PMX 53

Names

[ CAS No. ]:
219639-75-5

[ Name ]:
PMX 53

[Synonym ]:
Benzenepropanamide, α-(acetylamino)-N-[3-(cyclohexylmethyl)-9-[3-[(diaminomethylene)amino]propyl]eicosahydro-6-(1H-indol-3-ylmethyl)-1,4,7,10,16-pentaoxopyrrolo[1,2-a][1,4,7,10,13]pentaazacyclooct adecin-15-yl]-
Nα-Acetyl-N-[3-(cyclohexylmethyl)-9-{3-[(diaminomethylene)amino]propyl}-6-(1H-indol-3-ylmethyl)-1,4,7,10,16-pentaoxoicosahydropyrrolo[1,2-a][1,4,7,10,13]pentaazacyclooctadecin-15-yl]phenylalaninam idato

Biological Activity

[Description]:

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; inhibits zymosan-, carrageenan-, LPS- and antigen-induced hypernociception in rats.

[References]

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. View Related Products by Target Complement System

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Molecular Formula ]:
C₄₇H₆₅N₁₁O₇

[ Molecular Weight ]:
896.089

[ Exact Mass ]:
895.506836

[ LogP ]:
0.81

[ Index of Refraction ]:
1.684

[ Storage condition ]:
-20°C

Related Compounds

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