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[CAS NO. 1192500-31-4] Avibactam free acid
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-14879 |
| Brand: | MCE |
| CAS: | 1192500-31-4 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 265.24 |
| Molecular Formula | C7H11N3O6S |
| SMILES | O=S(ON1[C@]2([H])CC[C@@H](C(N)=O)[N@@](C2)C1=O)(O)=O |
56 Publications Citing Use of MCE
- [1]Biosens Bioelectron. 2021 Jul 21;193:113526.
- [2]Int J Antimicrob Agents. 2018 Aug;52(2):269-271.
- [3]J Clin Microbiol. 2023 Apr 18;e0164722.
- [4]J Clin Microbiol. 2020 Aug 24;58(9):e00932-20.
- [5]Int J Infect Dis. 2021 Apr 14;S1201-9712(21)00346-5.
- [6]Int J Infect Dis. 2020 Apr;93:252-257.
- [7]J Infect Dis. 2019 Jul 2;220(3):484-493.
- [8]Int J Mol Sci. 2021, 22(6), 3051.
- [9]ACS Infect Dis. 2021 Jun 30.
- [10]J Antimicrob Chemother. 2023 Feb 13;dkad032.
- [11]J Antimicrob Chemother. 2022 Jul 15;dkac232.
- [12]J Antimicrob Chemother. 2021 May 6;dkab141.
- [13]J Antimicrob Chemother. 2021 Feb 11;76(3):653-658.
- [14]J Antimicrob Chemother. 2020 Sep 1;75(9):2609-2615.
- [15]J Antimicrob Chemother. 2017 Jul 1;72(7):1930-1936.
- [16]J Antimicrob Chemother. 2017 Sep 1;72(9):2483-2488.
- [17]Antimicrob Agents Chemother. 2023 Sep 8;e0030123.
- [18]Antimicrob Agents Chemother. 2023 Sep 6;e0052823.
- [19]Antimicrob Agents Chemother. 2023 May 31;e0033923.
- [20]Antimicrob Agents Chemother. 2023 May 18;e0160322.
- [21]Antimicrob Agents Chemother. 2023 Jan 23;e0145922.
- [22]Antimicrob Agents Chemother. 2022 Jun 1;e0240221.
- [23]Antimicrob Agents Chemother. 2020 Sep 21;64(10):e00409-20.
- [24]Antimicrob Agents Chemother. 2020 Feb 21;64(3):e02025-19.
- [25]Antimicrob Agents Chemother. 2019 Sep 16;63(12):e01515-19.
- [26]Antimicrob Agents Chemother. 2019 Aug 23;63(9):e01374-19.
- [27]Antimicrob Agents Chemother. 2018 Dec 21;63(1). pii: e01809-18.
- [28]Antimicrob Agents Chemother. 2018 Sep 24;62(10). pii: e00873-18.
- [29]Antimicrob Agents Chemother. 2018 Jul 27;62(8). pii: e00433-18.
- [30]Antimicrob Agents Chemother. 2018 Jul 27;62(8). pii: e00414-18.
- [31]Antimicrob Agents Chemother. 2018 May 25;62(6). pii: e00282-18.
- [32]Antimicrob Agents Chemother. 2017 Mar 24;61(4). pii: e02260-16.
- [33]Antibiotics (Basel). 2023 Jul 20, 12(7), 1212.
- [34]Antibiotics (Basel). 2022, 11(10), 1280.
- [35]Antibiotics (Basel). 2021, 10(11), 1341.
- [36]Antibiotics (Basel). 2021 Sep 14;10(9):1110.
- [37]Adv Ther (Weinh). 2024 Jan 12.
- [38]Sci Rep. 2022 Oct 7;12(1):16814.
- [39]BMC Microbiol. 2020 Jun 29;20(1):187.
- [40]BMC Microbiol. 2019 Nov 1;19(1):240.
- [41]Int J Med Microbiol. 2021 Oct;70(10).
