PMX 205

Name: PMX 205
Brand: Creative Peptides
SKU: 10-101-154
Availability: MadeToOrder

Potent C5a receptor peptide antagonist (IC50 = 31 nM). Ameliorates experimentally-induced colon inflammation in mice. Reduces fibrillar amyloid deposits, decreases hyperphosphorylated tau levels and rescues cognitive function in a mouse model of Alzheimer's Disease. Orally active and brain penetrant.

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CAT No: 10-101-154

CAS No: 514814-49-4

Synonyms/Alias: PMX 205;514814-49-4;PMX-205;Hydrocinnamate-(orn-Pro-dcha-Trp-Arg);PMX205;DC25O3L7KZ;LP-16;UNII-DC25O3L7KZ;Cyclic hexapeptide complement C5a antagonist;N-[(3S,9S,12S,15R,18S)-15-(cyclohexylmethyl)-9-[3-(diaminomethylideneamino)propyl]-12-(1H-indol-3-ylmethyl)-2,8,11,14,17-pentaoxo-1,7,10,13,16-pentazabicyclo[16.3.0]henicosan-3-yl]-3-phenylpropanamide;ALS-205;CHEBI:144869;hydrocinnamate-cyclo(ornithyl-prolyl-D-cyclohexylalanyl-tryptophyl-arginyl);(5->1)-lactam-N(2)-(1-oxo-3-phenylpropyl)-L-ornithyl-L-prolyl-3-cyclohexyl-D-alanyl-L-tryptophyl-L-arginine;N-[(3R,6S,9S,15S,20aS)-9-(3-carbamimidamidopropyl)-3-(cyclohexylmethyl)-6-(1H-indol-3-ylmethyl)-1,4,7,10,16-pentaoxoicosahydropyrrolo[1,2-a][1,4,7,10,13]pentaazacyclooctadecin-15-yl]-3-phenylpropanamide;HC-[OP(D-Cha)WR];N-((3R,6S,9S,15S,20aS)-9-(3-carbamimidamidopropyl)-3-(cyclohexylmethyl)-6-(1H-indol-3-ylmethyl)-1,4,7,10,16-pentaoxoicosahydropyrrolo(1,2-a)(1,4,7,10,13)pentaazacyclooctadecin-15-yl)-3-phenylpropanamide;N-((3S,9S,12S,15R,18S)-15-(cyclohexylmethyl)-9-(3-(diaminomethylideneamino)propyl)-12-(1H-indol-3-ylmethyl)-2,8,11,14,17-pentaoxo-1,7,10,13,16-pentazabicyclo(16.3.0)henicosan-3-yl)-3-phenylpropanamide;C5a receptor peptide antagonist;GTPL5762;SCHEMBL12971708;EX-A5705;PVA81449;AKOS040735090;DA-56943;HY-110136;CS-0032991;G79478;851-045-5;N-((3R,6S,9S,15S,20AS)-6-((1H-indol-3-yl)methyl)-3-(cyclohexylmethyl)-9-(3-guanidinopropyl)-1,4,7,10,16-pentaoxoicosahydropyrrolo[1,2-a][1,4,7,10,13]pentaazacyclooctadecin-15-yl)-3-phenylpropanamide;

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Specification Technical Data Publications Customer reviews and Q&A

M.F/Formula	C45H62N10O6
M.W/Mr.	839
Sequence	Three Letter Code:hydrocinnamoyl-Orn(1)-Pro-D-Cha-Trp-Arg-(1)
Labeling Target	Complement C5a receptor
Application	PMX-205 is a potent antagonist of C5a receptor. It is used as anti-inflammatory drug.
Appearance	Solid powder
Purity	>98% (or refer to the Certificate of Analysis)
Activity	Agonist
Biological Activity	PMX 205 is a potent C5a receptor peptide antagonist (IC50 = 31 nM).
Areas of Interest	Alzheimer's Disease,Anti-inflammatory
Functions	Toxic substance binding

