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PMX 205 Trifluoroacetate

Cat. No. M10114
PMX 205 Trifluoroacetate Structure
Synonym:

PMX 205 TFA

Size Price Availability Quantity
1mg USD 90  USD90 In stock
5mg USD 240  USD240 In stock
10mg USD 390  USD390 In stock
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Biological Activity

PMX 205 Trifluoroacetate is a potent complement antagonist of C5a (C5aR; CD88) receptor. PMX 205 is orally active, PMX 205 (1 mg/kg/day; oral) treated display a significant extension of survival time and a reduction in end-stage motor scores, as compared with vehicle-treated rats. In 3xTg mice, PMX205 also significantly reduced hyperphosphorylated tau (69%).



Chemical Information
Molecular Weight 953.06
Formula C47H63F3N10O8
CAS Number 514814-49-4 (free base)
Solubility (25°C) DMSO 95 mg/mL
Storage -20°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Nurneqman Nashreq Kosni, et al. J Cancer Res Ther. Expression of complement C5a receptor and the viability of 4T1 tumor cells following agonist-antagonist treatment

[2] Maria I Fonseca, et al. J Immunol. Treatment with a C5aR antagonist decreases pathology and enhances behavioral performance in murine models of Alzheimer's disease

[3] Trent M Woodruff, et al. J Immunol. The complement factor C5a contributes to pathology in a rat model of amyotrophic lateral sclerosis

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Keywords: PMX 205 Trifluoroacetate, PMX 205 TFA supplier, Complement System, inhibitors, activators


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