Home Tools

Enmetazobactam

Catalog No. T14081 CAS 1001404-83-6

Synonyms: AAI101

Enmetazobactam (AAI101) is an extended-spectrum β-lactamase inhibitor for the treatment of multi-drug resistant gram-negative bacterial infections.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Enmetazobactam, CAS 1001404-83-6

Pack Size	Availability	Price/USD
2 mg	In stock	$ 46.00
5 mg	In stock	$ 74.00
10 mg	In stock	$ 124.00
50 mg	In stock	$ 374.00
100 mg	In stock	$ 537.00
1 mL * 10 mM (in DMSO)	In stock	$ 82.00

Bulk Inquiry

Select Batch

Purity: 99.78%

Purity: 98.34%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Enmetazobactam (AAI101) is an extended-spectrum β-lactamase inhibitor for the treatment of multi-drug resistant gram-negative bacterial infections.
In vitro	AAI101, a novel extended-spectrum β-lactamase inhibitor.?Of the 223 cefepime non-susceptible isolates, 95% were ceftazidime non-susceptible, 49% ertapenem non-susceptible, 57% piperacillin/tazobactam non-susceptible, 90% were multidrug-resistant (resistant to 3 drug classes), 22% produced carbapenemases, and 67% produced ESBLs.?Addition of AAI101 restored the activity of cefepime such that the MIC50 was reduced from >64 mg/L for cefepime to 0.13 mg/L for cefepime/AAI101, supporting its continued development treatment for infections caused by these organisms.AAI101 shows potent activity against specific resistance phenotypes with MIC50 and MIC90 of 0.125 mg/L and 64 mg/L[1].?Cefepime-AAI101 MICs decreases with increasing concentrations of AAI101 (over the range from 1 to 16 mg/L) for most strains.?which is demonstrating a concentration dependence of AAI101 on restoration of the antibacterial activity of the cephalosporin[1].
In vivo	Against a panel of 20 mostly carbapenemase-producing cefepime-nonsusceptible strains of the family Enterobacteriaceae, we evaluated the MICs of cefepime in the presence of various fixed AAI101 concentrations (1, 2, 4, 8, and 16 mg/liter) and the in vivo efficacy of simulated human doses of cefepime and cefepime-AAI101 in a neutropenic murine thigh infection model.?At 2 h after inoculation, mice were dosed with regimens that provided a profile mimicking the free drug concentration-time profile observed in humans given cefepime at 2 g every 8 h (q8h;?as a 30-min infusion) or cefepime-AAI101 at 2 g/0.5 g q8h (as a 30-min infusion).?Efficacy was determined by calculation of the change in thigh bacterial density (log10 number of CFU) after 24 h relative to the starting inoculum (0 h). After 24 h, bacterial growth of 2.7 0.1 log10 CFU (mean standard error) was observed in control animals.?Efficacy for cefepime monotherapy was observed against only 3 isolates, whereas increases in bacterial density similar to that in the control animals were noted for the remaining 17 strains (all with cefepime MICs of 64 mg/liter).?The humanized cefepime-AAI101 dosing regimen resulted in bacterial reductions of 0.5 log10 CFU for 12 of the 20 strains[2].

Synonyms	AAI101
Molecular Weight	314.32
Formula	C11H14N4O5S
CAS No.	1001404-83-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 113.3 mg/mL (360.46 mM)

References and Literature

1. Crandon JL, et al. In Vitro Activity of Cefepime/AAI101 and Comparators against Cefepime Non-susceptible Enterobacteriaceae. Pathogens. 2015 Aug 18;4(3):620-5. 2. Crandon JL, et al. In vivo activities of simulated human doses of cefepime and cefepime-AAI101 against multidrug-resistant Gram-negative Enterobacteriaceae. Antimicrob Agents Chemother. 2015 May;59(5):2688-94.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Inhibitor Library ReFRAME Related Library NO PAINS Compound Library Anti-Infection Compound Library Bioactive Compound Library Drug-induced Liver Injury (DILI) Compound Library Covalent Inhibitor Library Beta-Lactam Compound Library Antibiotics Library

Related Products

Related compounds with same targets

Propylparaben Clindamycin 4-Hydroxybenzoic acid Antimicrobial agent-14 WCK-4234 sodium Vinaxanthone Dalbavancin Azathramycin

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Enmetazobactam 1001404-83-6 Microbiology/Virology Antibacterial Bacterial inhibit AAI-101 AAI 101 AAI101 Inhibitor inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.