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Durlobactam sodium salt

Name: Durlobactam sodium salt
Brand: TargetMol
SKU: T11125
Price: 616 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T11125Cas No. 1467157-21-6

Alias ETX2514 sodium salt

Durlobactam sodium salt (ETX2514) is a beta-lactamase inhibitor with IC50 values of 4 nM, 14 nM and 190 nM against class A KPC-2, class C AmpC and class D OXA-24.

Durlobactam sodium salt

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Purity: 99.03%

Catalog No. T11125Alias ETX2514 sodium saltCas No. 1467157-21-6

Durlobactam sodium salt (ETX2514) is a beta-lactamase inhibitor with IC50 values of 4 nM, 14 nM and 190 nM against class A KPC-2, class C AmpC and class D OXA-24.

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
2 mg	$616	In Stock	In Stock
5 mg	$993	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.03%

Appearance:Solid

Color:White to Yellow

Resource Download

COA HNMR HPLC

Product Introduction

Bioactivity

Description	Durlobactam sodium salt (ETX2514) is a beta-lactamase inhibitor with IC50 values of 4 nM, 14 nM and 190 nM against class A KPC-2, class C AmpC and class D OXA-24.
Targets&IC50	AmpC (Class C):14 nM, KPC2 (Class A):4 nM, OXA24 (Class D):190 nM
In vitro	Method: After pre-incubation of Durlobactam sodium salt (ETX2514) with enzyme for 5 minutes, the IC50 value of Durlobactam for representative class A, C and D β-lactamases was measured. RESULTS The IC50 values of Durlobactam against Class A KPC-2, Class C AmpC, and Class D OXA-24 are 0.004μM, 0.014μM and 0.19μM respectively. [1] METHODS: Antimicrobial susceptibility testing of BCC and B. gladioli clinical isolates was performed with Durlobactam (2-64 μg/ml). RESULTS Durlobactam showed moderate activity (MIC90= 16 μg/ml). [2]
In vivo	METHODS: Subjects were randomly assigned to 1 of 6 sequences, including a single 3-hour intravenous infusion of Durlobactam sodium salt (ETX2514) 4 g, a single 3-hour intravenous infusion of placebo, and a single 3-hour intravenous infusion of placebo plus a single dose. The second oral dose of moxifloxacin 400 mg was given open label at the end of the intravenous infusion. During each treatment period, ambulatory electrocardiogram (ECG) measurements were obtained from before dosing to 24 hours after the start of infusion. RESULTS Durlobactam had no significant effect on electrocardiographic parameters, including QT interval prolongation. Durlobactam carries a low risk of prolonging the QT interval and is unlikely to produce any proarrhythmic effects. [3]
Synonyms	ETX2514 sodium salt

Chemical Properties

Molecular Weight	299.23
Formula	C₈H₁₀N₃NaO₆S
Cas No.	1467157-21-6
Smiles	CC1=C[C@@H]2CN(C(N2OS(=O)([O-])=O)=O)[C@@H]1C(N)=O.[Na+]
Relative Density.	1.31g/cm3

Storage & Solubility Information

Storage

store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 50 mg/mL (167.1 mM), Sonication is recommended.

H2O: 2.5 mg/mL (8.35 mM), Sonication is recommended.

Solution Preparation Table

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	3.3419 mL	16.7096 mL	33.4191 mL	167.0955 mL
5 mM	0.6684 mL	3.3419 mL	6.6838 mL	33.4191 mL

DMSO

	1mg	5mg	10mg	50mg
10 mM	0.3342 mL	1.6710 mL	3.3419 mL	16.7096 mL
20 mM	0.1671 mL	0.8355 mL	1.6710 mL	8.3548 mL
50 mM	0.0668 mL	0.3342 mL	0.6684 mL	3.3419 mL
100 mM	0.0334 mL	0.1671 mL	0.3342 mL	1.6710 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

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

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