Calcium Channel Activator

D-myo-inositol 1,4,5-trisphosphate sodium salt is a widely distributed intracellular second messenger. D-myo-inositol 1,4,5-trisphosphate sodium salt acts as a potent agonist of the Ins (1,4,5) P₃ receptor with an EC₅₀ of 0.12 μM and inhibits bovine PLC-δ1, with an IC₅₀ of 5.4 μM for binding and an IC₅₀ of 12.4 μM for hydrolysis. D-myo-inositol 1,4,5-trisphosphate sodium saltis metabolized into Ins (1,4) P₂ and Ins (1,3,4,5) P₄. D-myo-inositol 1,4,5-trisphosphate sodium salt mediates various cellular processes, including growth, development, fertilization, secretion, contraction and neuromodulation. D-myo-inositol 1,4,5-trisphosphate sodium salt inhibits PIP₂ hydrolysis and Ca²⁺-ATPase activity. D-myo-inositol 1,4,5-trisphosphate sodium salt is used for cardiac preconditioning, exerts cardioprotective effects and mimics ischemic preconditioning. D-myo-inositol 1,4,5-trisphosphate sodium salt is applied in studies related to intracellular calcium and phosphoinositol signaling pathways.

D-myo-Inositol-4-phosphate monoammonium is a metabolite of D-myo-Inositol 1,4,5-trisphosphate. D-myo-Inositol 1,4,5-trisphosphate, a second messenger, elicits Ca²⁺ mobilization. D-myo-Inositol 1,4,5-trisphosphate inhibits the binding of phosphoinositide-specific phospholipase C-delta 1 (PLC-delta 1) to bilayer membranes composed of phosphatidylcholine (PC) and phosphatidylinositol 4,5-bisphosphate (PIP2) .

24-Oxo-25-hydroxyvitamin D3 is a vitamin D3 metabolite and an intermediate in the renal mitochondrial side-chain oxidation pathway. 24-Oxo-25-hydroxyvitamin D3 enhances intestinal calcium transport in rats. 24-Oxo-25-hydroxyvitamin D3 can be used in studies related to X-linked hypophosphatemic rickets.

FPR2 agonist 5 is a selective Formyl Peptide Receptor 2 (FPR2) agonist. FPR2 agonist 5 induces Ca²⁺ mobilization in FPR2-HL60 transfected cells with an EC₅₀ of 1.2 μM and causes FPR2 desensitization with an IC₅₀ of 0.32 μM. FPR2 agonist 5 exerts neuroprotective effects by mitigating LDH release, NO production, IL-1β, IL-6, IL-33, and IL-10 levels in LPS (HY-D1056)-induced mouse primary microglial cells. FPR2 agonist 5 can be used for the study of neuroinflammatory-related diseases.

MRS2690 disodium is a selective P2Y14 receptor agonist. MRS2690 disodium inhibits adenylyl cyclase activity, thereby reducing intracellular cAMP levels and mediating concentration-dependent vasoconstriction of porcine coronary arteries. MRS2690 disodium induces intracellular calcium mobilization, activates P38 and stimulates [³⁵S]GTPγS binding to RBL-2H3 cell membranes. MRS2690 enhances antigen (NP-BSA)-, C3a-induced β-hexosaminidase (β-Hex) release. MRS2690 disodium can be used for ischemic heart disease.

NADH disodium hydrate (Disodium NADH hydrate) is an orally effective reduced coenzyme. NADH disodium hydrate plays a role in regenerating electron donors during cellular energy metabolism, including glycolysis, β-oxidation, and the tricarboxylic acid (TCA) cycle. NADH disodium hydrate regulates calcium homeostasis by promoting the opening of IP3-gated Ca²⁺ channels and inhibiting Ryanodine receptor, and affects mitochondrial function through direct interaction with VDAC. NADH disodium hydrate is used in cytoprotective studies related to cerebral ischemic injury, neurodegenerative diseases, aging, and signal transduction.

Insecticidal agent 39 (compound I ai) is a potent insecticide that targets Ryanodine Receptor (RyR). The LC₅₀ of Insecticidal agent 39 against M. separata is 0.26 mg/L. Insecticidal agent 39 specifically binds to and activates RyR, inducing the release of Ca²⁺ from the sarcoplasmic reticulum into the cytoplasm, which leads to sustained muscle contraction and eventual paralysis and death of the pest. Insecticidal agent 39 can be used in studies related to lepidopteran pest infestation.

SERCA2a activator 2 (Compound 25) is a potent SERCA2a (cardiac type) activator, which also has an activating effect on SERCA1a (skeletal muscle type). SERCA2a activator 2, under [Ca²⁺]MAX conditions activates the ATPase activity of SERCA2a and promotes Ca²⁺ uptake, with its EC₅₀ values being 4 μM and 0.80 μM respectively. SERCA2a activator 2 also exhibits consistent activating effects under more physiological [Ca²⁺]MID conditions. SERCA2a activator 2 has low cytotoxicity and can be used for research on diseases such as heart failure.

