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PMX-53

  Cat. No.:  DC22200   Featured
Chemical Structure
219639-75-5
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More than 5000 active chemicals with high quality for research!
Field of application
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.
Cas No.: 219639-75-5
Chemical Name: Ac-Phe-cyclo(Orn-Pro-D-Cha-Trp-Arg)
Synonyms: PMX53|PMX 53;Ac-Phe-cyclo(Orn-Pro-D-Cha-Trp-Arg);PM-X53
SMILES: N=C(NCCC[C@H](NC([C@@H](NC([C@H](NC([C@H]1N(CCC1)C([C@@H](NC([C@@H](NC(C)=O)CC2=CC=CC=C2)=O)CCCN3)=O)=O)CC4CCCCC4)=O)CC5=CNC6=C5C=CC=C6)=O)C3=O)N
Formula: C47H65N11O7
M.Wt: 896.1
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: 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.
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
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