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PAT-048

Names

[ CAS No. ]:
1359983-15-5

[ Name ]:
PAT-048

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)
Research Areas >> Inflammation/Immunology

[Target]

IC50: 20 nM (Autotaxin, in mouse plasma)[1] IC90: 200 nM (Autotaxin, in mouse plasma)[1]


[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C22H18ClF2N3O2S

[ Molecular Weight ]:
461.91

Related Compounds