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PMX 205 Trifluoroacetate (514814-49-4 free base)

Catalog No. T12506   CAS T12506
Synonyms: PMX 205 Trifluoroacetate

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

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PMX 205 Trifluoroacetate (514814-49-4 free base) Chemical Structure
PMX 205 Trifluoroacetate (514814-49-4 free base), CAS T12506
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PMX 205 Trifluoroacetate is a potent complement antagonist of C5a receptor.
In vitro PMX205, which is an antagonist, gave more effects towards the cell as compared with the treatment of EP54.
In vivo 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].
Synonyms PMX 205 Trifluoroacetate
Molecular Weight 953.06
Formula C47H63F3N10O8
CAS No. T12506

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (104.93 mM)

H2O: 0.67 mg/mL (0.70 mM), Sonication is recommended.

TargetMolReferences and Literature

1. 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. 2. 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. 3. 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.

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Keywords

PMX 205 Trifluoroacetate (514814-49-4 free base) T12506 Others 514814-49-4 PMX205 Trifluoroacetate PMX 205 Trifluoroacetate (514814 49 4 free base) PMX 205 Trifluoroacetate (514814494 free base) PMX-205 Trifluoroacetate PMX 205 Trifluoroacetate 514814-49-4 free base inhibitor inhibit

 

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