcoplasmic reticulum Ca²⁺ release in Ca²⁺-overloaded ventricular myocytes, and increases sarcoplasmic reticulum Ca²⁺ load. Tetracaine can be used in research related to eye diseases.

Palmitoylglycine (N-palmitoyl glycine), an endogenous lipid that acts as a modulator of calcium influx and nitric oxide () production in sensory neurons. Palmitoylglycine is linked to an increased risk of Background Brugada syndrome (BrS) and interacts with BrS-associated proteins, demonstrating moderate binding affinities for DCC, CR1, CTSB, NAAA, DEFB1, EPHA1, IGF1/IGFBP3/ALS, and LTA.

Hypaconitine inhibits the KCNH2 current with an IC₅₀ of 8.1 nM, and exhibits cardiotoxicity. Hypaconitine inhibits TGF-β1-induced epithelial-mesenchymal transition (EMT) in A549 cell through the inhibition of NF-κB nuclear translocation. Hypaconitine acts as the neuromuscular blocker. Hypaconitine is orally active.

REM127 is an orally active, blood-brain barrier-penetrant septin 6/7 molecular glue degrader. REM127 binds to SEPT6 with high affinity and promotes the assembly of SEPT2/6/7 cortical filaments, thereby normalizing cytoplasmic calcium levels, cerebrospinal fluid hyperphosphorylated tau protein levels, synaptic function and cognitive function. REM127 can be used in research related to Alzheimer's disease.

Aladorian (ARM036; S44121) is a non-peptidic ryanodine receptor 2 (RyR2) stabilizer. Aladorian stabilizes RyR2 channels and rectifies abnormal Ca²⁺ handling in cardiomyocytes. Aladorian improves cardiomyocyte Ca²⁺ homeostasis independent of dystrophin restoration. Aladorian attenuates early cardiomyopathy and enhances left ventricular function in a canine muscular dystrophy model. Aladorian can be used for the research of heart failure, Duchenne muscular dystrophy-associated cardiomyopathy and muscular dystrophy.

Cyclandelate is a vasodilator that can be used in the study of claudication, arteriosclerosis, Raynaud's disease, nocturnal leg cramps, and migraines.

Benzocaine hydrochloride is an orally active local anesthetic. Benzocaine hydrochloride non-competitively inhibits the binding of Ca-ATPase to Ca²⁺, with an IC₅₀ of 47.1 mM. Benzocaine hydrochloride exerts anesthetic effects by blocking voltage-gated sodium channels. Benzocaine hydrochloride induces methemoglobinemia in various experimental animals.

4-Bromo A23187 is a halogenated analog of the highly selective calcium ionophore A-23187. 4-Bromo A23187, a calcium modulator, induces apoptosis in different cells, including HL-60 cells.

CBD3063 is a selective modulator of collapsin response mediator protein 2 (CRMP2). CBD3063 uncouples Cav2.2 from CRMP2. CBD3063 reverses neuropathic and inflammatory pain by reducing membrane expression of CaV2.2.

Brevetoxin B (Brevetoxin-2) is a red tide toxin. Brevetoxin B affects sodium, potassium and calcium currents in nerve terminals. Brevetoxin B also modulates the metabolic activity of Jurkat cells, reduces cell viability and induces apoptosis. Brevetoxin B can be used in research on synaptic transmission and tumors.

Lyso-PAF C-18 is a single-chain ether phospholipid with membrane regulatory activity, and Lyso-PAF is the deacetylated inactive precursor of PAF. Lyso-PAF C-18 regulates the activity of plasma membrane Ca²⁺-ATPase, and its mechanism of action may involve altering the lipid microenvironment of this enzyme. Lyso-PAF C-18 activates the calcium ATPase in rat synaptosomal membranes and inhibits the calcium ATPase in rat leukocyte membranes. Lyso-PAF C-18 can be used in cell membrane-related research.

Quinpirole (LY 171555; (-)-LY 141865) is a D2/D3 dopamine receptor agonist and a CaV1.3 calcium channel modulator. Quinpirole normalizes dendritic spine density in dopamine-depleted striatum, upregulates the protein expression of BCL2 and GluR2, downregulates the protein expression of BAX, and delays the onset of seizures. Quinpirole enhances learning and memory, inhibits neuronal apoptosis (apoptosis), and induces anxiety-like, stereotyped, and compulsive behaviors. Quinpirole disrupts prepulse inhibition in rhesus monkeys, enhances the activity of paraventricular thalamic neurons to promote recovery from Isoflurane anesthesia, and alters the composition of the gut microbiota in rats. Quinpirole can be used in research related to dyskinesia, pain, epilepsy, and neurological disorders including anxiety disorder, obsessive-compulsive disorder, and schizophrenia.

SNJ-1945 is an orally active Calpain inhibitor that can cross the blood-brain barrier. SNJ-1945 protects rat hearts against cardiac arrest-reperfusion injury by inhibiting the hydrolysis of α-fodrin. SNJ-1945 inhibits VEGF-induced angiogenesis in retinal endothelial cells. SNJ-1945 also protects SH-SY5Y cells from damage induced by MPP+ (HY-W008719) and Rotenone (HY-B1756). SNJ-1945 exhibits anti-inflammatory and neuroprotective activities in a mouse model of multiple sclerosis. SNJ-1945 can be used for the research of cardiovascular, nervous system and inflammatory diseases.

Monascorubrin is a compound that can be isolated from Monascus mycelia. Monascorubrin has activities such as anti-inflammatory, anti-tumor, antibacterial, and immunomodulatory. Monascorubrin also has certain embryotoxicity, with an ED₅₀ of 4.3 μg for chicken embryos. Monascorubrin can be used for the research of tumors and inflammatory diseases.