PAT-048

PAT-048 is a potent, selective and orally active autotaxin inhibitor, inhibits IL-6 mRNA expression, but shows no effect on autotaxin protein and pulmonary lysophosphatidic acid (LPA) production in lung fibrosis model. PAT-048 shows an IC50 and IC90 of 20 nM and 200 nM for autotaxin in mouse plasma. PAT-048 reduces dermal fibrosis in vivo[1][2].

Product Specifications

CAS Number

[1359983-15-5]

UNSPSC

12352005

Target

Phosphodiesterase (PDE)

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/pat-048.html

Solubility

10 mM in DMSO

Smiles

CCCN1N=CC(N2C3=C(C(SC4=CC=CC(C(O)=O)=C4F)=C2C)C=CC(Cl)=C3F)=C1

Molecular Formula

C22H18ClF2N3O2S

Molecular Weight

461.91

References & Citations

[1]Castelino FV, et al. An Autotaxin/Lysophosphatidic Acid/Interleukin-6 Amplification Loop Drives Scleroderma Fibrosis. Arthritis Rheumatol. 2016 Dec;68 (12) :2964-2974.|[2]Black KE, et al. Autotaxin activity increases locally following lung injury, but is not required for pulmonary lysophosphatidic acid production or fibrosis. FASEB J. 2016 Jun;30 (6) :2435-50.