MUT-056399

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种新型、高效的金黄色葡萄球菌和大肠杆菌 FabI 酶抑制剂。

A novel, highly potent inhibitor of the FabI enzyme of both Staphylococcus aureus and Escherichia coli; shows activity against S. aureus strains, including MSSA, MRSA, linezolid-resistant, and multidrug-resistant strains with MIC90s of 0.03-0.12 ug/ml; also has active against coagulase-negative staphylococci with MIC90s of 0.12-4 ug/ml; active in vivo (19.3-49.6 mg/kg/day).Bacterial Infection Preclinical.

MUT056399 (Fab-001) is a highly potent new inhibitor of the FabI enzyme of both Staphylococcus aureus and Escherichia coli. MUT056399 is very active against S. aureus strains, including methicillin-susceptible S. aureus (MSSA), methicillin-resistant S. aureus (MRSA), linezolid-resistant, and multidrug-resistant strains, with MIC90s between 0.03 and 0.12 μg/ml. MUT056399 is also active against coagulase-negative staphylococci, with MIC90s between 0.12 and 4 μg/ml.MUT056399 is very active against the 118 S. aureus strains tested, including MSSA and MRSA isolates and linezolid-resistant and multidrug-resistant strains, with MIC90s between ≤0.03 and 0.12 μg/ml.

MUT056399 (Fab-001), administered subcutaneously, protected mice from a lethal systemic infection induced by MSSA, MRSA, and vancomycin-intermediate S. aureus strains (50% effective doses ranging from 19.3 mg/kg/day to 49.6 mg/kg/day). In the nonneutropenic murine thigh infection model, the same treatment with MUT056399 reduced the bacterial multiplication of MSSA and MRSA in the thighs of immunocompetent mice.

FAB-001

GPCR/G Protein

Antibacterial

Antibacterial

Infection

Bacterial Infection

1269055-85-7

293.2654

C15H13F2NO3

>98% (HPLC)

DMSO: ≥ 31 mg/mL

CCC1=CC(=C(C=C1F)OC2=C(C=C(C=C2)C(=O)N)F)O

Benzamide, 4-(4-ethyl-5-fluoro-2-hydroxyphenoxy)-3-fluoro-

(-20℃)

With Ice Pack

≥ 2 years