Anti-Mouse CD3E Antibody (500A2) is an antibody targeting mouse CD3ε, which specifically binds to the region on CD3ε adjacent to the T cell receptor binding site. Anti-Mouse CD3E Antibody (500A2) triggers functional signal transduction in immature T cells and activates naive T cells. When cross-linked, Anti-Mouse CD3E Antibody (500A2) induces a rapid, robust and transient increase in cytoplasmic calcium concentration, acting as a potent calcium flux inducer. Anti-Mouse CD3E Antibody (500A2) is suitable for multiple experimental techniques such as flow cytometry, immunoprecipitation and EMARS reactions. It can be used to detect CD3E expression on thymocytes, mature T lymphocytes and NK-T cells from different mouse strains, or to identify membrane cluster components of the TCR complex, and shows no cross-reactivity with rat leukocytes.

20:4 Lyso PI acts as an activator of GPR55 and RhoA. 20:4 Lyso PI activates the GPR55-RhoA-ROCK pathway, thereby inducing morphological changes, cytoskeleton assembly, cell rounding and stress fiber formation. 20:4 Lyso PI can be used in research related to diseases such as those of the nervous system.

γ-Glutamylserine TFA (γ-Glu-Ser TFA) is a calcium receptor activator. γ-Glutamylserine TFA can be used for Parkinson's disease research, as well as diabetes or obesity study.

Adenophostin A is an IP₃ receptor (inositol 1,4,5-trisphosphate receptors) modulator and Ca²⁺ releaser, with an IC₅₀ of 1.3 nM, an EC₅₀ of 1.4 nM, and a K_i of 0.18 nM in rats, and an IC₅₀ of 0.95 nM in humans. Adenophostin A activates IP₃ receptors, stimulates Ca²⁺ release from intracellular stores and microsomes, inhibits the binding of [³H]IP₃ to plasma membrane receptors, and activates chloride channels. Adenophostin A resists phosphorylation and dephosphorylation by IP₃ metabolic enzymes to maintain its activity, and increases cytoplasmic [Ca²⁺] levels via calcium mobilization from the endoplasmic reticulum of vascular smooth muscle cells. Adenophostin A is applicable to research related to hemorrhagic shock.

PeS-9 is an Androgen Receptor (AR) degrader that induces androgen receptor degradation PeS-9 induces mitochondrial and ER stress by promoting cytotoxic ROS production, leading to the release of mitochondrial cytochrome C and AIF. PeS-9 subsequently activates caspases-9 and -3, causing DNA fragmentation and apoptotic cell death. PeS-9 has anticancer activity against prostate cancer and exerts in vivo antitumor and antimetastatic activity with minor side effects. PeS-9 can be used for the study of targeting monotherapy against GLUT-1-overexpressing tumors.

PAQ (Compound 4c) is a quinoxaline derivative. PAQ is an orally active neuroprotective agent, which targets dopamine (DA) neurons and activates reticulum endoplasmic ryanodine receptor (RyR) channels, without effects on glia cells.

MCaE12A is a high-affinity modulator of RyR2 and increases RyR2 sensitivity to cytoplasmic calcium concentrations promoting channel opening. MCaE12A acts as an important tool for RyR2 structure-to-function studies as well as for manipulating Ca2+ homeostasis and dynamic of cardiac cell.

Prostaglandin D1-d₄ (PGD1-d₄) is the d₄-labeled Prostaglandin D1 (HY-113096). Prostaglandin D1 (PGD1) is a CatSper activator that triggers Ca²⁺ influx through sperm-specific Ca²⁺ channels via the prostaglandin binding site and competes with other prostaglandins.

Minocycline-d₆ is deuterium labeled Minocycline (HY-17412A). Minocycline is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect.

AZ-DF 265 is a hypoglycemic agent that stimulates insulin release. AZ-DF-265 inhibits ATP-sensitive potassium channels, activates voltage-dependent calcium channels, allows calcium ion influx, and ultimately promotes insulin secretion. AZ-DF 265 can be used in diabetes-related research.

MRS2690 is a selective P2Y14 receptor agonist. MRS2690 inhibits adenylyl cyclase activity, thereby reducing intracellular cAMP levels and mediating concentration-dependent vasoconstriction of porcine coronary arteries. MRS2690 induces intracellular calcium mobilization, activates P38 and stimulates [³⁵S]GTPγS binding to RBL-2H3 cell membranes. MRS2690 enhances antigen (NP-BSA)-, C3a-induced β-hexosaminidase (β-Hex) release. MRS2690can be used for ischemic heart disease.

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