(±)-Lisofylline is a potent anti-inflammatory agent in which only the (-) optical isomer is biologically active. (±)-Lisofylline was found to inhibit the generation of phosphatidic acid from cytokine-activated lysophosphatidic acyl transferase. Lisofylline was able to suppress IFN-γ production, reduce the onset of insulitis and diabetes, and inhibit diabetes.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO 10 mM|
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MRE-269(ACT-333679) is a prostaglandin I2 (IP) receptor agonist with a binding affinity for the human IP receptor that is 130-fold greater than that for other human prostanoid receptor.
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PMX-53 is a potent CD88 (C5aR) antagonist that inhibits C5a-induced neutrophil myeloperoxidase release and chemotaxis with IC50 values of 22 nM and 75 nM, respectively. PMX-53 is also a low-affinity MrgX2 agonist that stimulates MrgX2-mediated mast cell degranulation. PMX-53 has anti-inflammatory, anti-cancer and anti-atherosclerotic effects.
Perflubron (1-Bromoperfluorooctane, Perfluorooctyl bromide, Oxygent, PFOB) exhibits anti-inflammatory activity thus decreases cytokine production in human alveolar macrophages. Perflubron also attenuates oxidative damage to both biological and nonbiological systems which is independent of its anti-inflammatory properties.
Adelmidrol is an analogue of palmitoylethanolamide (PEA) with anti-inflammatory activities.
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