Avibactam sodium dihydrate (Synonyms: NXL-104 dihydrate)

Cat. No.: HY-14879C: Data Sheet Handling Instructions
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Avibactam sodium (NXL-104) dihydrate is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC₅₀s of 8 nM and 5 nM, respectively.

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Other In-stock Forms of Avibactam sodium dihydrate:

Avibactam free acid Avibactam sodium Avibactam sodium hydrate

Other Forms of Avibactam sodium dihydrate:

92 Publications Citing Use of MCE Avibactam sodium dihydrate

Bio/Physico-chemical Assay

RT-PCR

In Vivo Efficacy Study

Cell Proliferation/Viability Assay

: Avibactam sodium dihydrate purchased from MedChemExpress. Usage Cited in: Cell Rep. 2024 Nov 9;43(11):114962. [Abstract]; SREBP2 target gene transcript levels after treatment with Avibactam (0.69 μM, 24 h) analyzed by qPCR. Actin Beta (ACTB) was used as a reference gene.

: Avibactam sodium dihydrate purchased from MedChemExpress. Usage Cited in: Cell Rep. 2024 Nov 9;43(11):114962. [Abstract]; S-acylation levels of SCAP in Huh7 cells treated with Avibactam (0.69 μM, 24 h).

: Avibactam sodium dihydrate purchased from MedChemExpress. Usage Cited in: Cell Rep. 2024 Nov 9;43(11):114962. [Abstract]; Protein levels of SCAP and its downstream target proteins in Huh7 cells following treatment with Avibactam (0.69 μM, 24 h).

: Avibactam sodium dihydrate purchased from MedChemExpress. Usage Cited in: J Antimicrob Chemother. 2022 Sep 30;77(10):2803-2808. [Abstract]; In vivo change in log10 cfu/thigh of each isolate treated with saline control, Ceftazidime 2 g IV q8h 2 h infusion HSR, Ceftazidime/Avibactam 2.5 g q8h 2 h infusion HSR or meropenem 2 g q8h 3 h infusion HSR for three P. aeruginosa with inserted GES β-lactamases. (a) PSA 2136, with inserted GES-1 (ESBL). (b) PSA 2137, with inserted GES-5 (carbapenemase). (c) PSA 2138, with inserted GES-15. P values in the boxes represent the results from one-way ANOVA; P values are presented if between-group differences were present. The x-axis describes the treatment HSR [MIC (mg/L), % fT>MIC]. CAZ, Ceftazidime; CAZ-AVI, Ceftazidime/Avibactam; MEM, meropenem.

: Avibactam sodium dihydrate purchased from MedChemExpress. Usage Cited in: Biosens Bioelectron. 2021 Dec 1:193:113526. [Abstract]; Avibactam sodium (AVI: 6.3-50 mg/L) in the presence or absence of 200 mg/L ceftriaxone and/or 0.8 U/L CTX-M-14.

: Avibactam sodium dihydrate purchased from MedChemExpress. Usage Cited in: Biosens Bioelectron. 2021 Dec 1:193:113526. [Abstract]; Analysis of mixed mock samples containing 0.8 U/L each of NDM-1/CTX-M-14 were incubated with penicillin, ceftriaxone, cefepime, cefoxitin or meropenem (200 mg/L) in the presence and absence of 25 mg/L Avibactam sodium (AVI) for 15 min, then the NDM-1/CTX-M-14 treated and untreated antibiotic samples were analyzed.

: Avibactam sodium dihydrate purchased from MedChemExpress. Usage Cited in: J Antimicrob Chemother. 2017 Jul 1;72(7):1930-1936. [Abstract]; Total β-lactamase activity for bacterial lysates is measured using the chromogenic substrate nitrocefin, with or without Avibactam at 4 mg/L. (b) GR20263 hydrolysis activity of different bacterial lysates is determined with or without Avibactam at 4 mg/L.

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Biological Activity
Purity & Documentation
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Customer Review

Description

IC₅₀ & Target

IC₅₀: 5 nM (CTX-M-15), 8 nM (TEM-1)^[1]

In Vitro

Avibactam is a molecule with little antibacterial activity, that inhibits class A and C β-lactamases, but not metallo types and Acinetobacter OXA carbapenemases^[2].
Ceftazidime (HY-B0593)-Avibactam (0-256 mg/L) inhibits 16 bla_KPC-2 positive and 1 of bla_OXA-232 positive Klebsiella pneumonia growth with MIC₅₀ and MIC₉₀ for both 8 mg/L^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Ceftazidime-Avibactam (0.375 mg/g; s.c.; q8h for 10 days) has a significant effect on the bacteria and led to a certain therapeutic efficacy in K. pneumoniae strain Y8 infected mouse model^[3].
Avibactam (64 mg/kg; s.c.; once) shows mean estimated half-life in plasma in the terminal phase of 0.24 h in Pseudomonas aeruginosa infected neutropenic mice with lung infection^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Six-week-old BALB/c mice (female), K. pneumoniae strain Y8 infection model^[4]
Dosage:	0.375 mg/g in combination with Ceftazidime
Administration:	Subcutaneous injection, 4 h post infection and given every 8 h for 10 days
Result:	70% of infection group mice died within 4 days, and all mice in the PBS group died within 13 days. All treatment group mice survived at 10 days post infection with the antibiotic applied every 8 h, whereas 100% of mice in this group died within 4 days after the antibiotic treatment stopped. The spleen and liver of treatment group mice showed lower CFU counts, as compare with that of infected group.

Molecular Weight

323.26

Formula

C₇H₁₄N₃NaO₈S

SMILES

O=S(ON1[C@]2([H])CC[C@@H](C(N)=O)[N@@](C2)C1=O)(O[Na])=O.O.O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Ehmann DE, Jahic H, Ross PL, Gu RF, Hu J, Kern G, Walkup GK, Fisher SL. Avibactam is a covalent, reversible, non-β-lactam β-lactamase inhibitor. Proc Natl Acad Sci U S A. 2012 Jul 17;109(29):11663-8. [Content Brief]

[2]. Castanheira M, Sader HS, Farrell DJ, Mendes RE, Jones RN. Activity of Ceftaroline-Avibactam Tested against Gram-Negative Organism Populations, including Strains Expressing One or More β-Lactamases and Methicillin-Resistant Staphylococcus aureus Carrying Various Staphylococcal Cassette Chromosome mec Types. Antimicrob Agents Chemother. 2012 Sep;56(9):4779-85. [Content Brief]

[3]. Livermore DM, Mushtaq S, Barker K, Hope R, Warner M, Woodford N. Characterization of β-lactamase and porin mutants of Enterobacteriaceae selected with ceftaroline + avibactam (NXL104). J Antimicrob Chemother. 2012 Jun;67(6):1354-8. [Content Brief]

[4]. Zhang W, et al. In vitro and in vivo bactericidal activity of ceftazidime-avibactam against Carbapenemase-producing Klebsiella pneumoniae. Antimicrob Resist Infect Control. 2018 Nov 21;7:142. [Content Brief]

Avibactam sodium dihydrate Related Classifications

Infection

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Avibactam sodium dihydrateNXL-104 dihydrateBeta-lactamaseBacterialAntibioticβ-lactamaseTEM-1CTX-M-15antibacterialKlebsiella pneumoniaPseudomonas aeruginosaInhibitorinhibitorinhibit

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