Autotaxin is a specific member of the ectonucleotide pyrophosphatase/phosphodiesterase (NPP2 or ENPP2) family of enzymes that are important for generating the lipid signaling molecule lysophosphatidic acid (LPA). The activity of the secreted phosphodiesterase autotaxin produces the inflammatory signaling molecule LPA and has been associated with a number of human diseases including idiopathic pulmonary fibrosis (IPF).

Our company is offering the synthesis a series of novel (R)-N-(1-(1-(1H-Indazol-5-yl)-3-methyl-2,4-dioxo-1,3,8-triazaspiro[4.5]decan-8-yl)-3-methyl-1-oxobutan-2-yl)-2-fluoro-5-(trifluoromethyl)benzamide derivatives as promising autotaxin inhibitors. A set of novel small compounds will be synthesized exclusively upon your request.

In a recent paper from the J. Med. Chem. 2020*, scientists demonstrated that X-165 is a potent, selective, and bioavailable small molecule inhibitor of the LPA synthetic phosphodiesterase, autotaxin:

C₂₈H₂₈F₄N₆O₄

X-165

pIC₅₀ 7.3 (IC₅₀ 5.5x10^-8 M)

Design and synthesis of small compounds with the high inhibition potency against autotaxin is a perspective area to discover new bioactive compounds for treatment of diseases caused by ATX-LPA signaling disorders.

*J. Med. Chem. 2020, 63, 14, 7840–7856; DOI: 10.1021/acs.jmedchem.0c00688

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