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MedKoo Cat#: 530524 | Name: PMX205
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

PMX205 is a C5a receptor antagonist. PMX205 ameliorates experimentally induced colitis associated with increased IL-4 and IL-10. Pharmacological inhibition of C5a activity by PMX205 is efficacious in preventing DSS-induced colitis, providing further evidence that targeting CD88 in IBD patients could be a valuable therapeutic option PMX205 reduces inflammation in a murine model of allergic asthma.

Chemical Structure

PMX205
PMX205
CAS#514814-49-4

Theoretical Analysis

MedKoo Cat#: 530524

Name: PMX205

CAS#: 514814-49-4

Chemical Formula: C45H62N10O6

Exact Mass: 838.4854

Molecular Weight: 839.06

Elemental Analysis: C, 64.42; H, 7.45; N, 16.69; O, 11.44

Price and Availability

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1mg USD 650.00 2 Weeks
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Related CAS #
No Data
Synonym
PMX205; PMX-205; PMX 205.
IUPAC/Chemical Name
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
InChi Key
VATFHFJULBPYLM-ILOBPARPSA-N
InChi Code
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
SMILES Code
O=C([C@]([H])(CC1=CNC2=C1C=CC=C2)NC([C@@H](CC3CCCCC3)NC([C@]4(N5CCC4)[H])=O)=O)N[C@@H](CCCNC(N)=N)C(NCCC[C@@]([H])(C5=O)NC(CCC6=CC=CC=C6)=O)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
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.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 839.06 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Staab EB, Sanderson SD, Wells SM, Poole JA. Treatment with the C5a receptor/CD88 antagonist PMX205 reduces inflammation in a murine model of allergic asthma. Int Immunopharmacol. 2014 Aug;21(2):293-300. doi: 10.1016/j.intimp.2014.05.008. PubMed PMID: 24859057; PubMed Central PMCID: PMC4108528. 2: 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. doi: 10.1111/j.1476-5381.2012.02183.x. PubMed PMID: 22924972; PubMed Central PMCID: PMC3572573. 3: 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. PubMed PMID: 22707924; PubMed Central PMCID: PMC3375023. 4: Kosni NN, Ganti N, Noor MH, Razak IS, Ajat MM, Omar AR. Expression of complement C5a receptor and the viability of 4T1 tumor cells following agonist-antagonist treatment. J Cancer Res Ther. 2016 Apr-Jun;12(2):590-6. doi: 10.4103/0973-1482.146066. PubMed PMID: 27461615. 5: Ager RR, Fonseca MI, Chu SH, Sanderson SD, Taylor SM, Woodruff TM, Tenner AJ. Microglial C5aR (CD88) expression correlates with amyloid-beta deposition in murine models of Alzheimer's disease. J Neurochem. 2010 Apr;113(2):389-401. doi: 10.1111/j.1471-4159.2010.06595.x. PubMed PMID: 20132482; PubMed Central PMCID: PMC2921960. 6: Breivik T, Gundersen Y, Gjermo P, Taylor SM, Woodruff TM, Opstad PK. Oral treatment with complement factor C5a receptor (CD88) antagonists inhibits experimental periodontitis in rats. J Periodontal Res. 2011 Dec;46(6):643-7. doi: 10.1111/j.1600-0765.2011.01383.x. PubMed PMID: 21722134. 7: Woodruff TM, Costantini KJ, Crane JW, Atkin JD, Monk PN, Taylor SM, Noakes PG. The complement factor C5a contributes to pathology in a rat model of amyotrophic lateral sclerosis. J Immunol. 