PMX 53 acetate(219639-75-5 free base)

SKU: orb1296311

Description

PMX-53 is a potent, orally bioavailable antagonist of the complement C5a receptor (CD88), inhibiting C5a-mediated neutrophil responses. It also acts as an agonist for Mas-related G-protein coupled receptor X2 (MrgX2). This compound is widely used in research models of inflammation, including in vivo studies of arthritis, psoriasis, and sepsis.

Research Area

Stem Cell & Developmental Biology

Key Properties

• CAS Number: 852629-88-0
• MW: 956.16
• Purity: 99.91% (May vary between batches)
• Formula: C₄₉H₆₉N₁₁O₉
• SMILES: N=C(N)NCCC[C@@H]1NC([C@H](CC2=CNC3=C2C=CC=C3)NC([C@@H](CC4CCCCC4)NC([C@H]5N(C([C@H](CCCNC1=O)NC([C@H](CC6=CC=CC=C6)NC(C)=O)=O)=O)CCC5)=O)=O)=O.CC(O)=O
• Target: Complement System,Endogenous Metabolite
• Solubility: DMSO:125 mg/mL (130.73 mM);H2O:95.6 mg/mL (99.98 mM)

Bioactivity

• In Vivo:
  Local pretreatment of rats with PMX-53 (60-180 μg per paw) inhibits zymosan-, carrageenan-, lipopolysaccharide (LPS)- and antigen-induced hypernociception. Pharmacokinetic analyses demonstrate that PMX-53 appears in the plasma within 5 min of oral administration (3 mg/kg) to rats, with peak blood levels of approximately 0.3 μM being reached within 20 min. The plasma elimination half-life was approximately 70 min in this case.
• In Vitro:
  In HMC-1 cells, PMX-53 (10 nM) inhibits C5a-induced Ca2+ mobilization, but at higher concentrations( ≥30 nM) it causes degranulation in LAD2 mast cells, CD34+ cell-derived mast cells, and RBL-2H3 cells stably expressing MrgX2. Replacement of Trp with Ala and Arg with dArg eliminates the ability of PMX-53 to inhibit C5a-induced Ca2+ mobilization in HMC-1 cells and to cause degranulation in RBL-2H3 cells expressing MrgX2.

Storage & Handling

• Storage: keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PMX 53 acetate(219639 75 5 free base), PMX 53 acetate(219639755 free base), PMX 53 acetate(219639-75-5 free base), complement 5a receptor (C5aR), ComplementSystem, Complement System

Compound Identifiers

PubChem CID

163285794