calcium ionophore

Ionomycin 是一种钙离子载体和一种结合钙离子(Ca2+)的抗生素。它是由联合链霉菌(Streptomyces conglobatus)产生的。它在研究中用于提高细胞内钙水平(Ca2+)，并作为了解 Ca2+跨生物膜运输的研究工具。Ionomycin 可促进细胞凋亡，诱导蛋白激酶 C (PKC)活化。

Ionomycin calcium (SQ23377 calcium) 是一种有效的，选择性的钙离子载体 (calcium ionophore)，对二价阳离子具有高度特异性 (Ca>Mg>Sr=Ba)。

Monatepil maleate (AJ-2615 maleate) 是一种具有口服活性的 Ca2+-通道和α1-肾上腺素受体拮抗剂，也是非竞争性肝酰辅酶A：胆固醇酰基转移酶（ACAT）抑制剂，具有抗高血压活性。Monatepil maleate 可用于研究高脂血症和动脉粥样硬化。

Oxodipine 是一种二氢吡啶型钙拮抗剂 ，抑制了KCl 诱导的兔主动脉收缩，降低了效力较低的大鼠心室试纸收缩的心脏力量。在大鼠培养的新生儿心室肌细胞中，Oxodipine 降低了L 型Ca 电流（I），IC 为0.24μM，对T 型Ca 电流（I）的IC 为0.41μM。Oxodipine 会使小鼠便秘和狗牙龈增生。

Calcium Ionophore I 在生命科学相关研究中具有广泛的应用。

Calcium ionophore II (N,N,N′,N′-Tetracyclohexyl-3-oxapentanediamide) 是一种亲脂性离子载体，可用于制备钙离子选择性电极。

AACOCF3（Arachidonyl trifluoromethyl ketone）是一种细胞可渗透的三氟甲基酮类花生四烯酸模拟物。它是一个强效且选择性的85-kDa胞质型磷脂酶A2（cPLA2）缓慢结合抑制剂。通过阻止钙离子载体挑战的血小板中花生四烯酸和12-羟基二十四碳五烯酸的生成，AACOCF3抑制了它们的合成。此外，AACOCF3还能抑制从分离的大鼠岛细胞中诱导的葡萄糖引起的胰岛素释放。鉴于其多样的应用，AACOCF3对心血管疾病研究具有潜在的应用价值。

4-Bromo A23187 is a halogenated analog of the calcium ionophore A-23187. 4-Bromo A23187 is a calcium modulator and induces apoptosis in different 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) 是一种抗菌剂。

Torososide B 是一种抗过敏化合物，能够抑制由钙离子载体 A 诱导的大鼠腹膜肥大细胞释放白三烯。

LY255283 是白三烯 B4 (LTB4) 受体的特异性拮抗剂，抑制人外周血多形核白细胞和由钙离子载体 A23187 激活的单核细胞中 LTB(4) 的产生。

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 that contains stearic acid at the sn-1 position and 15(S)-HETE at the sn-2 position. It is formed in human peripheral monocytes activated by the calcium ionophore A23187 by 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，一种具有抗生素功能的独特二价阳离子离子载体（例如钙离子和镁离子），通过提高细胞内钙浓度而诱导Ca2+依赖性细胞死亡。该化合物还能抑制革兰氏阳性细菌和部分真菌生长，同时抑制ATP酶活性并解耦哺乳动物细胞的氧化磷酸化（OXPHOS），触发细胞凋亡（apoptosis）。

Prostaglandin E2抑制剂3是一种microsomal prostaglandin E合酶-1 (mPGES-1; IC50 = 0.2 µM)的抑制剂，相较于COX-1、COX-2、5-lipoxygenase (5-LO)和soluble epoxide hydrolase (sEH)，在10 µM的无细胞试验中表现出对mPGES-1的选择性。在10 µM和1 µM的浓度下，该抑制剂能抑制A549细胞中IL-1β诱导的PGE2生成以及在J774A.1巨噬细胞中，LPS诱导的IL-6和PGE2生成。同时，它还能抑制由钙离子载体A23187单独或结合花生四烯酸和A23187诱导的5-LO产物形成，包括白三烯B4 (LTB4) 和5-H(p)ETE（IC50s分别为4.9和5.2 µM）。在体内，10 mg/kg剂量的Prostaglandin E2抑制剂3能防止在zymosan诱导的小鼠腹膜炎模型中白细胞渗入腹腔液中。

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.

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.

Nesiritide, a 32-amino acid natriuretic peptide and recombinant form of human brain natriuretic peptide, enhances vasorelaxation ex vivo in porcine hearts from an acute coronary occlusion model when given as a 2 µg/kg bolus dose followed by a 0.01 µg/kg per minute infusion, facilitated by the calcium ionophore A23187. Formulations containing nesiritide have been utilized in managing congestive heart failure.