2008 Dec 15;181(12):8727-34. PubMed PMID: 19050293. 8: Fonseca MI, Ager RR, Chu SH, Yazan O, Sanderson SD, LaFerla FM, Taylor SM, Woodruff TM, Tenner AJ. Treatment with a C5aR antagonist decreases pathology and enhances behavioral performance in murine models of Alzheimer's disease. J Immunol. 2009 Jul 15;183(2):1375-83. doi: 10.4049/jimmunol.0901005. PubMed PMID: 19561098; PubMed Central PMCID: PMC4067320. 9: Lee JD, Kumar V, Fung JN, Ruitenberg MJ, Noakes PG, Woodruff TM. Pharmacological inhibition of complement C5a-C5a(1) receptor signalling ameliorates disease pathology in the hSOD1(G93A) mouse model of amyotrophic lateral sclerosis. Br J Pharmacol. 2017 Jan 27. doi: 10.1111/bph.13730. [Epub ahead of print] PubMed PMID: 28128456. 10: de Vries MR, Wezel A, Schepers A, van Santbrink PJ, Woodruff TM, Niessen HW, Hamming JF, Kuiper J, Bot I, Quax PH. Complement factor C5a as mast cell activator mediates vascular remodelling in vein graft disease. Cardiovasc Res. 2013 Feb 1;97(2):311-20. doi: 10.1093/cvr/cvs312. PubMed PMID: 23071133. 11: Yang F, Li D, Xu S. [The roles of C5a and C5aR antagonist in TNF-α secretion and CD88 expression of BV2 microglial cells treated with Aβ1-42 oligomer]. Xi Bao Yu Fen Zi Mian Yi Xue Za Zhi. 2013 Mar;29(3):265-8. Chinese. PubMed PMID: 23643083. 12: Beck KD, Nguyen HX, Galvan MD, Salazar DL, Woodruff TM, Anderson AJ. Quantitative analysis of cellular inflammation after traumatic spinal cord injury: evidence for a multiphasic inflammatory response in the acute to chronic environment. Brain. 2010 Feb;133(Pt 2):433-47. doi: 10.1093/brain/awp322. PubMed PMID: 20085927; PubMed Central PMCID: PMC2858013. 13: Hernandez MX, Namiranian P, Nguyen E, Fonseca MI, Tenner AJ. C5a Increases the Injury to Primary Neurons Elicited by Fibrillar Amyloid Beta. ASN Neuro. 2017 Feb;9(1):1759091416687871. doi: 10.1177/1759091416687871. PubMed PMID: 28078911; PubMed Central PMCID: PMC5298486. 14: Woodruff TM, Pollitt S, Proctor LM, Stocks SZ, Manthey HD, Williams HM, Mahadevan IB, Shiels IA, Taylor SM. Increased potency of a novel complement factor 5a receptor antagonist in a rat model of inflammatory bowel disease. J Pharmacol Exp Ther. 2005 Aug;314(2):811-7. PubMed PMID: 15879003. 15: Biggins P, Brennan F, Taylor S, Woodruff T, Ruitenberg M. The alternative receptor for complement component 5a, C5aR2, conveys neuroprotection in traumatic spinal cord injury. J Neurotrauma. 2017 Feb 7. doi: 10.1089/neu.2016.4701. [Epub ahead of print] PubMed PMID: 28173736. 16: Fonseca MI, McGuire SO, Counts SE, Tenner AJ. Complement activation fragment C5a receptors, CD88 and C5L2, are associated with neurofibrillary pathology. J Neuroinflammation. 2013 Feb 8;10:25. doi: 10.1186/1742-2094-10-25. PubMed PMID: 23394121; PubMed Central PMCID: PMC3605123. 17: Proctor LM, Woodruff TM, Sharma P, Shiels IA, Taylor SM. Transdermal pharmacology of small molecule cyclic C5a antagonists. Adv Exp Med Biol. 2006;586:329-45. PubMed PMID: 16893082. 18: Woodruff TM, Crane JW, Proctor LM, Buller KM, Shek AB, de Vos K, Pollitt S, Williams HM, Shiels IA, Monk PN, Taylor SM. Therapeutic activity of C5a receptor antagonists in a rat model of neurodegeneration. FASEB J. 2006 Jul;20(9):1407-17. PubMed PMID: 16816116.