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Durlobactam sodium salt

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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

Durlobactam sodium salt

🥰Excellent
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 SizePriceAvailabilityQuantity
1 mg$168In Stock
5 mg$419In Stock
10 mg$679In Stock
25 mg$1,360In Stock
50 mg$2,190In Stock
100 mg$3,550In Stock
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Purity:99.03%
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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 , OXA24 (Class D):190 nM , KPC2 (Class A):4 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]
AliasETX2514 sodium salt
Chemical Properties
Molecular Weight299.23
FormulaC8H10N3NaO6S
Cas No.1467157-21-6
SmilesCC1=C[C@@H]2CN(C(N2OS(=O)([O-])=O)=O)[C@@H]1C(N)=O.[Na+]
Relative Density.1.31g/cm3
Storage & Solubility Information
Storagestore at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 50 mg/mL (167.1 mM)
H2O: 2.5 mg/mL (8.35 mM), Sonication is recommended.
Solution Preparation Table
H2O/DMSO
1mg5mg10mg50mg
1 mM3.3419 mL16.7096 mL33.4191 mL167.0955 mL
5 mM0.6684 mL3.3419 mL6.6838 mL33.4191 mL
DMSO
1mg5mg10mg50mg
10 mM0.3342 mL1.6710 mL3.3419 mL16.7096 mL
20 mM0.1671 mL0.8355 mL1.6710 mL8.3548 mL
50 mM0.0668 mL0.3342 mL0.6684 mL3.3419 mL
100 mM0.0334 mL0.1671 mL0.3342 mL1.6710 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 mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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