ChemicalBook CAS DataBase List 2408422-41-1

2408422-41-1

Name	SPR206 acetate
CAS	2408422-41-1
Molecular Formula	C54H86ClN15O14
Molecular Weight	1204.82
MOL File	2408422-41-1.mol

Chemical Properties

form	Solid
color	White to off-white

Hazard Information

Uses

SPR206 acetate is a polymyxin analog with antibiotic activity against Gram-negative pathogens, including multidrug-resistant (MDR) variants. SPR206 acetate has an anti-bacterial infection effect by interacting with the bacterium’s outer membrane. The MIC values of SPR206 acetate against Pseudomonas aeruginosa Pa14 and Acinetobacter baumannii NCTC13301 are both 0.125 mg/L[1][2].

in vivo

SPR206 (0.125-30 mg/kg; intravenous injection or subcutaneous injection; every 8 hours or every 4 hours; for 16 hours or 24 hours; neutropenic mice) treatment reduces the burden of Pa14 and NCTC13301 in lung tissue and in the thigh model^[2].

Animal Model:	Neutropenic mice infected Pa14 or NCTC13301^[2]
Dosage:	3 mg/kg, 10 mg/kg, 20 mg/kg, 30 mg/kg (intravenous injection); 0.125 mg/kg, 0.5 mg/kg, 1 mg/kg, 4 mg/kg (subcutaneous injection)
Administration:	Intravenous injection or subcutaneous injection; every 8 hours or every 4 hours; for 16 hours or 24 hours
Result:	In lung tissue, reduced the burden of Pa14 and NCTC13301 by 1.5 and 3.6 log₁₀ CFU/mL. In the thigh model, reduced the burden of Ab13301 by 3.4 and 4.3 log₁₀ CFU/g.

References

[1] Brown P, et al. Design of Next Generation Polymyxins with Lower Toxicity: The Discovery of SPR206. ACS Infect Dis. 2019 Oct 11;5(10):1645-1656. DOI:10.1021/acsinfecdis.9b00217
[2] L. Grosser, et al. In Vivo Efficacy of SPR206 in Murine Lung and Thigh Infection Models Caused by Multidrug Resistant Pathogens Pseudomonas aeruginosa and Acinetobacter baumanii. Poster-139 ASM ESCMID 2018 Lisbon, Portugal.
[3] Noushin Akhoundsadegh, et al. Outer Membrane Interaction Kinetics of New Polymyxin B Analogs in Gram-Negative Bacilli. Antimicrob Agents Chemother. 2019 Sep 23;63(10):e00935-19. DOI:10.1128/AAC.00935-19

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