Calcium Channel Activator

Acetylcholine-d₉ (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent and BBB-permeable cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs). Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro.

Calenduloside E is a pentacyclic triterpenoid saponin that can be extracted from the bark and roots of Aralia ovata, and has anti-inflammatory and anti-apoptotic activities. Calenduloside E alleviates atherosclerosis by regulating macrophage polarization, improves mitochondrial function by regulating the AMPK-SIRT3 pathway, and alleviates acute liver injury. In addition, Calenduloside E promotes the interaction between L-type calcium channels and Bcl-2 related apoptosis genes, inhibits calcium overload, and alleviates myocardial ischemia/reperfusion injury. Calenduloside E also improves non-alcoholic fatty liver disease by regulating heat shock-dependent pathways, and inhibits ROS mediated JAK1-STAT3 pathways to reduce cellular inflammatory responses.

Nefiracetam is a cognition-enhancing agent. Nefiracetam is an activator of nAChR, N-methyl-D-aspartate receptor (NMDAR), mGluR5, PKC, gamma-aminobutyric acid (GABA), and N/L-type Ca²⁺ channels. Nefiracetam promotes neuroplasticity and enhances neuroprotection. Nefiracetam can be used in Alzheimer's disease, epilepsy, and cerebral ischemia research.

Hirudin (54-65) is a thrombin antagonist and YAP suppressor with anticoagulatory properties.Hirudin (54-65) blocks thrombin's anion binding site, acts on soluble and thrombus-bound thrombin.Hirudin (54-65) suppresses thrombin-induced profibrotic YAP activity, reduces YAP expression, nuclear translocation, and downstream effector signaling in vascular endothelial cells.Hirudin (54-65) ameliorates obstructive cholestasis, attenuates liver fibrosis symptoms, fibrosis-associated angiogenesis, and endothelial-to-mesenchymal transition.Hirudin (54-65) reduces liver inflammation and tissue hypoxia.Hirudin (54-65) promotes extracellular calcium influx through L-type calcium channels in canine coronary artery smooth muscle, mediates contraction.Hirudin (54-65) induces endothelium-independent contraction of canine coronary arterial segments; this response is not affected by indomethacin pretreatment.Hirudin (54-65) can be used for the research of liver obstructive cholestasis, liver fibrosis.

Syringaresinol is a lignan-type phytochemical with anti-inflammatory activities. Syringaresinol inhibits the NF-κB and AKT signaling pathway in IL-1β-activated mouse chondrocytes. Syringaresinol increases phosphorylation of AMPK, eNOS, and intracellular Ca²⁺ levels in HUVECs. Syringaresinol attenuates osteoarthritis progression in mice with Destabilization of the Medial Meniscus (DMM)-induced osteoarthritis. Syringaresinol can be used for the study of osteoarthritis (OA).

ZSET1446 is a novel cognitive enhancer that significantly improves learning deficits in various types of Alzheimer disease (AD) models.

α-L-Rhamnose monohydrate is a neutral sugar present in plants, animals, viruses and bacteria. α-L-Rhamnose monohydrate is a ligand for α-L-rhamnose-recognizing lectin sites, trigger intracellular signaling pathways. α-L-Rhamnose monohydrate induces rhaE and rhaA expression as a specific carbon source in Aspergillus nidulans, while glucose inhibits its cellular uptake. α-L-Rhamnose monohydrate induces rapid and transient increases in intracellular free Ca²⁺ concentration in normal human dermal fibroblasts.

SERCA2a activator 1 (Compound A) is a sarco/endoplasmic reticulum Ca²⁺-dependent ATPase 2a (SERCA2a) activator. SERCA2a activator 1 attenuates phospholamban inhibition and enhances the systolic and diastolic functions of the heart. SERCA2a activator 1 can be used for heart failure.

VHB937 is a potent and selective TREM2 agonist, a human monoclonal antibody, with sub-nanomolar affinity. VHB937 enhances TREM2 surface expression and downstream signaling, such as Syk phosphorylation and calcium mobilization. VHB937 exhibits robust neuroprotective effects in vivo, significantly reducing pathology and pro-inflammatory markers across a broad range of animal models of neuroinflammation and neurodegeneration. VHB937 can be used for neurodegenerative diseases research.

