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Biological Activity for PMX 53
PMX 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.
Technical Data for PMX 53
(Modifications: Phe-1 = N-terminal Ac, X-2 = Orn, X-4 = D-Cha, Lactam bridge: Orn-2 to Arg-6)
|Storage||Store at -20°C|
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.
Solubility Data for PMX 53
|Solubility||Soluble to 2 mg/ml in water|
References for PMX 53
References are publications that support the biological activity of the product.
Ting et al (2008) Role of complement C5a in mechanical inflammatory hypernociception: potential use of C5a receptor antagonists to control inflammatory pain. Br.J.Pharmacol. 153 1043 PMID: 18084313
Subramanian et al (2011) PMX-53 as a dual CD88 antagonist and an agonist for Mas-related gene 2 (MrgX2) in human mast cells. Mol.Pharmacol. 79 1005 PMID: 21441599
Finch et al (1999) Low-molecular-weight peptidic and cyclic antagonists of the receptor for the complement factor C5a. J.Med.Chem. 42 1965 PMID: 10354404
Vadrevu et al (2014) Complement c5a receptor facilitates cancer metastasis by altering T-cell responses in the metastatic niche. Cancer Res. 74 3454 PMID: 24786787
Manthey et al (2011) Complement C5a inhibition reduces atherosclerosis in ApoE-/- mice. FASEB J 25 2447 PMID: 21490292
Kumar et al (2018) Development and validation of a LC-MS/MS assay for pharmacokinetic studies of complement C5a receptor antagonists PMX53 and PMX205 in mice. Sci.Rep. 8 8101 PMID: 29802264
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Keywords: PMX 53, PMX 53 supplier, PMX53, potent, c5a, complement, system, receptors, antagonists, mrgx2, mas-related, agonists, hypernociception, MRGPRX2, Complement, Mas-related, G, Protein-Coupled, Receptors, 5473, Tocris Bioscience
4 Citations for PMX 53
Citations are publications that use Tocris products. Selected citations for PMX 53 include:
Liu (2018) Orthosteric and allosteric action of the C5a receptor antagonists. Nat Struct Mol Biol 25 472 PMID: 29867214
Sharma et al (2021) Epithelial phenotype restoring drugs suppress macular degeneration phenotypes in an iPSC model. Nat Commun 12 7293 PMID: 34911940
Heping et al (2022) Complement activation contributes to subretinal fibrosis through the induction of epithelial-to-mesenchymal transition (EMT) in retinal pigment epithelial cells. J Neuroinflammation 19 182 PMID: 35831910
Sarah Y et al (2020) Gut Ischemia Reperfusion Injury Induces Lung Inflammation via Mesenteric Lymph-Mediated Neutrophil Activation. Front Immunol 11 586685 PMID: 33042165
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Reviews for PMX 53
Average Rating: 5 (Based on 1 Review.)
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We used this inhibitor to study the biological activity of staphylococcal leukocidin PVL, which uses C5aR as a receptor to target host immune cells. We treated neutrophils with different concentrations (2.5, 5, and 10 uM) of pmx-53 for 1 h before incubated with 1 ug/ml PVL, and the cytotoxicity of treated cells was measured by LDH assay kit. As expected, pmx-53 treatment resulted in a dose-dependent reduction of PVL cytotoxicity to neutrophils.
Literature in this Area
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