Source#	Synthetic
Long-term Storage Conditions	Soluble in DMSO.
Shipping Condition	Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Short-term Storage Conditions	Dry, dark and at 0 - 4 °C
Solubility	-20 °C
Organism	Human
InChI	InChI=1S/C45H62N10O6/c46-45(47)49-24-9-18-34-40(57)48-23-10-19-35(51-39(56)22-21-29-12-3-1-4-13-29)44(61)55-25-11-20-38(55)43(60)54-36(26-30-14-5-2-6-15-30)41(58)53-37(42(59)52-34)27-31-28-50-33-17-8-7-16-32(31)33/h1,3-4,7-8,12-13,16-17,28,30,34-38,50H,2,5-6,9-11,14-15,18-27H2,(H,48,57)(H,51,56)(H,52,59)(H,53,58)(H,54,60)(H4,46,47,49)/t34-,35-,36+,37-,38-/m0/s1
InChI Key	VATFHFJULBPYLM-ILOBPARPSA-N
Isomeric SMILES	C1CCC(CC1)C[C@@H]2C(=O)N[C@H](C(=O)N[C@H](C(=O)NCCC[C@@H](C(=O)N3CCC[C@H]3C(=O)N2)NC(=O)CCC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65
BoilingPoint	N/A
ShelfLife	>2 years if stored properly
References	Anti-complement therapies have not been advanced for treating the inflammatory bowel diseases (IBDs) despite a growing body of evidence that blocking C5a protects against induced colitis in rodents. The purpose of this study was to further build on this evidence by examining the efficacy, mechanism and specificity of a potent, non-competitive and orally active C5a receptor (CD88) antagonist, PMX205, in the dextran sulphate sodium (DSS) model of murine innate colitis. Jain, U., Woodruff, T. M., & Stadnyk, A. W. (2013). The C5a receptor antagonist PMX205 ameliorates experimentally induced colitis associated with increased IL‐4 and IL‐10. British journal of pharmacology, 168(2), 488-501. Allergic asthma is a chronic inflammatory airway disease arising from an aberrant immune response following exposure to environmental stimuli in genetically susceptible persons. The complement component 5 (C5)/C5a Receptor (C5aR/CD88) signaling pathway has been implicated in both experimental allergic asthma and human asthmatic disease. Targeting the C5a/C5aR signaling pathway in rodent models has been shown to either enhance or reduce allergic asthma consequences. Treatment with a recombinant humanized monoclonal antibody directed against C5 has shown unclear results in patients with asthma. The objective of this proof-of-concept animal study was to determine whether the low molecular weight C5aR peptidomimetic antagonist, PMX205, would reduce experimental allergic asthma consequences in mice. PMX205 or vehicle control was administered subcutaneously to BALB/c mice prior to and during standard ovalbumin (OVA) allergen sensitization and aerosolized challenge phases. PMX205 substantially reduced OVA-induced total cell (60%), neutrophil (66%) and eosinophil (65%) influxes in lavage fluid sampling. There were also significant reductions in OVA-induced lavage fluid IL-13 protein and lung Th2 cytokine gene expression with PMX205 administration. PMX205 treatment also diminished OVA-induced lung parenchyma cellular infiltration. PMX205 administration did not reduce OVA-induced serum IgE levels or epithelial mucous/goblet cell generation. There was no evidence of toxicity observed with PMX205 treatment in saline or OVA-challenged animals. These data provide evidence that pharmacologic blockade of C5aR by a low molecular weight antagonist (PMX205) reduces airway inflammatory cell and cytokine responses in experimental allergic asthma, and suggests that PMX205 might represent a novel therapeutic agent for reducing asthmatic outcomes. Staab, E. B., Sanderson, S. D., Wells, S. M., & Poole, J. A. (2014). Treatment with the C5a receptor/CD88 antagonist PMX205 reduces inflammation in a murine model of allergic asthma. International immunopharmacology, 21(2), 293-300.
Melting Point	N/A

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