lysophosphatidic

1-Oleoyl lysophosphatidic acid sodium (1-Oleoyl lysophosphatidic acid sodium salt) salt 是 LPA1 和 LPA2 的内源性激动剂，可通过诱导 DNA 合成促进有丝分裂，参与正常和病理性情绪反应，如焦虑和抑郁。

LY294002 (SF 1101) 是一种 PI3K 的广谱抑制剂，抑制 PI3Kα、PI3Kδ 和 PI3Kβ (IC50=0.5 0.57 0.97 μM)。LY294002 也是 DNA-PK 抑制剂 (IC50=1.4 μM) 和 CK2 抑制剂 (IC50=98 nM)。LY294002 可以激活凋亡和自噬。

LPA1 receptor antagonist 1(LPA1 R antagonist 1) 是一种具有选择性和高效性的溶血磷脂酸 (LPA1) 受体拮抗剂( IC50 : 25 nM)，可用于研究特发性肺纤维化。

Tetradecyl Phosphonate 是溶血磷脂酸 1 (LPA1)、LPA2 和 LPA3 受体的泛拮抗剂。

LY-294002 hydrochloride (NSC 697286) 是一种合成的 PI3Kα δ β 分子抑制剂（IC50：0.5 0.57 0.97 μM，在无细胞试验中）；在溶液中比 Wortmannin 更稳定，也是自噬体形成的阻断剂。

(R)-Lisofylline ((R)-Lisophylline) 是溶血磷脂酸酰基转移酶的抑制剂 (IC50 = 0.6 µM)。 (R)-Lisofylline 可中断 IL-12 信号介导的 STAT4 激活，可用于治疗 1 型糖尿病和自身免疫性疾病的研究。

AS2717638 是一种具有口服生物活性的，选择性的溶血磷脂酸受体5 (LPA5) 的拮抗剂，其对 hLPA4 的 IC50值为38 nM。AS2717638 还能显著改善 PGE2、PGF2α以及 AMPA 诱导的异位疼痛。

Autotaxin-IN-3 是 Autotaxin 的抑制剂(IC50 = 2.4 nM)，Autotaxin 负责增加腹水和血浆中的溶血磷脂酸。

DBIBB 是一种特异性溶血磷脂酸 (LPA2) 的 2 型 G 蛋白偶联受体的非脂质激动剂，是一种能够治疗高强度γ 射线对造血和胃肠系统引起的急性放射综合征的潜在活性分子 ，是一种作未有机合成和药物研究中的中间体。 DBIBB 可用于制备各种化合物，可减轻胃肠道辐射综合征，增加肠隐窝存活率和肠细胞增殖，并减少细胞凋亡 。

Z-HA155 (CS-963) 是一种高效的 ATX 选择性抑制剂，其 IC50=5.7 nM。

PF8380 是有效的autotaxin 抑制剂，在体外酶实验和人类全血细胞实验中的IC50分别为 2.8 nM 和 101 nM。

ONO-7300243 是溶血磷脂酸受体 1 (LPA1)拮抗剂，IC50为 0.16 μM。

H2L 5765834 是溶血磷脂酸受体 LPA1、LPA3和 LPA5拮抗剂，IC50值分别为 94、752 和 463 nM。

1-Oleoyl Lysophosphatidic Acid (1-Oleoyl LPA) 是一种具有生物活性的磷脂，通过激活至少六种同源 G 蛋白偶联受体及其异源三聚体 G 蛋白的复杂网络，可以在肾脏的各种疾病状态下发挥多种生物效应。1-Oleoyl Lysophosphatidic Acid 促进 BV-2 和原代鼠小胶质细胞向 M1 样表型的极化,可用于研究癌症和动脉粥样硬化。

Lysophosphatidic acid is a bioactive chemical.

