A cell-permeable, orally available, and metabolically stable macrocyclic hexapeptidomimetic compound that acts as a non-competitive antagonist of complement C5a receptor (C5aR; CD88; IC50 = 240 nM) and as a low-affinity agonist for MrgX2, a GPCR, in human mast cells Shown to specifically bind to C5aR1 and not to CaR2 and C3aR. Displays a broad range of anti-inflammatory effects, both in vitro and in vivo. Shown to inhibit C5a-induced neutrophil myeloperoxidase release (IC50 = 22 nM) and chemotaxis (IC50 = 75 nM). Preincubation with PMX-53 (~10 nM) blocks C5a-induced Ca2+ responses in HMC-1 and RBL-2H3 cells, but does not affect C3a responses. Suppresses the growth of 4T1 mammary carcinoma tumor xenograft in mice (1 mg/kg/every 2-3 days, s.c.). Reported to diminish C5a-mediated increase in pluripotency in human embryonic stem cells in the absence of FGF2.
Biochem/physiol Actions
Cell permeable: yes
Primary Target C5aR
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Sequence
Ac-Phe-[Orn-Pro-dCha-Trp-Arg]
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Lillegard, K., et al. 2014. JPET.351,344. Vadrevu, S. K., et al. 2014. Cancer Res.74, 3454. Liang, S., et al. 2011. J. Immun.186, 869. Woodruff, T., et al. 2005. JPET.314, 811.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
13 - Non Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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