PA-824 Inhibitor CAS No. 187235-37-6

Cat. No.	Name	Size	Price
KI0567	PA-824	5 mg	$336
	PA-824	10 mg	$432
	PA-824	50 mg	$1552
	PA-824	200 mg	$3472

Chemical Characteristic

Product Name	PA-824
CAS No.	187235-37-6
Molecular Weight	359.26
Formula	C₁₄H₁₂F₃N₃O₅
Chemical Name	(S)-6,7-Dihydro-2-nitro-6-[[4-(trifluoromethoxy)phenyl]methoxy]-5H-imidazo[2,1-b][1,3]oxazine
Smiles	O1c2n(C[C@@H](C1)OCc1ccc(cc1)OC(F)(F)F)cc(n2)[N](=O)O
Chemical Structure

Biological activities

PA-824 is an anti-tuberculosis agent. The MIC of PA-824 is ranging from 0.015 to 0.25 μg/mL against Mycobacterium tuberculosis. The MIC of PA-824 against M. tuberculosis H37Rv is 60 ng/mL. PA-824 inhibits synthesis of ketomycolates, an essential component of the mycobacterial cell wall.^[1] PA-824 acts directly as an NO donor. PA-824 treatment leads to an upregulation of the fasI gene as well as many genes in the fasII operon; along with efpA and iniBAC operon. PA-824 treatment also results in an upregulation of the cyd operon (cydA, cydB, cydD and cydC) encoding the non-proton-pumping cytochrome bd oxidase, the nitrate reductase narGHIJ and other genes involved in respiration.^[2] Single doses of PA-824 up to 1,456 mg/kg are well tolerated.^[1]

Protocols

CP-91149 is dissolved in either 0.25% (wt/vol) methyl cellulose in water or 0.1% Pluronic P105 Block Copolymer Surfactant in 0.1% saline.^[1]

References

[1] Ahmad Z, et al. PA-824 exhibits time-dependent activity in a murine model of tuberculosis. Antimicrob Agents Chemother. 2011, 55(1): 239-245. [2] Manjunatha U, et al. The mechanism of action of PA-824: Novel insights from transcriptional profiling. Commun Integr Biol. 2009, 2(3): 215-218.

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