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PMX53

Chemical Structure : PMX53

CAS No.: 219639-75-5

PMX53 (PMX 53;Ac-Phe-cyclo(Orn-Pro-D-Cha-Trp-Arg))

Catalog No.: PC-35224Not For Human Use, Lab Use Only.

PMX53 (Ac-Phe-cyclo(Orn-Pro-D-Cha-Trp-Arg)) is a potent C5a receptor (CD88) antagonist with IC50 of 20 nM, also is an agonist for Mas-related gene 2 (MrgX2) in human mast cells.

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Biological Activity

PMX53 (Ac-Phe-cyclo(Orn-Pro-D-Cha-Trp-Arg)) is a potent C5a receptor (CD88) antagonist with IC50 of 20 nM, also is an agonist for Mas-related gene 2 (MrgX2) in human mast cells.
PMX-53 (10 nM) inhibited C5a-induced Ca(2+) mobilization in HMC-1 cells, but at higher concentrations (>30 nM) it caused degranulation in LAD2 mast cells, CD34(+) cell-derived mast cells, and RBL-2H3 cells stably expressing MrgX2.
PMX53 inhibits zymosan-, carrageenan-, LPS- and antigen-induced hypernociception in rats.

Physicochemical Properties

M.Wt 896.1
Formula C47H65N11O7
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Ac-Phe-cyclo(Orn-Pro-D-Cha-Trp-Arg)

References

1. Ting E, et al. Br J Pharmacol. 2008 Mar;153(5):1043-53.

2. Subramanian H, et al. Mol Pharmacol. 2011 Jun;79(6):1005-13.

3. Liu H, et al. Nat Struct Mol Biol. 2018 Jun;25(6):472-481.

4. Finch AM, et al. J Med Chem. 1999 Jun 3;42(11):1965-74.

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