PMX-53

PMX-53 (3D53) is a synthetic peptidic and a potent and orally active complement C5a receptor (CD88) antagonist with an IC50 of 20 nM. PMX-53 is also a low-affinity MrgX2 agonist that stimulates MrgX2-mediated mast cell degranulation. PMX-53 specifically binds to C5aR1 and does not bind to the second C5aR (C5L2) and C3aR. PMX-53 has anti-inflammatory, anticancer and antiatherosclerotic effects[1][2][3][4][5][6].

Product Specifications

CAS Number

[219639-75-5]

Product Name Alternative

3D53

UNSPSC

12352209

Target

Complement System

Type

Reference compound

Related Pathways

Immunology/Inflammation

Applications

COVID-19-immunoregulation

Field of Research

Cancer; Inflammation/Immunology; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/pmx-53.html

Purity

99.85

Solubility

DMSO : 100 mg/mL (ultrasonic) |H2O : ≥ 50 mg/mL

Smiles

O=C(N[C@H](C(NCCC[C@@H]1NC([C@@H](NC(C)=O)CC2=CC=CC=C2)=O)=O)CCCNC(N)=N)[C@@H](NC([C@H](NC([C@@](CCC3)([H])N3C1=O)=O)CC4CCCCC4)=O)CC5=CNC6=CC=CC=C56

Molecular Formula

C47H65N11O7

Molecular Weight

896.09

References & Citations

[1]Subramanian H, et al. PMX-53 as a dual CD88 antagonist and an agonist for Mas-related gene 2 (MrgX2) in human mast cells. Mol Pharmacol. 2011 Jun;79 (6) :1005-13.|[2]Ting E, et al. Role of complement C5a in mechanical inflammatory hypernociception: potential use of C5a receptor antagonists to control inflammatory pain. Br J Pharmacol. 2008 Mar;153 (5) :1043-53.|[3]Holland MC, et al. Synthetic small-molecule complement inhibitors. Curr Opin Investig Drugs. 2004 Nov;5 (11) :1164-73.|[4]Finch AM, et al. Low-molecular-weight peptidic and cyclic antagonists of the receptor for the complement factor C5a. J Med Chem. 1999 Jun 3;42 (11) :1965-74.|[5]Manthey HD, et al. Complement C5a inhibition reduces atherosclerosis in ApoE-/- mice. FASEB J. 2011 Jul;25 (7) :2447-55.|[6]Vadrevu SK, et al. Complement c5a receptor facilitates cancer metastasis by altering T-cell responses in the metastatic niche. Cancer Res. 2014 Jul 1;74 (13) :3454-65.