1. Anti-infection
  2. Bacterial
  3. AAI101

AAI101 

Cat. No.: HY-103095 Purity: >98.0%
Handling Instructions

AAI101 is an extended-spectrum β-lactamase inhibitor, against many resistant Gram-negative pathogens.

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

AAI101 Chemical Structure

AAI101 Chemical Structure

CAS No. : 1001404-83-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 145 In-stock
Estimated Time of Arrival: December 31
5 mg USD 132 In-stock
Estimated Time of Arrival: December 31
10 mg USD 192 In-stock
Estimated Time of Arrival: December 31
25 mg USD 348 In-stock
Estimated Time of Arrival: December 31
50 mg USD 588 In-stock
Estimated Time of Arrival: December 31
100 mg USD 828 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

AAI101 is an extended-spectrum β-lactamase inhibitor, against many resistant Gram-negative pathogens.

In Vitro

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, demonstrating a concentration dependence of AAI101 on restoration of the antibacterial activity of the cephalosporin[1].

In Vivo

In neutropenic animals, cefepime-AAI101 treatment results in reductions in bacterial density of ≥0.5 log10 CFU for 12 of the 20 strains tested and reductions of ≥1 log10 CFU for 6 of these. Increases in bacterial density are for only four strains, three of which have cefepime-AAI101 MICs of ≥64 mg/L, irrespective of the AAI101 concentration[2].

Clinical Trial
Storage

-20°C, protect from light, stored under nitrogen

Solvent & Solubility
In Vitro: 

DMSO : ≥ 113.3 mg/mL (360.46 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1815 mL 15.9074 mL 31.8147 mL
5 mM 0.6363 mL 3.1815 mL 6.3629 mL
10 mM 0.3181 mL 1.5907 mL 3.1815 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (6.62 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (6.62 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (6.62 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[2]

The 20 Enterobacteriaceae strains are used to infect groups of three mice each. At 2 h after inoculation, mice are treated with humanized regimens of cefepime or cefepime-AAI101. All doses are administered as 0.2-mL subcutaneous injections. To serve as control animals, an additional group of mice is administered normal saline at the same volume and frequency and by the same route. Thighs from all animals are harvested at 24 h after initiation of therapy. The harvesting procedure for all study mice began with euthanasia by CO2 exposure, followed by cervical dislocation. After sacrifice, thighs are removed and homogenized individually in normal saline. For determinations of the numbers of CFU, serial dilutions of thigh homogenates are spread onto Trypticase soy agar with 5% sheep blood using a spiral plater. In addition to the aforementioned treatment and control groups, another group of three infected but untreated mice is harvested at the initiation of dosing and served as a 0-h control. Efficacy, expressed as the change in bacterial density, is determined by calculation of the change in the log10 number of CFU obtained in mice after 24 h of treatment from the densities observed in the 0-h control animals.

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

References
Molecular Weight

314.32

Formula

C₁₁H₁₄N₄O₅S

CAS No.

1001404-83-6

SMILES

C[N+]1=NN(C[[email protected]@](S([[email protected]]2([H])C3)(=O)=O)(C)[[email protected]](C([O-])=O)N2C3=O)C=C1

Shipping

Room temperature in continental US; may vary elsewhere

Purity: >98.0%

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Product Name:
AAI101
Cat. No.:
HY-103095
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AAI101

Cat. No.: HY-103095