calcium ionophore

Calcium Ionophore I has a wide range of applications in life science related research.

Calcium ionophore II (N,N,N′,N′-Tetracyclohexyl-3-oxapentanediamide) is a lipophilic ionophore utilized in preparing calcium ion-selective electrodes.

Ionomycin is a calcium ion carrier and an antibiotic that binds to calcium ions (Ca2+). The main function of Ionomycin is to induce cellular responses by increasing the intracellular calcium ion concentration. In experiments, Ionomycin is typically used to activate calcium-dependent processes, such as apoptosis and enzyme activity.

Ionomycin calcium (SQ23377 calcium) is an effective and selective calcium ionophore, demonstrating high specificity for divalent cations (Ca>Mg>Sr=Ba).

Monatepil maleate (AJ-2615 maleate) is an orally active Ca2+-channel and α1-adrenoceptor antagonist and non-competitive heparanoyl-coenzyme A:cholesterol acyltransferase (ACAT) inhibitor with antihypertensive activity.Monatepil maleate is used in studies of hyperlipidemia and atherosclerosis. Monatepil maleate is used to study hyperlipidemia and atherosclerosis.

AACOCF3 (Arachidonyl trifluoromethyl ketone) is a cell-permeable trifluoromethyl ketone analog of arachidonic acid and a potent, selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2). By blocking the production of arachidonate and 12-hydroxyeicosatetraenoic acid in calcium ionophore-challenged platelets, AACOCF3 hinders their synthesis. Additionally, AACOCF3 inhibits glucose-induced insulin secretion from isolated rat islets, making it promising for cardiovascular disease research.

Oxodipine, a dihydropyridine-type calcium antagonist, inhibited KCl-induced aortic contraction in rabbits and reduced cardiac force in less potent rat ventricular test-paper contractions. In rat cultured neonatal ventricular myocytes, Oxodipine reduced L-type Ca currents (I) with an IC of 0.24 μM, and against T-type Ca currents (I) with an IC of 0.41 μM. Oxodipine causes constipation in mice and gingival hyperplasia in dogs.

4-Bromo A23187, a halogenated analog of the calcium ionophore A-23187, acts as a calcium modulator and induces apoptosis in various cells.

Calcimycin (A-23187) hemicalcium salt is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). It induces Ca2+-dependent cell death by increasing intracellular calcium concentration.

Lasalocid sodium (Lasalocid-A sodium) is a cationic ionophore antibiotic derived from Streptomyces lasaliensis that disrupts calcium fluxes in muscle fibers. It is primarily used as a coccidiostat, particularly in poultry.

Torososide B is an anti-allergic compound that inhibits leukotriene release from calcium ionophore A-stimulated rat peritoneal mast cells.

LY255283 is a specific antagonit of leukotriene B4 (LTB4) receptor. It inhibits the production of LTB(4) in human peripheral blood polymorphonuclear leukocytes (PMNL) and in monocytes activated by calcium ionophore A23187.

TSI-01, a pro-inflammatory phospholipid mediator, is rapidly synthesized by lyso-PAF acetyltransferase (lyso-PAFAT) in response to extracellular stimuli. Two types of lyso-PAFAT have been identified: LPCAT1, predominantly expressed in lungs, and LPCAT2, expressed in inflammatory cells. TSI-01 is a selective inhibitor of LPCAT2 (IC50 values of 0.47 μM and 3.02 μM for human LPCAT2 and LPCAT1, respectively). At 60 μM, it suppresses PAF biosynthesis in calcium ionophore-stimulated mouse peritoneal macrophages.

Deethylindanomycin is a polyether antibiotic that has been found in S. setonii. It is active against a variety of Gram-positive bacteria, including various strains of S. aureus and Streptococcus, as well as one strain of S. pneumoniae (MICs = 4, 4, and 2 μg/ml, respectively). It is also active against coccidia in vitro, inhibiting E. tenella development, but is inactive against E. tenella infection in chicks when administered at a dose of 200 μg/g in the diet. Deethylindanomycin acts as an ionophore in lipid bilayer membranes and is more selective for potassium ions than calcium, magnesium, and sodium ions. It induces histamine release from rodent mast cells and human basophils in vitro in a calcium-dependent manner.

1-Stearoyl-2-15(S)-HETE-sn-glycero-3-PE is a phospholipid containing stearic acid at the sn-1 position and 15(S)-HETE at the sn-2 position, formed in human peripheral monocytes activated by the calcium ionophore A23187 through direct oxidation of 1-stearoyl-2-arachidonoyl-sn-glycero-3-PE by 15-LO. Phosphoethanolamine (PE) HETEs (PE-HETEs), including 1-stearoyl-2-15(S)-HETE-sn-glycero-3-PE, are the main source of esterified HETE in ionophore-activated monocytes.

