An inhibitor of autotaxin (IC50 = 2.8 nM in an enzyme assay); reverses leptin-induced MMP-13 expression in human OA chondrocytes at 10 µM; reduces LPA production by >95% following carrageenan-induced inflammation in rats at 30 mg/kg; inhibits autotaxin activity in human whole blood (IC50 = 101 nM)

PF-8380 – 5 mg

Brand:
Cayman
CAS:
1144035-53-9
Storage:
-20
UN-No:
Non-Hazardous - /

Autotaxin converts lysophosphatidylcholine to lysophosphatidic acid (LPA), which can mediate changes in cell proliferation, angiogenesis, and cytokine secretion.{21340} PF-8380 is a potent inhibitor of autotaxin (IC50 = 2.8 nM in an enzyme assay), the enzyme that converts lysophosphatidylcholine to lysophosphatidic acid (LPA).{21340} It reverses MMP-13 expression induced by leptin in human OA chondrocytes when used at a concentration of 10 µM.{35249} PF-8380 (30 mg/kg) reduces LPA production by >95% following carrageenan-induced inflammation in rats and inhibits autotaxin activity in human whole blood (IC50 = 101 nM).{21340}  

 

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SKU: 12018 - 5 mg Category:

Description

An inhibitor of autotaxin (IC50 = 2.8 nM in an enzyme assay); reverses leptin-induced MMP-13 expression in human OA chondrocytes at 10 µM; reduces LPA production by >95% following carrageenan-induced inflammation in rats at 30 mg/kg; inhibits autotaxin activity in human whole blood (IC50 = 101 nM)

Formal name: 4-[3-(2,3-dihydro-2-oxo-6-benzoxazolyl)-3-oxopropyl]-(3,5-dichlorophenyl)methyl ester-1-piperazinecarboxylic acid

Synonyms: 

Molecular weight: 478.3

CAS: 1144035-53-9

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Immunology & Inflammation

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