TSI-01

Platelet-activating factor (PAF) 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). At 60 µM it was shown to suppress PAF biosynthesis in mouse peritoneal macrophages stimulated with a calcium ionophore.Formal Name: 4-(3,4-dichloro-2,5-dihydro-2,5-dioxo-1H-pyrrol-1-yl)-benzoic acid, 1-methylethyl ester. CAS Number: 704878-75-1. Molecular Formula: C14H11Cl2NO4. Formula Weight: 328.2. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 50 mg/ml, DMF:PBS (pH 7.2)(1:3): 0.25 mg/ml, DMSO: 30 mg/ml, Ethanol: 1 mg/ml. lambdamax: 245 nm. SMILES: O=C(C(Cl)=C1Cl)N(C2=CC=C(C(OC(C)C)=O)C=C2)C1=O. InChi Code: InChI=1S/C14H11Cl2NO4/c1-7(2)21-14(20)8-3-5-9(6-4-8)17-12(18)10(15)11(16)13(17)19/h3-7H,1-2H3. InChi Key: LZAMLWVXUVJMPU-UHFFFAOYSA-N.