ACHN-975-TFA-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEACHN-975 TFACat. No.: HY-19936ACAS No.: 1410809-37-8分式: CHFNO分量: 483.44作靶点: Bacterial作通路: Anti-infection储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 monthBIOLOGICAL ACTIVITY物活性 ACHN-975细酶 LpxC 的选择性抑制剂，表现出亚纳尔级

2、 LpxC 抑制活性。ACHN-975 对多种兰性 MIC 值低于 1 g/mL。IC50 & Target IC50: LpxC 1体外研究 ACHN-975 is against Enterobacteriaceae spp with an IC50 of 0.02 nM 1.ACHN-975 is againstEnterobacteriaceae spp, Pa, and Ab with MIC90 values of 1, 0.5, and 64 g/mL, respectively 1.ACHN-975is potently against the P. aeruginosa is

3、olates tested, inhibiting 100% of the isolates at an MIC of 2g/ml. Itagainst Pseudomonas aeruginosa with an MIC50 and MIC90 of 0.06 and 0.25g/ml, respectively 2.ACHN-975 is against six P. aeruginosa isolates, it against P. aeruginosa APAE1064, APAE1232, andAPAE1064 isolates with MIC values of 0.12,

4、0.06 and 0.06 g/ml, respectively 2.LpxC is highly conservedin gram-negative bacteria and catalyzes the first committed step of lipid A biosynthesis. LpxC is the bacterialenzyme Zinc-dependent metalloamidase UDP-3-O-(R)-3-hydroxymyristoyl-N-acetylglucosaminedeacetylase 1.体内研究ACHN-975 TFA (intraperito

5、neal administration; 5-30mg/kg; single dose) leads to a steady reduction inbacterial titers in the first 4h following treatment for all dosing groups. The sampling shows that the level offree drug in this model drops below the ACHN-975 MIC for this isolate (0.25g/ml) by 2h after treatment withthe 10

6、 mg/kg dose and by 4h after treatment with the 30 mg/kg dose 2.1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEAnimal Model: Neutropenic mouse thigh model with P. aeruginosa ATCC 27853 2Dosage: 5-30 mg/kgAdministration: Intraperitoneal administration; single doseResult: Had a bactericidal activity

7、and was against the P. aeruginosa ATCC27853 strain in vivo.REFERENCES1. Kalinin DV, et al. Insights into the Zinc-Dependent Deacetylase LpxC: Biochemical Properties and Inhibitor Design. Curr Top Med Chem.2016;16(21):2379-430.2. Krause KM,et al. Potent LpxC Inhibitors with In Vitro Activity against Multidrug-Resistant Pseudomonas aeruginosa.Antimicrob AgentsChemother. 2019 Oct 22;63(11). pii: e00977-19.McePdfHeightCaution: Product has not been fully validated for medical applications.For resea