autotaxin in 1

Autotaxin-IN-1 is a potent autotaxin inhibitor, which has favorable potency (IC50=2.2 nM), PK properties, and a robust PK PD relationship and it is used in treatment of osteoarthritis pain[1].

Autotaxin modulator 1 is a new modulator of Autotaxin.

Lysophosphatidylcholine 18:2是一种小鼠代谢物，在功能上与亚油酸有关。1-亚油酰-2-羟基-SN-甘油-3-卵磷脂是氧化低密度脂蛋白的主要成分，​​​血浆中低水平的18:2 LysoPC与糖耐量受损、胰岛素抵抗、2 型糖尿病和冠状动脉疾病等代谢紊乱相关。1-Linoleoyl-2-Hydroxy-sn-glycero-3-PC同时也是Autotaxin(LysoPLD)生成溶血磷脂酸(LPA)的底物，在细胞运动中起重要作用。

Sphingomyelins are complex membrane lipids composed of phosphorylcholine, sphingosine, and an acylated group, such as a fatty acid. Lysosphingomyelin is a naturally-occurring lipid which is produced by the removal of the acylated group of sphingomyelin by a deacylase. Lysosphingomyelin may, in turn, serve as a substrate for autotaxin, which removes choline to produce sphingosine-1-phosphate. The receptors and signaling pathways that are activated by lyso-sphingosine are diverse and vary between cell types. Lysosphingomyelin occurs naturally in plasma, is a constituent of lipoproteins, and is increased in some diseases, including dermatitis and Niemann-Pick disease.

ATX inhibitor 15 (compound 30) is an indole-based carbamate derivative with a strong inhibitory effect on autotaxin (ATX), demonstrated by an IC50 of 2.17 nM. Additionally, ATX inhibitor 15 effectively inhibits ATX activity in vivo and suppresses the expression of pro-fibrotic genes. Furthermore, ATX inhibitor 15 exhibits protective effects in lung fibrosis induced by Bleomycin in mice [1].

Autotaxin-IN-6 (compound 23)，一种ATX (自分泌运动分子)抑制剂，具有30 nM的IC50值，能够减少细胞迁移，适用于抗癌研究。

Palmitoleoyl 3-carbacyclic phosphatidic acid (3ccPA 16:1) 作为一种autotaxin (ATX) 抑制剂，具有中等效力，IC50值为620 nM。该化合物适用于黑色素瘤的研究。

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.