- [42]Int J Med Microbiol. 2020 Jul;69(7):928-931.
- [43]RSC Adv. 2023 Nov 30;13(49):34884-34890.
- [44]Infect Drug Resist. 2021 Jun 30;14:2499-2507.
- [45]Infect Drug Resist. 2020 Aug 18;13:2883-2890.
- [46]Microbiol Spectr. 2023 Nov 20:e0304723.
- [47]Microbiol Spectr. 2023 Apr 24;e0069223.
- [48]Microbiol Spectr. 2022 Dec 8;e0303822.
- [49]Microbiol Spectr. 2022 Aug 16;e0139022.
- [50]Microbiol Spectr. 2022 Aug 24;e0203522.
- [51]Microb Drug Resist. 2020 Apr;26(4):334-340.
- [52]J Infect Dev Ctries. 2021 Mar 31;15(3):404-414.
- [53]Acta Microbiol Immunol Hung. 2021 Jul 29.
- [54]Preprints. 2023 Jun 21.
- [55]bioRxiv. 2021 Mar 13.
- [56]Biomed Res Int. 2018 Jul 2;2018:3579832.
Summary
Avibactam (NXL-104) free acid is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC 50 s of 8 nM and 5 nM, respectively [1] .
IC50 & Target
IC 50 : 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 MIC
50
and MIC
90
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. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT05340530 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. |
Infections
|
April 2022 | Phase 1 |
| NCT05487586 | Pfizer |
Hospital Acquired Pneumonia|Ventilator Acquired Pneumonia|Complicated Intra Abdominal Infections
|
October 18, 2022 | |
| NCT01689207 | Pfizer |
Complicated Infection|Bacterial Infections
|
September 2012 | Phase 1 |
| NCT02475733 | Pfizer |
Complicated Intra-abdominal Infections
|
August 1, 2015 | Phase 2 |
| NCT04402359 | King Abdul Aziz Specialist Hospital |
Ventilator Associated Pneumonia
|
July 5, 2018 | |
| NCT02497781 | Pfizer|PRA Health Sciences |
Complicated Urinary Tract Infections
|
September 24, 2015 | Phase 2 |
| NCT01281462 | Forest Laboratories |
Urinary Tract Infections
|
December 2010 | Phase 2 |
| NCT01599806 | Pfizer|Forest Laboratories |
Complicated Urinary Tract Infection (cUTI) Including Acute Pyelonephritis
|
October 2012 | Phase 3 |
| NCT01290900 | Pfizer |
Healthy Male Volunteers
|
February 2011 | Phase 1 |
| NCT01595438 | Pfizer|Forest Laboratories |
Complicated Urinary Tract Infection (cUTI) Including Acute Pyelonephritis
|
October 2012 | Phase 3 |
| NCT01291602 | Pfizer |
Healthy Male and Female Japanese Volunteers
|
February 2011 | Phase 1 |
| NCT01644643 | Pfizer|Forest Laboratories |
Complicated Urinary Tract Infection|Complicated Intra-abdominal Infection
|
January 2013 | Phase 3 |
| NCT01430910 | Pfizer |
Healthy
|
September 2011 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 125 mg/mL ( 471.27 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.7702 mL | 18.8509 mL | 37.7017 mL |
| 5 mM | 0.7540 mL | 3.7702 mL | 7.5403 mL |
| 10 mM | 0.3770 mL | 1.8851 mL | 3.7702 mL |
-
1.
-
2.
-
3.
References
- [1] Ehmann DE, et al. 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.
- [2] Livermore DM, et al. Characterization of β-lactamase and porin mutants of Enterobacteriaceae selected with ceftaroline + avibactam (NXL104). J Antimicrob Chemother. 2012 Jun;67(6):1354-8.
- [3] Berkhout J, et al. Pharmacokinetics and penetration of ceftazidime and avibactam into epithelial lining fluid in thigh- and lung-infected mice. Antimicrob Agents Chemother. 2015 Apr;59(4):2299-304.
- [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.
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