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PMX 205

In stock
Catalog No.
B7787
C5a receptor peptide antagonist
Grouped product items
SizePriceStock Qty
500ug
$156.00
In stock
1mg
$260.00
In stock
5mg
$910.00
In stock

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Background

PMX205 is a cyclic hexapeptide (c[Arg-Trp-D-Cha-Pro-Orn]-Hca), which is an antagonist of the C5a complement receptor. [1]

Human C5a, a complement-derived anaphylatoxin, is a potent mediator of human leukocyte chemotaxis. C5a in particular is a potent inflammatory mediator and signalling through CD88 mediates chemotaxis of leukocytes, vascular permeability could be increased, mast cells release inflammatory mediator and smooth muscle cell contracts and other activities, but all the activities contribute to inflammation and potent tissue damage. C5a-mediated leukocyte chemotaxis release from cytochalasin B-treated cells closely paralleled uptake of the ligand, clearly indicating that it is a receptor-C5a interaction that leads to stimulation of these cellular responses. [2]

PMX205 have been shown to be effective in causing a significant reduction in fibrillar amyloid deposits and activated glia in two mouse models of Alzheimer’s disease. PMX205 -treated rats exhibited reduced striatal lesion size, apoptosis, neutrophil infiltration, and hemorrhage.[3]

PMX205 is used as anti-inflammatory drug. PMX205 significantly prevented DSS-induced colon inflammation, and dealed with PMX205, subjected rats had lower pro-inflammatory. Additionally, the levels of anti-inflammatory cytokines IL-4 and IL-10 were increased. PMX205 did not affect C5a’s levels. The positive effect of PMX205 was seen in two strains of mice of differing sensitivities to DSS inflammation. Pharmacological inhibition of C5a activity by PMX205 is efficacious in preventing DSS-induced colitis.[3]

References:
[1] Delisle Milton RC, Milton SC, Chamberlin AR.  Improving the Fmoc Solid Phase Synthesis of the Cyclic Hexapeptide Complement C5a Antagonist, PMX205. Int J Pept Res Ther. 2011 Dec;17(4):337-342.
[2] Chenoweth DE, Hugli TE.  Demonstration of specific C5a receptor on intact human polymorphonuclear leukocytes. Proc Natl Acad Sci U S A. 1978 Aug;75(8):3943-7.
[3] Jain U, Woodruff TM, Stadnyk AW.  The C5a receptor antagonist PMX205 ameliorates experimentally induced colitis associated with increased IL-4 and IL-10. Br J Pharmacol. 2013 Jan;168(2):488-501.

Chemical Properties

Physical AppearanceWhite lyophilised solid
StorageStore at -20°C
M.Wt839.05
Cas No.514814-49-4
FormulaC45H62N10O6
SolubilitySoluble in 20% ethanol / sterile H2O
Chemical NameN-((3S,6R,9R,15R,20aR)-6-((1H-indol-3-yl)methyl)-3-(cyclohexylmethyl)-9-(3-((diaminomethylene)amino)propyl)-1,4,7,10,16-pentaoxoicosahydropyrrolo[1,2-a][1,4,7,10,13]pentaazacyclooctadecin-15-yl)-3-phenylpropanamide
SDFDownload SDF
Canonical SMILESO=C(N1[[email protected]](CCC1)C(N[[email protected]@H](CC2CCCCC2)C3=O)=O)[[email protected]](NC(CCC4=CC=CC=C4)=O)CCCNC([[email protected]@H](CCC/N=C(N)/N)NC([[email protected]@H](CC5=CNC6=CC=CC=C65)N3)=O)=O
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

PMX 205