1-Arachidonoyl lysophosphatidic acid is a phospholipid containing arachidonic acid at the sn-1 position. It has been found in rat brain as 37% of the arachidonic acid-containing lysophosphatidic acid (LPA) species and is a precursor to 1-arachidonoyl glycerol . 1-Arachidonoyl lysophosphatidic acid binds to the LPA2/EDG4 receptor with an EC50 value of approximately 10 nM. It prevents TNF-α and IL-6 secretion in wild-type but not Lpa2-/- dendritic cells stimulated by LPS. It also decreases differentiation of HT-29 human colon carcinoma cells to goblet cells in the presence of sodium butyrate.

1-Palmitoyl lysophosphatidic acid (1-Palmitoyl LPA) is a LPA analog containing palmitic acid at the sn-1 position. LPA binds to one of five different G protein-coupled receptors (GPCRs) to mediate a variety of biological responses including cell proliferation, smooth muscle contraction, platelet aggregation, neurite retraction, and cell motility. In addition to playing a role in the aforementioned biological responses, 1-palmitoyl LPA enhances the action of β-lactam antibiotics (ampicillin, piperacillin, and ceftazidime) on various strains of Pseudomonas aeruginosa, a pathogen associated with pulmonary disease and pneumonia, via binding both Ca2+ and Mg2+.

1-Linoleoyl LPA（1-亚油酰LPA）是LPA2受体的激动剂，属于一种含有亚油酸的甘油磷脂，在sn-1位置含亚油酸。它是小鼠和人体血浆中最丰富的LPA。1-Linoleoyl LPA在表达LPA2受体的Sf9细胞中选择性地增加细胞内钙水平（EC50约为10 nM），相较于表达LPA1和LPA3受体的Sf9细胞（EC50分别约为200和80 nM）。携带NCTC克隆2472肿瘤的小鼠中，1-linoleoyl LPA的血清水平增加。与患有初发进行性多发性硬化症的患者相比，复发缓解型多发性硬化症患者的血浆1-Linoleoyl LPA水平降低，且与神经功能缺损严重程度负相关。

Oleoyl-L-alpha-lysophosphatidic acid sodium salt为必需的细胞膜生物合成代谢物，可通过与G蛋白偶联受体（GPCR）（即LPA受体）相互作用来介导信号传导，是LPA1和LPA2受体的内源性激动剂。

1-Octadecyl lysophosphatidic acid (1-octadecyl LPA) is a LPA analog containing stearic acid at the sn-1 position. LPA binds to one of five different G protein linked receptors to mediate a variety of biological responses including cell proliferation, smooth muscle contraction, platelet aggregation, neurite retraction, and cell motility. Alkyl ether-linked LPA derivatives have a higher platelet aggregating activity than the acyl derivatives, most likely stemming from an alkyl-specific LPA receptor. For example, 1-octadecyl LPA has a platelet aggregating EC50 value of 9 nM versus 1-octadecanoyl LPA which has an EC50 value of 177 nM.

1-Palmitoyl Lysophosphatidic Acid 是 LPA 的类似物，通过结合 Ca2+ 和 Mg2+ 提高氨苄西林、哌拉西林和头孢他啶对各种铜绿假单胞菌菌株的作用。

1-花生四烯酰基溶血磷脂酸（1-arachidoyl LPA）是溶血磷脂酸受体1（LPA1）的激动剂，并且是一种含有花生四烯酸的甘油磷脂，花生四烯酸位于sn-1位置。它能在主要表达LPA1而非LPA2-LPA6的人类肺成纤维细胞中诱导钙离子动员（EC50 = 3.6 µM）。在无细胞试验中，1-Arachidoyl LPA（2.5 µM）还能结合到过氧化物酶体增殖物激活受体γ（PPARγ）的配体结合域。人类尿液中也发现了该化合物。

LPA5 antagonist 3 (Example 74)，作为一种溶血磷脂酸受体 5 (LPA5) 的拮抗剂，其IC50值为 170 nM。该化合物主要用于对疼痛疾病和动脉粥样硬化进行研究。

LPA receptor antagonist-1 (example 52) 作为溶血磷脂酸(LPA)受体的一种拮抗剂，可广泛应用于多种研究领域。

PAT-048 is an effective and selective autotaxin inhibitor. PAT-048 reduces dermal fibrosis in vivo. PAT-048 also inhibits IL-6 mRNA expression but displays no effect on autotaxin protein and pulmonary lysophosphatidic acid (LPA) production in the lung fibrosis model. PAT-048 has an IC50 and IC90 of 20 nM and 200 nM for autotaxin in mouse plasma.

