PMX 53

Tocris Bioscience, part of Bio-Techne | Catalog # 5473

(1)

Citations (21)

COA / SDS

Potent C5a receptor antagonist

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Product Description
Product Specifications
Solubility
Calculators
Background References
Product Documents
Specific Notices

Key Product Details

Description

Potent C5a receptor antagonist

View all Complement Signaling Compounds »

Product Description

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.

Product Specifications

Molecular Weight

896.10

Formula

C₄₇H₆₅N₁₁O₇

Storage

Store at -20°C

Purity

≥95% (HPLC)

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.

Solubility

Soluble to 2mg/ml in water

Calculators

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Background References

References are publications that support the biological activity of the product.

Kumar Development and validation of a LC-MS/MS assay for pharmacokinetic studies of complement C5a receptor antagonists PMX53 and PMX205 in mice. Sci.Rep. 2018 PMID: 29802264
Manthey Complement C5a inhibition reduces atherosclerosis in ApoE-/- mice. FASEB J 2011 PMID: 21490292
Vadrevu Complement c5a receptor facilitates cancer metastasis by altering T-cell responses in the metastatic niche. Cancer Res. 2014 PMID: 24786787
Finch Low-molecular-weight peptidic and cyclic antagonists of the receptor for the complement factor C5a. J.Med.Chem. 1999 PMID: 10354404
Subramanian PMX-53 as a dual CD88 antagonist and an agonist for Mas-related gene 2 (MrgX2) in human mast cells. Mol.Pharmacol. 2011 PMID: 21441599
Ting Role of complement C5a in mechanical inflammatory hypernociception: potential use of C5a receptor antagonists to control inflammatory pain. Br.J.Pharmacol. 2008 PMID: 18084313