704878-75-1
Chemical Structure
TSI-01
- CAS No.: 704878-75-1
- Formula:C14H11Cl2NO4
- Molecular Weight:328.15
IUPAC Name: isopropyl 4-(3,4-dichloro-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)benzoate
InChIKey: LZAMLWVXUVJMPU-UHFFFAOYSA-N
SMILES: O=C(C1=CC=C(N2C(C(Cl)=C(C2=O)Cl)=O)C=C1)OC(C)C
Biological Activity: TSI-01 is a pro-inflammatory phospholipid mediator that is rapidly synthesized by lyso-PAF acetyltransferase (lyso-PAFAT) in response to extracellular stimuli. Two types of lyso-PAFAT have been identified: lysophosphatidylcholine acyltransferase (LPCAT)1, which is mostly expressed in the lungs, and LPCAT2, which is expressed in inflammatory cells. TSI-01 is a selective inhibitor of LPCAT2 (IC50s=0.47 versus 3.02 μM for human LPCAT2 and LPCAT1, respectively). 60 μM it is shown to suppress PAF biosynthesis in mouse peritoneal macrophages stimulated with a calcium ionophore.
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TSI-01 | 98.52% | TSI-01 is a pro-inflammatory phospholipid mediator that is rapidly synthesized by lyso-PAF acetyltransferase (lyso-PAFAT) in response to extracellular stimuli. Two types of lyso-PAFAT have been identified: lysophosphatidylcholine acyltransferase (LPCAT)1, which is mostly expressed in the lungs, and LPCAT2, which is expressed in inflammatory cells. TSI-01 is a selective inhibitor of LPCAT2 (IC50s=0.47 versus 3.02 μM for human LPCAT2 and LPCAT1, respectively). 60 μM it is shown to suppress PAF biosynthesis in mouse peritoneal macrophages stimulated with a calcium ionophore. | ||||||||||||||||||||
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Keywords