XY-4是1-棕榈酰基溶血磷脂酸(1-palmitoyl LPA094)的衍生物，同时也是过氧化物酶体增殖物激活受体γ(PPARγ)的激动剂。当浓度为5 µM时，能在表达过氧化物酶体增殖物反应元件(PPRE)的RAW 264.7巨噬细胞中诱导报告基因的表达。XY-4不作为溶血磷脂酸受体1(LPA1)、LPA2或LPA3的激动剂。在1 µM的浓度下，它能在体外诱导血小板聚集。XY-4诱导大鼠颈动脉内膜新生。

BMP-22 is an inhibitor of autotaxin (IC50 = 170 nM). It is selective for autotaxin over the phosphodiesterases NPP6 and NPP7 at 10 μM. BMP-22 (0.1-1,000 nM) inhibits autotaxin-mediated production of lysophosphatidic acid (LPA) from lysophosphatidylcholine in vitro in a concentration-dependent manner. It inhibits LPC-dependent MM1 cell invasion of a human umbilical vein endothelial cell (HUVEC) monolayer. BMP-22 (0.5 mg/kg per day) decreases the number of lung metastatic foci in a B16/F10 syngeneic mouse melanoma model of lung metastasis.

ONO-0740556 是一种有效的 Gi 偶联人类溶血磷脂酸受体1 (LPA1) 激动剂，其EC50值为 0.26 nM。

NAEPA, an LPA mimetic, is a selective agonist of the lysophosphatidic acid-1 (LPA1) receptor.

VPC12249, a lysophosphatidic acid receptor type 1 (LPA1) antagonist, plays a functional role in osteoclast differentiation and bone resorption activity.

Palmitoyl 3-carbacyclic phosphatidic acid，一种棕榈酰化的Carba类环磷脂酸，作为溶血磷脂酸(LPA)的类似物，展现了与LPA不同的功能。该化合物通过抑制RhoA的激活，进而能够阻止黑色素瘤细胞的迁移。在B16-F0异种移植小鼠模型中，Palmitoyl 3-carbacyclic phosphatidic acid有效抑制了实验性肺转移，并显著减少了肿瘤结节的数量。

PAT-347 is a potent Autotaxin Inhibitor. Autotaxin (ATX) is a secreted enzyme responsible for the hydrolysis of lysophosphatidylcholine (LPC) to the bioactive lysophosphatidic acid (LPA) and choline. The ATX-LPA signaling pathway is implicated in cell survival, migration, and proliferation; thus, the inhibition of ATX is a recognized therapeutic target for a number of diseases including fibrotic diseases, cancer, and inflammation, among others.

ONO-9780307 是 LPA1 (lysophosphatidic acid receptor 1) 的特异性拮抗剂 (IC50: 2.7 nM)。

BMS-986020 sodium 是高亲和力的溶血磷脂酸受体 1 (LPA1) 拮抗剂，能够抑制胆汁酸和磷脂转运蛋白，并抑制 BSEP (IC50: 4.8 μM)，MRP4 (IC50: 6.2 μM) 和 MDR3 (IC50: 7.5 μM)。BMS-986020 sodium 表现出特发性肺纤维化 (IPF) 的研究潜力。

DCP-Rho1 is a fluorescent probe for the detection of sulfenic acid-containing proteins.1,2 It displays excitation emission maxima of 560 581 nm, respectively, and has been used to visualize protein oxidation sites in situ. |1. Klomsiri, C., Rogers, L.C., Soito, L., et al. Endosomal H2O2 production leads to localized cysteine sulfenic acid formation on proteins during lysophosphatidic acid-mediated cell signaling. Free Rad. Biol. Med. 71, 49-60 (2014).|2. Holmila, R.J., Vance, S.A., Chen, X., et al. Mitochondria-targeted probes for imaging protein sulfenylation. Sci. Rep. 8(1), 6635 (2018).

