G0775 | Bacterial SPase LepB inhibitor | Probechem Biochemicals

Chemical Structure : G0775

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G0775 (G-0775)

货号: PC-22138Not For Human Use, Lab Use Only.

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生物&药学活性

G0775 is a novel potent, broad-spectrum antibiotic against Gram-negative bacteria (MDR K. pneumoniae CDC 0106, MIC=0.5 ug/mL), inhibits the Gram-negative type I signal peptidase (SPase) LepB with Ki of 0.44 nM, a new antibiotic target.
G0775 is at least 500-fold more potent than arylomycin A-C16 against the ESKAPE pathogens E. coli and K. pneumoniae as well as against related pathogens from the same family.
G0775 is active against a panel of 49 MDR clinical isolates of E. coli and K. pneumonia.
G0775 binds the LepB protease domain to form an irreversible covalent bond with catalytic lysine 146.
G0775 is bacteriostatic at 2 mg/kg and bactericidal at 20 mg/kg, protects mice from a lethal challenge of K. pneumoniae Zstrain ATCC 43816 in a mucin peritonitis model.

物理化学性质&存储条件

分子量	890.06
分子式	C47H59N11O7
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(8S,11S,14S)-14-[[(2S)-4-amino-2-[[2-(4-tert-butylphenyl)-4-methylpyrimidine-5-carbonyl]amino]butanoyl]-methylamino]-3,18-bis(2-aminoethoxy)-N-(cyanomethyl)-11-methyl-10,13-dioxo-9,12-diazatricyclo[13.3.1.12,6]icosa-1(18),2,4,6(20),15(19),16-hexaene-8-carboxamide

参考文献

1. Peter A Smith, et al. Nature. 2018 Sep;561(7722):189-194.

G0775 (G-0775)

生物&药学活性

物理化学性质&存储条件

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G0775 (G-0775)

生物&药学活性

物理化学性质&存储条件

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