PMX 53

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Cat.No. 5473 - PMX 53 | Ac-Phe-cyclo(Orn-Pro-D-Cha-Trp-Arg) | CAS No. 219639-75-5
Description: Potent C5a receptor antagonist
Datasheet
Citations (1)
Reviews
Literature

Biological Activity

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

M. Wt 896.1
Formula C47H65N11O7
Sequence FXPXWR

(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
CAS Number 219639-75-5
PubChem ID 23526550
InChI Key YOKBGCTZYPOSQM-UHFFFAOYSA-N
Smiles NC(=NCCCC1NC(=O)C(NC(=O)C(CC2CCCCC2)NC(=O)C2N(C(=O)C(CCCNC1=O)NC(=O)C(Cc1ccccc1)NC(=O)C)CCC2)Cc1c[nH]c2c1cccc2)N

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solubility Soluble to 2 mg/ml in water

Product Datasheets

Certificate of Analysis / Product Datasheet
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References

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, Complement, 5473, Tocris Bioscience

1 Citation 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


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