MMK1 is a potent and selective human formyl peptide receptor like-1 (FPRL-1/FPR2) agonist with EC₅₀s of <2 nM and >10000 nM for FPRL-1 and FPR1, respectively. MMK1 is a potent chemotactic and calcium-mobilizing agonist. MMK1 potently activates phagocytic leukocytes and enhances Pertussis Toxin-sensitive production by human monocytes of proinflammatory cytokines IL-1b and IL-6. MMK1 exerts anxiolytic-like activity.

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.

Flubendiamide (NNI-0001) is an orally active phthalic diamide insecticide that acts by targeting insect ryanodine receptors (RyRs), causing insect muscle dysfunction, paralysis and death. Flubendiamide disrupts molting, metamorphosis and reproductive processes, induces oxidative stress by increasing the levels of ROS/RNS, MDA and 8OHdG and decreasing the levels of SOD, CAT and GST, activates the CncC/Maf apoptosis pathway, impairs calcium homeostasis, promotes adipogenesis, increases triglyceride accumulation, and upregulates the expression of regulatory factors for adipocyte differentiation and adipogenesis.

Isopimaric acid is a coniferous tree defense compound. Isopimaric acid binds to AKT and inhibits mTOR phosphorylation, thereby regulating the AKT/mTOR pathway. Isopimaric acid inhibits oxidative stress, inflammation, microglial migration, apoptosis, autophagic flux, ornithine decarboxylase activity, breast cancer proliferation and metastasis, and fungal spore germination. Isopimaric acid also induces M2 microglial polarization, mitochondrial damage, ROS accumulation, starvation-induced colon cancer cell apoptosis, and breast cancer cell cycle arrest. Isopimaric acid activates potassium channels, regulates sodium channels and calcium channels, reduces myocardial excitability, and improves arrhythmia. Isopimaric acid acts as an oxidative substrate for CYP6BW1/3, down-regulates PINK1/Parkin, and regulates calcium homeostasis, oxidative phosphorylation, EMT, and the Wnt pathway. Isopimaric acid exhibits activity against drug-resistant Staphylococcus aureus, repels feeding, and promotes the growth of rice seedlings. Isopimaric acid is suitable for research related to epilepsy, tumors, drug-resistant bacterial infections, atrial fibrillation, hypertension, hyperlipidemia, pulmonary tuberculosis, etc.

Imperatoxin A TFA is a peptide toxin derived from the venom of the African scorpion Pandinus imperator. Imperatoxin A TFA is a Ca²⁺-release channels/ryanodine receptors (RyRs) activator. Imperatoxin A TFA enhances the influx of Ca²⁺ from the sarcoplasmatic reticulum into the cell.

Hexadecylphosphoserine TFA is a phospholipid molecule that contains a long-chain alkyl (hexadecyl) and a phosphoserine group, giving it a high affinity for the cell membrane. Hexadecylphosphoserine TFA can exert antitumor activity by modulating [Ca⁺⁺]_i and its related signaling pathways, making it useful for research in the field of breast cancer.

Hexadecylphosphoserine is a phospholipid molecule that contains a long-chain alkyl (hexadecyl) and a phosphoserine group, giving it a high affinity for the cell membrane. Hexadecylphosphoserine can exert antitumor activity by modulating [Ca⁺⁺]_i and its related signaling pathways, making it useful for research in the field of breast cancer.

2',3'-Cyclic NADP disodium (2',3'-cNADP+; β-Nicotinamide adenine dinucleotide-2',3'-cyclic phosphate) is a substrate for 2',3'-cyclic nucleotide 3'-phosphodiesterase (CNP), an enzyme abundant in myelin. It has been used in a coupled enzyme assay to quantify CNP activity. 2',3'-Cyclic NADP disodium (5 μM) increases calcium overload-induced calcium release and prevents calcium-induced swelling in rat brain mitochondria.

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

VK-II-36 is a carvedilol analog that suppresses sarcoplasmic reticulum Ca²⁺release but does not block the β-receptor.VK-II-36 inhibits triggered activities evoked by both early and delayed after depolarizations.

ISX-9 (Isoxazole 9) is a potent inducer of adult neural stem cell differentiation.