PMX 205 Trifluoroacetate, Inhibitor | PMX205, inhibitor

PMX 205 Trifluoroacetate

Cat. Num. AAA5753710

• Purity: 98.00%
• Synonyms: PMX 205 Trifluoroacetate; PMX205; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: DMSO: 100mg/mL (104.93mM); H2O: 0.67mg/mL (0.70mM) Need ultrasonic; (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C47H63F3N10O8
• SMILES: OC(C(F)(F)F)=O.O=C([C@H](NC([C@@]1([H])N(CCC1)C([C@](NC(CCC2=CC=CC=C2)=O)([H])CCCNC([C@H](CCCNC(N)=N)NC3=O)=O)=O)=O)CC4CCCCC4)N[C@@]3([H])CC5=CNC6=CC=CC=C56
• Target & IC50: Others
• In Vitro: oral delivery of a cyclic hexapeptide C5a receptor antagonist (PMX205) for 2-3 mo resulted in substantial reduction of pathological markers such as fibrillar amyloid deposits (49-62%) and activated glia (42-68%) in two mouse models of AD. The reduction in pathology was correlated with improvements in a passive avoidance behavioral task in Tg2576 mice. In 3xTg mice, PMX205 also significantly reduced hyperphosphorylated tau (69%). These data provide the first evidence that inhibition of a proinflammatory receptor-mediated function of the complement cascade (i.e., C5aR) can interfere with neuroinflammation and neurodegeneration in AD rodent models, suggesting a novel therapeutic target for reducing pathology and improving cognitive function in human AD patients[3].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for PMX205, inhibitor

PMX 205 Trifluoroacetate is a potent complement antagonist of C5a receptor.

References

Kosni NN, et al. 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.
Kosni NN, et al. 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.
Woodruff TM, et al. The complement factor C5a contributes to pathology in a rat model of amyotrophic lateral sclerosis. J Immunol. 2008 Dec 15;181(12):8727-34.
Woodruff TM, et al. The complement factor C5a contributes to pathology in a rat model of amyotrophic lateral sclerosis. J Immunol. 2008 Dec 15;181(12):8727-34.
Fonseca MI, et al. 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.
Fonseca MI, et al. 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.