PMX-53

PMX-53

• CAS Number: 219639-75-5
• UNSPSC Description: 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].
• Target Antigen: 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: 99.98
• Solubility: DMSO : 100 mg/mL (ultrasonic)|H2O : 2.5 mg/mL (ultrasonic;warming;heat to 60°C)
• 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 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.
• Shipping Conditions: Blue Ice
• Storage Conditions: -80°C, 2 years; -20°C, 1 year (Powder, sealed storage, away from moisture and light, under nitrogen)
• Clinical Information: Phase 2