5.33683

PMX53

≥98% (HPLC), solid, C5aR antagonist, Calbiochem^®

• Synonym(e): C5aR Antagonist, PMX53, Ac-(cyclo-2,6)-F-[OPdChaWR], C5aR Inhibitor, PMX53, C5a Receptor Inhibitor, PMX53, CD88 Inhibitor, PMX53, MrgX2 Agonist, PMX53
• Empirische Formel (Hill-System): C₄₇H₆₅N₁₁O₇ · xC₂HF₃O₂
• CAS-Nummer: 219639-75-5
• Molekulargewicht: 896.09 (free base basis)
• MDL number: MFCD07363866
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: solid
• Quality level: 100
• Storage condition: OK to freeze, protect from light

Eigenschaften

• Produktname: C5aR Antagonist, PMX53,
• assay: ≥98% (HPLC)
• Quality Level: 100
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: off-white
• solubility: DMSO: 50 mg/mL
• storage temp.: 2-8°C

Beschreibung

General description

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

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Ac-Phe-[Orn-Pro-dCha-Trp-Arg]

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

Disclaimer

Toxicity: Standard Handling (A)

Sicherheitshinweise

• Lagerklasse: 13 - Non Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable