transcellular

Salcaprozate sodium (SNAC) 是口服吸收促进剂，有作为口服形式的肝素和胰岛素递送剂的潜力。它可提高非共价大分子络合引起的亲脂性，从而增加小肠上皮细胞的被动跨细胞渗透。

VSWRAPTA is a promoter of neuronal branching via transcellular activation of the focal adhesion kinase (FAK) and the ERK1/2 signaling pathway in vitro.

Lipoxin A4 methyl ester (LXA4 methyl ester) is a more lipid soluble, prodrug formulation of the transcellular metabolite LXA4. LXA4 is a trihydroxy fatty acid containing a conjugated tetraene, produced by the metabolism of 15-HETE or 15-HpETE with human leukocytes.[1] LXA4 is equipotent to leukotriene B4 (LTB4) in inducing superoxide generation in human neutrophils at 0.1 μM.[2] LXA4 is associated with several other biological functions including leukocyte activation, chemotaxis effects, natural killer cell inhibition, and monocyte migration and adhesion.[2],[3],[4]

Leukotriene C4 (LTC4) is the parent cysteinyl-leukotriene produced by the LTC4 synthase-catalyzed conjugation of glutathione to LTA4. LTC4 is produced by neutrophils, macrophages, and mast cells, and by transcellular metabolism in platelets. It is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A) and exhibits potent smooth muscle contracting activity. LTC4-induced bronchoconstriction and enhanced vascular permeability contribute to the pathogenesis of asthma and acute allergic hypersensitivity. The concentration of LTC4 required to produce marked contractions of lung parenchymal strips and isolated tracheal rings is about 1 nM. LTC4 methyl ester is a more lipid soluble form of LTC4. The biological activity of LTC4 methyl ester has not been reported.

N-methyl Leukotriene C4 (250 μg/ml solution in ethanol) 是 Leukotriene C4 的一种代谢稳定型合成类似物，可抵抗酶促转化为 LTD4 和 LTE4。N-methyl Leukotriene C4 是研究白三烯信号转导、炎症介质生物学、类二十烷酸代谢及受体相关炎症通路的重要实验工具。

Resolvin E4 (RvE4) is a member of the specialized pro-resolving mediator (SPM) family of bioactive lipids.1It is produced from eicosapentaenoic acid by 15-lipoxygenase (15-LO)via15(S)-HpEPE and 15S-hydroxy, 5S-HpEPE intermediatesin vitroand by isolated human M2 macrophages or polymorphonuclear (PMN) neutrophils under normoxic or hypoxic conditions. RvE4 synthesis is enhanced in M2 macrophage and neutrophil co-cultures, indicating transcellular biosynthesis by a potential 15-LO and 5-LO mechanism. It has been found in mouse inflammatory exudates. RvE4 (10 nM) increases efferocytosis of apoptotic neutrophils or senescent red blood cells (sRBCs) by human M2 macrophages under hypoxic conditionsin vitro. Intraperitoneal administration of RvE4 (100 ng/animal) inhibits increases in inflammatory exudate neutrophil infiltration in a mouse model of hemorrhagic peritonitis induced by zymosan A and thrombin. It also increases inflammatory exudate macrophage infiltration and efferocytosis of apoptotic neutrophils and/or RBCs in the same model. 1.Norris, P.C., Libreros, S., and Serhan, C.N.Resolution metabolomes activated by hypoxic environmentSci. Adv.5(10)eaax4895(2019)

Lipoxin B4 (LXB4) methyl ester is a lipid soluble prodrug form of the transcellular metabolite LXB4 . LXB4 is a positional isomer of LXA4 produced by the metabolism of 15-HETE or 15-HpETE by human leukocytes. At a concentration of 100 nM, LXB4 inhibits polymorphonuclear leukocyte (PMN) migration stimulated by leukotriene B4 and inhibits LTB4-induced adhesion of PMNs with an IC50 value of 0.3 nM.

PBT434 methanesulfonate 为一种有效、口服活性并能穿透血脑屏障的α-synuclein aggregation抑制剂，同时担任铁螯合剂和跨细胞铁运输的调节剂。该化合物抑制铁介导的氧化还原活性及α-synuclein聚集，可有效防止SNpc神经元丢失，显示出在PD研究中的应用潜力。

pTH-Related Protein (1-40) (human, mouse, rat) 促进大鼠肠细胞通过PTHR1受体和PKCα/β信号通路的钙吸收作用。该蛋白增加了甲状旁腺激素1受体（PTHR1）表达，提升了四种跨膜钙转运蛋白—TRPV6、CaBP-D9k、NCX1和PMCA1的水平。

Oleoyl 3-carbacyclic Phosphatidic Acid 属于天然存在的lysophosphatidic acid（LPA）类似物，其结构特征为sn-2羟基与sn-3磷酸基团形成五元环结构。Oleoyl 3-Carbacyclic Phosphatidic Acid (3-ccPA 18:1) 在甘油骨架sn-1位含有18:1脂肪酸oleate，并作为环状LPA类似物发挥作用。在25 μM条件下，Oleoyl 3-Carbacyclic Phosphatidic Acid (3-ccPA 18:1) 可抑制胎牛血清诱导的MM1细胞跨间皮细胞单层迁移达90.1%，并抑制LPA诱导迁移达99.9%，且不影响细胞增殖。此外，在0.1–1.0 μM浓度范围内，Oleoyl 3-Carbacyclic Phosphatidic Acid (3-ccPA 18:1) 可显著抑制autotaxin活性，而autotaxin与肿瘤细胞存活、生长、迁移、侵袭及转移过程相关。这些结果支持Oleoyl 3-Carbacyclic Phosphatidic Acid (3-ccPA 18:1) 在溶血磷脂信号转导、肿瘤细胞生物学、细胞迁移及autotaxin相关机制研究中的应用。

15(R)-HETE, a monohydroxy fatty acid, is synthesized from arachidonic acid via aspirin-acetylated COX-2, leading to the formation of specialized pro-resolving mediators 15(R)-lipoxin A4 and B4 through a transcellular mechanism involving 5-lipoxygenase (5-LO). Additionally, this compound is produced by the cytochrome P450 (CYP) isoform CYP2C9 and can be generated from arachidonic acid by COX-1 in human mast cells, where it accumulates due to its resistance to conversion into 15-KETE by 15-hydroxyprostaglandin dehydrogenase (15-PGDH). As an agonist of PPARβ/δ, 15(R)-HETE induces the expression of a target gene in NIH3T3 cells, demonstrating its biological significance.