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CHIR-090

Cat. No. M9772
CHIR-090 Structure
Synonym:

CHIR090

Size Price Availability
5mg USD 197 4-7 Days
10mg USD 315 4-7 Days
50mg USD 852 4-7 Days
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Quality Control
  • Current batch:
  • Purity >98.5%
  • COA
  • MSDS
Biological Activity

CHIR-090 is a very potent and selective LpxC inhibitor, it is also a two-step slow, tight-binding inhibitor of E. coli LpxC with Ki = 4.0 nM. 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. A strain of E. coli W3110 is able to grow on LB agar plates containing 1 to 10 μg/mL CHIR-090, which is 4 to 40 times above the MIC of 0.25 μg/mL under our conditions for wild-type E. coli W3110. The doubling time of W3110RL is 40 min in the presence of 1 μg/mL CHIR-090, which is exactly the same rate as wild-type in the absence of inhibitor.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 437.49
Formula C24H27N3O5
CAS Number 728865-23-4
Purity >98.5%
Solubility DMSO 10 mM
Storage at -20°C
References

In Vitro and In Vivo Efficacy of an LpxC Inhibitor, CHIR-090, Alone or Combined with Colistin against Pseudomonas aeruginosa Biofilm
Jun Hou Tan, et al. Antimicrob Agents Chemother. 2017 Jun 27;61(7):e02223-16. PMID: 28461320.

Mechanisms decreasing in vitro susceptibility to the LpxC inhibitor CHIR-090 in the gram-negative pathogen Pseudomonas aeruginosa
Ruth E Caughlan, et al. Antimicrob Agents Chemother. 2012 Jan;56(1):17-27. PMID: 22024823.

Structure of the deacetylase LpxC bound to the antibiotic CHIR-090: Time-dependent inhibition and specificity in ligand binding
Adam W Barb, et al. Proc Natl Acad Sci U S A. 2007 Nov 20;104(47):18433-8. PMID: 18025458.

Inhibition of lipid A biosynthesis as the primary mechanism of CHIR-090 antibiotic activity in Escherichia coli
Adam W Barb, et al. Biochemistry. 2007 Mar 27;46(12):3793-802. PMID: 17335290.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CHIR-090, CHIR090 supplier, Anti-infection, inhibitors

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