A potent antagonist of C5aR
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PMX-205 (trifluoroacetate salt)

Item No. 13607

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N2-(1-oxo-3-phenylpropyl)-L-ornithyl-L-prolyl-3-cyclohexyl-D-alanyl-L-tryptophyl-L-arginine, (5→1)-lactam, 2,2,2-trifluoroacetate
Molecular Formula
C45H62N10O6 • XCF3COOH
Formula Weight
839.1
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH 7.2) (1:6): 0.14mg/ml
λmax
219, 281 nm
SMILES
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.OC(C(F)(F)F)=O
InChi Code
InChI=1S/C45H62N10O6.C2HF3O2/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;3-2(4,5)1(6)7/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);(H,6,7)/t34-,35-,36+,37-,38-;/m0./s1
InChi Key
JPQOMEWKZCTQMA-AZRFDLDXSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $214

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    1 mg

    $341

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    Product Description

    PMX-205 is a cyclic hexapeptide that acts as a potent antagonist of C5a receptor (C5aR; IC50 = 31 nM).1 It is orally active and blocks inflammatory signaling and symptoms in animal models of colitis and allergic asthma.2,3 PMX-205 is also brain penetrant and reduces neuroinflammation and neurodegeneration in an animal model of Alzheimer’s disease.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. March, D.R., Proctor, L.M., Stoermer, M.J., et al. Potent cyclic antagonists of the complement C5a receptor on human polymorphonuclear leukocytes. Relationships between structures and activity. Mol. Pharmacol. 65(4), 868-879 (2004).

    2. Jain, U., Woodruff, T.M., and Stadnyk, A.W. The C5a receptor antagonist PMX205 ameliorates experimentally induced colitis associated with increased IL-4 and IL-10. Br. J. Pharmacol. 168(2), 488-501 (2013).

    3. Staab, E.B., Sanderson, S.D., Wells, S.M., et al. Treatment with the C5a receptor/CD88 antagonist PMX205 reduces inflammation in a murine model of allergic asthma. Int. Immunopharmacol. 21(2), 293-300 (2014).

    4. Fonseca, M.I., Ager, R.R., Chu, S.-H., et al. Treatment with a C5aR antagonist decreases pathology and enhances behavioral performance in murine models of Alzheimer’s disease. J. Immunol. 183(2), 1375-1383 (2009).