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PMX 53

Catalog #: 5473
4 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
5473/1
PMX 53
1 Image
Description: Potent C5a receptor antagonist

Purity: ≥95%

Product Details
Citations (4)
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Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

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

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)

Solubility:
Soluble to 2 mg/ml in water
Purity:
≥95%
Storage:
Store at -20°C
CAS No:
219639-75-5

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.

Additional Information

Other Product-Specific Information:

Background References

  1. Attenuation of cGVHD by C5a/C5aR blockade is associated with increased frequency of Treg
    Y Wang, P Lai, X Chen, C He, X Huang, S Geng, C Luo, S Wu, W Ling, L Zhong, Z Lu, P Li, J Weng, X Du
    Sci Rep, 2017;7(1):3603.
  2. PMX-53 as a dual CD88 antagonist and an agonist for Mas-related gene 2 (MrgX2) in human mast cells.
    Subramanian et al.
    Mol.Pharmacol., 2011;79:1005
  3. Complement C5a inhibition reduces atherosclerosis in ApoE-/- mice.
    Manthey et al.
    FASEB J, 2011;25:2447
  4. 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.
    Sci.Rep., 2018;8:8101
  5. Role of complement C5a in mechanical inflammatory hypernociception: potential use of C5a receptor antagonists to control inflammatory pain.
    Ting et al.
    Br.J.Pharmacol., 2008;153:1043
  6. Low-molecular-weight peptidic and cyclic antagonists of the receptor for the complement factor C5a.
    Finch et al.
    J.Med.Chem., 1999;42:1965
  7. Complement c5a receptor facilitates cancer metastasis by altering T-cell responses in the metastatic niche.
    Vadrevu et al.
    Cancer Res., 2014;74:3454
  8. Mechanisms Driving Neutrophil-Induced T-cell Immunoparalysis in Ovarian Cancer
    TR Emmons, T Giridharan, KL Singel, ANH Khan, J Ricciuti, K Howard, SL Silva-Del, IL Debreceni, CEM Aarts, MC Brouwer, S Suzuki, TW Kuijpers, I Jongerius, LH Allen, VP Ferreira, A Schubart, H Sellner, J Eder, SM Holland, S Ram, JA Lederer, KH Eng, KB Moysich, K Odunsi, MB Yaffe, E Zsiros, BH Segal
    Cancer Immunology Research, 2021;9(7):790-810.

Product Datasheets

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Citations for PMX 53

The citations listed below are publications that use Tocris products. Selected citations for PMX 53 include:

4 Citations: Showing 1 - 4

  1. Complement activation contributes to subretinal fibrosis through the induction of epithelial-to-mesenchymal transition (EMT) in retinal pigment epithelial cells.
    Authors: Heping Et al.
    J Neuroinflammation  2022;19:182
  2. Epithelial phenotype restoring drugs suppress macular degeneration phenotypes in an iPSC model.
    Authors: Sharma Et al.
    Nat Commun  2021;12:7293
  3. Gut Ischemia Reperfusion Injury Induces Lung Inflammation via Mesenteric Lymph-Mediated Neutrophil Activation.
    Authors: Sarah Y Et al.
    Front Immunol  2020;11:586685
  4. Orthosteric and allosteric action of the C5a receptor antagonists.
    Authors: Liu
    Nat Struct Mol Biol  2018;25:472

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