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.
|Solubility (25°C)||DMSO 100 mg/mL
Water 10 mg/mL
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|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.
 Yubo Hou, et al. In Vitro Cell Dev Biol Anim. Gingipain of Porphyromonas gingivalis manipulates M1 macrophage polarization through C5a pathway
 George Hajishengallis, et al. Adv Exp Med Biol. Complement Involvement in Periodontitis: Molecular Mechanisms and Rational Therapeutic Approaches
 Haihui Wu, et al. Prog Histochem Cytochem. The Origin, Expression, Function and Future Research Focus of a G Protein-coupled Receptor, Mas-related Gene X2 (MrgX2)
 Hariharan Subramanian, et al. Mol Pharmacol. PMX-53 as a dual CD88 antagonist and an agonist for Mas-related gene 2 (MrgX2) in human mast cells
 Jrg Khl. Curr Opin Mol Ther. Drug evaluation: the C5a receptor antagonist PMX-53
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