Merck - 5.33683.0001 - 5336830001 C5aR Antagonist, PMX53 - Calbiochem

ITEM #: 11575563
A cell-permeable, orally available, and metabolically stable macrocyclic he x apeptidomimetic 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 myelopero x idase release (IC50 = 22 nM) and chemota x is (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 x enograft 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.
Synonyms: C5aR Antagonist, PMX53 - Calbiochem; Ac-(cyclo-2, 6)-F-[OPdChaWR], C5aR Inhibitor, PMX53, C5a Receptor Inhibitor, PMX53, CD88 Inhibitor, PMX53, MrgX2 Agonist, PMX53
Molecular Formula: C47H65N11O7 · x C2HF3O2
Linear Structural Formula: C47H65N11O7 · x C2HF3O2
Purity: >=98% (HPLC)
Biochem Physiol Actions: Reversible: yes
: CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes: Lillegard, K., et al. 2014. , 344.Vadrevu, S. K., et al. 2014. Cancer , 3454.Liang, S., et al. 2011. J. , 869.Woodruff, T., et al. 2005. , 811.
5336830001 C5aR Antagonist, PMX53 - Calbiochem
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