[CAS NO. 1192500-31-4] Avibactam free acid

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PRODUCTS SPECIFICATIONS [1192500-31-4]

Catalog

HY-14879

Brand

MCE

CAS

1192500-31-4

DESCRIPTION [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

For research use only. We do not sell to patients.

56 Publications Citing Use of MCE

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

In Vitro:

DMSO : 125 mg/mL ( 471.27 mM ; Need ultrasonic)

Preparing
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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% Saline

Solubility: ≥ 2.08 mg/mL (7.84 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (7.84 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (7.84 mM); Clear solution

* All of the co-solvents are available by MedChemExpress (MCE).