Phosphatidic acid is a phospholipid and an intermediate in glycerolipid biosynthesis. It is a transient intermediate in the synthesis of various phospholipid species that is synthesized de novo in cells via multiple routes, including the glycerol-3 phosphate and dihydroxyacetone phosphate pathways, enzymatic conversion of phosphatidylcholine by phospholipase D, and acetylation of lysophosphatidic acid by lysoPA-acyltransferase, among others. It has roles in shaping cellular membranes, cellular signaling, vesicle fission and fusion, as well as mitochondrial division and fusion. It stimulates respiratory burst in neutrophils independent of diacylglycerol and activates monoacylglycerol acyltransferase, phospholipase C (PLC), Ras, and phosphatidylinositol 4-phosphate (PIP4) kinase in several cell lines. Phosphatidic acids (egg) is a mixture of phosphatidic acids isolated from chicken egg with fatty acids of variable chain lengths.

LPA5 antagonist 1 是选择性的、强效的 lysophosphatidic acid receptor 5(LPA5) 拮抗剂，IC50 值为32 nM。LPA5 antagonist 1 具有高脑渗透性和抗痛活性，能够用于研究炎症性和神经性疼痛。

PAT-347 is a potent inhibitor of Autotaxin (ATX), a secreted enzyme responsible for the hydrolysis of lysophosphatidylcholine (LPC) to the bioactive lysophosphatidic acid (LPA) and choline.

ASP6432 is an antagonist of type 1 lysophosphatidic acid receptor (LPA1). For human LPA1 and rat LPA1, the IC50s are 11 nM and 30 nM , respectively.

Cyclic Phosphatidic Acids (cPAs) are naturally occurring lysophosphatidic acid (LPA) analogs, characterized by a 5-membered ring formed between the sn-2 hydroxy group and the sn-3 phosphate. Carba-derivatives of cPA (ccPA) modify the sn-2 (2-ccPA) or sn-3 (3-ccPA) linkage, hindering the conversion of cPA into LPA. Oleoyl 3-Carbacyclic Phosphatidic Acid (3-ccPA 18:1) incorporates the 18:1 fatty acid oleate at the sn-1 position on the glycerol backbone, acting as a cyclic LPA analog. This compound, at a concentration of 25 μM, blocks MM1 cells' transcellular migration through mesothelial cell monolayers induced by fetal bovine serum (by 90.1%) or LPA (by 99.9%), without impeding cell proliferation. Additionally, 3-ccPA 18:1, in the 0.1-1.0 μM range, notably suppresses autotaxin, which plays a vital role in various cancer cell behaviors including survival, growth, migration, invasion, and metastasis.

1-Palmitoyl-d9-2-hydroxy-sn-glycero-3-PA (1-palmitoyl-d9LPA) serves as an internal standard for the quantification of 1-palmitoyl LPA using GC- or LC-MS. This compound, an analog of LPA with palmitic acid at the sn-1 position, activates reporter gene expression in PC12 cells fitted with human lysophosphatidic acid receptor 4 (LPA4) at 0.01 to 10 µM concentrations. Additionally, 1-palmitoyl LPA prompts aggregation in isolated human platelets within the 12-300 µM range, a process reversible by prostaglandin E1 (PGE1), theophylline, or EDTA. It also interacts with calcium and magnesium to boost the efficacy of ampicillin, piperacillin, and ceftazidime against P. aeruginosa strains from cystic fibrosis patients.