Biological ActivityPMX 53 is a potent C5a receptor antagonist (IC50 = 20 nM). Also MrgX2 agonist. Stimulates MrgX2-mediated mast cell degranulation. Also inhibits C5a-induced hypernociception in rats, inhibits lung metastasis in a mouse breast cancer model and reduces atherosclerotic lesions in a mouse model of atherosclerosis.
Negative Control also available.
(Modifications: Phe-1 = N-terminal Ac, X-2 = Orn, X-4 = D-Cha, Lactam bridge: Orn-2 to Arg-6 )
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
PMX-53 as a dual CD88 antagonist and an agonist for Mas-related gene 2 (MrgX2) in human mast cells.
Subramanian et al.
Complement C5a inhibition reduces atherosclerosis in ApoE-/- mice.
Manthey et al.
FASEB J, 2011;25:2447
Development and validation of a LC-MS/MS assay for pharmacokinetic studies of complement C5a receptor antagonists PMX53 and PMX205 in mice.
Kumar et al.
Role of complement C5a in mechanical inflammatory hypernociception: potential use of C5a receptor antagonists to control inflammatory pain.
Ting et al.
Low-molecular-weight peptidic and cyclic antagonists of the receptor for the complement factor C5a.
Finch et al.
Complement c5a receptor facilitates cancer metastasis by altering T-cell responses in the metastatic niche.
Vadrevu et al.
Cancer Res., 2014;74:3454
Citation for PMX 53
The citations listed below are publications that use Tocris products. Selected citations for PMX 53 include:
1 Citation: Showing 1 - 1
Orthosteric and allosteric action of the C5a receptor antagonists.
Nat Struct Mol Biol 2018;25:472
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