CHIR-090

Research use only, not for human use.

CHIR-090 is a very potent and selective LpxC inhibitor with antibiotic activity.

CHIR-090 is a very potent and selective LpxC inhibitor. CHIR-090 has excellent antibiotic activity against Pseudomonas aeruginosa and Escherichia coli. CHIR-090 is also a two-step slow, tight-binding inhibitor of E. coli LpxC with Ki = 4.0 nM, Ki* = 0.5 nM, k5 = 1.9 min-1, and k6 = 0.18 min-1. CHIR-090 at low nanomolar levels inhibits LpxC orthologues from diverse Gram-negative pathogens, including P. aeruginosa, Neisseria meningitidis, and Helicobacter pylori. In contrast, CHIR-090 is a relatively weak competitive and conventional inhibitor (lacking slow, tight-binding kinetics) of LpxC from Rhizobium leguminosarum (Ki = 340 nM), a Gram-negative plant endosymbiont that is resistant to this compound. CHIR-090 is an excellent lead for the further development of new antibiotics targeting the lipid A pathway.

CHIR-090; CHIR 090; CHIR090

Others

Other Targets

Escherichia coli LpxC

Infection

——

728865-23-4

437.19

C24H27N3O5

97%

DMSO : ≥ 30 mg/mL; 68.57 mM

ONC(=O)[C@@H](NC(=O)c1ccc(cc1)C#Cc1ccc(cc1)CN1CCOCC1)[C@@H](C)O

N-[(2S,3R)-3-hydroxy-1-(hydroxyamino)-1-oxobutan-2-yl]-4-[2-[4-(morpholin-4-ylmethyl)phenyl]ethynyl]benzamide

(-20℃)

With Ice Pack

≥ 2 years