1359983-15-5
Chemical Structure
PAT-048
- CAS No.: 1359983-15-5
- Formula:C22H18ClF2N3O2S
- Molecular Weight:461.91
IUPAC Name: 3-((6-chloro-7-fluoro-2-methyl-1-(1-propyl-1H-pyrazol-4-yl)-1H-indol-3-yl)thio)-2-fluorobenzoic acid
InChIKey: QNKMXCMJVQFBLM-UHFFFAOYSA-N
SMILES: CCCN1N=CC(N2C3=C(C(SC4=CC=CC(C(O)=O)=C4F)=C2C)C=CC(Cl)=C3F)=C1
Biological Activity: 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].
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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. | |||||||||||||||||||||
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- [1]. Castelino FV, et al. An Autotaxin/Lysophosphatidic Acid/Interleukin-6 Amplification Loop Drives Scleroderma Fibrosis. Arthritis Rheumatol. 2016 Dec;68(12):2964-2974. [Content Brief]
- [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. [Content Brief]
Keywords
