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Lipids in Health & Disease - Dyslipidemias
Model 35840 - PMX-53 (Trifluoroacetate Salt)
PMX-53 is a macrocyclic complement 5a (C5a) peptidomimetic and an antagonist of the C5a receptor (IC50 = 0.3 µM).1 It inhibits C5a-induced secretion of myeloperoxidase (MPO) in isolated human polymorphonuclear leukocytes (PMNs). PMX-53 (10 mg/kg, p.o.) inhibits vascular leakage, PMN infiltration, and peritoneal TNF-α and IL-6 production in a rat model of the peritoneal Arthus reaction.1 It reduces body weight loss and anorexia and inhibits striatal degeneration in a rat model of Huntington’s disease induced by 3-nitropropionic acid (3-NP; Item No. 14684).2 PMX-53 (3 mg/kg) also reduces atherosclerotic lesion size and lipid content in ApoE-/- mice.3
Model 37481 - SP-8356
SP-8356 is a derivative of (1S)-(–)-verbenone and an inhibitor of CD147, also known as extracellular matrix metalloproteinase (MMP) inducer (EMMPRIN) and previously known as tumor cell-derived collagenase stimulatory factor (TCSF).1,2 It inhibits the dimerization of CD147 and the protein-protein interaction between CD147 and its ligand cyclophilin A. SP-8356 (10 µM) decreases recombinant human CD147-induced migration of A-10 vascular smooth muscle cells (VSMCs) and reduces cyclophilin A-induced increases in MMP-9 activity in, and adhesion of, isolated rat monocyte-derived macrophages. It also prevents glucose-oxygen deprivation-induced increases in reactive oxygen species (ROS) and lactate dehydrogenase (LDH) release in primary rat cortical neurons in an in vitro model of ischemia when used at a concentration of 10 µM.3 SP-8356 (5 µM) inhibits the migration and invasion of MDA-MB-231 breast cancer cells.
Lipids for Pharmaceutical Development - Lipid-Based Drug Delivery
Model 34274 - 1,2-Dioleoyl-sn-glycero-3-PA (sodium salt)
1,2-Dioleoyl-sn-glycero-3-PA is a phospholipid containing the long-chain (18:1) fatty acid oleic acid (Item Nos. 90260 | 24659) inserted at the sn-1 and sn-2 positions. It has been used in the generation of micelles, liposomes, and other artificial membranes.1,2