The group IVA phospholipase A2 (PLA2), known as calcium-dependent cytosolic PLA2 (cPLA2), selectively releases arachidonic acid (AA) from membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins (PGs) and leukotrienes (LTs). Pyrrophenone inhibits cPLA2α with an IC50 of 4.2 nM in enzyme assays and potently blocks the release of AA and the production of PGE2 and LTC4 in cells (IC50 = 24, 25, and 14 nM, respectively). Its action is reversible and selective, as pyrrophenone inhibits the secretory type IB and IIA PLA2s with more than a hundred-fold less potency. Pyrrophenone has also been shown to inhibit calcium ionophore (A23187)-stimulated AA release from monocytic cells, interleukin-1-induced PGE2 synthesis in mesangial cells, and the production of PGE2, LTs, and platelet-activating factor by human neutrophils, always with maximal inhibition at concentrations below 1 μM.

5(S),12(S)-DiHETE is a natural bioactive lipid derived from arachidonic acid . It is synthesized by glycogen-induced rabbit peritoneal polymorphonuclear leukocytes (PMNLs) incubated with AA. 5(S),12(S)-DiHETE can be produced by successive oxygenation of AA by 5-lipoxygenase (5-LO) in platelets and 12-LO in leukocytes. It can also be synthesized from 12(S)-HETE by 5-LO, in the presence of 5-LO activating protein (FLAP), activated with calcium ionophore. 5(S),12(S)-DiHETE is an epimer of leukotriene B4 that is weakly chemotactic for PMNL.

5(S),15(S)-DiHETE is synthesized by 15-LO from 5(S)-HETE. It potentiates the degranulation of human PMNL in response to PAF, but not fMLP, calcium ionophore A23187, or LTB4. 5(S),15(S)-DiHETE is chemotactic for eosinophils with an ED50 value of 0.3 μM.

Calcimycin (A-23187) hemimagnesium, an antibiotic and divalent cation ionophore (such as calcium and magnesium), serves various biological roles. It triggers Ca2+-dependent cell death by elevating intracellular calcium levels and suppresses the growth of Gram-positive bacteria and certain fungi. Additionally, this compound hinders ATPase activity and uncouples oxidative phosphorylation (OXPHOS) in mammalian cells, ultimately leading to apoptosis [1] [2] [3] [4].

Prostaglandin E2 (PGE2) inhibitor 3 is a selective inhibitor targeting microsomal prostaglandin E synthase-1 (mPGES-1; IC50 = 0.2 µM), demonstrating greater selectivity for mPGES-1 over COX-1, COX-2, 5-lipoxygenase (5-LO), and soluble epoxide hydrolase (sEH) in assays at 10 µM. This compound effectively reduces IL-1β-induced PGE2 production in A549 cells and decreases LPS-induced IL-6 and PGE2 in J774A.1 macrophages at concentrations of 10 and 1 µM, respectively. Additionally, it blocks the production of 5-LO-derived products, including leukotriene B4 (LTB4) and 5-H(p)ETE, in response to calcium ionophore A23187 alone or combined with arachidonic acid, with IC50 values of 4.9 and 5.2 µM, respectively. When administered in vivo at doses of 10 mg/kg, PGE2 inhibitor 3 effectively prevents leukocyte infiltration in a mouse model of zymosan-induced peritonitis.

U-51605, a stable analog of the endoperoxide prostaglandin H2 (PGH2), functions as an inhibitor with greater selectivity towards prostacyclin (PGI) synthase over thromboxane (TX) synthase. It also acts as a partial agonist at TP receptors. Studies show that at a concentration of 2.8 µM, U-51605 effectively inhibits PGI synthase in human foreskin fibroblasts, while a concentration of 5.6 µM is required to inhibit human platelet TX synthase. Furthermore, U-51605, at up to 1 µM, decreases the release of prostacyclin in SHR aorta triggered by the calcium ionophore A-23187 without impacting TXA2 production, and notably enhances the release of PGE2 and PGF2α.

Lasalocid sodium (Standard) is the standard substance of Lasalocid sodium, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Lasalocid sodium (Lasalocid-A sodium) is a cationic ionophore antibiotic obtained from Streptomyces lasaliensis that, among other effects, dissociates the calcium fluxes in muscle fibers. Lasalocid sodium is used as a coccidiostat, especially in poultry.

Morolic acid and moronic acid have shown sustained antidiabetic and antihyperglycemic action possibly mediated by an insulin sensitization with consequent changes of glucose, cholesterol and triglycerides, in part mediated by inhibition of 11β-HSD 1. Moro

Glutinone (IC50=24 microM) shows a significant effect on thromboxane B2 (TXB2)-release induced by calcium ionophore in human platelets.