PMX 53

Modify Date: 2024-04-14 17:48:39

PMX 53 Structure
PMX 53 structure
Common Name PMX 53
CAS Number 219639-75-5 Molecular Weight 896.089
Density 1.4±0.1 g/cm3 Boiling Point N/A
Molecular Formula C47H65N11O7 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of PMX 53


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.

 Names

Name 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]phenylalaninamidato
Synonym More Synonyms

 PMX 53 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
InChIKey YOKBGCTZYPOSQM-UNHORJANSA-N
SMILES CC(=O)NC(Cc1ccccc1)C(=O)NC1CCCNC(=O)C(CCCN=C(N)N)NC(=O)C(Cc2c[nH]c3ccccc23)NC(=O)C(CC2CCCCC2)NC(=O)C2CCCN2C1=O
Storage condition -20°C

 Synonyms

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
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