Relebactam |
| Catalog No.GC19308 |
Relebactam is a β-lactamase (AmpC) inhibitor that can irreversibly inhibit Class A (extended-spectrum β-lactamase and KPC enzymes) and Class C AmpC.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1174018-99-5
Sample solution is provided at 25 µL, 10mM.
Relebactam is a β-lactamase (AmpC) inhibitor that can irreversibly inhibit Class A (extended-spectrum β-lactamase and KPC enzymes) and Class C AmpC[1]. Relebactam is a diazabicyclooctane derivative that covalently binds to the active site serine residue of β-lactamase, irreversibly inhibiting its ability to hydrolyze β-lactam antibiotics, thereby restoring the bactericidal activity of imipenem against enzyme-producing resistant bacteria[2]. The combination of Relebactam and Imipenem can significantly reduce the minimum inhibitory concentration (MIC) and improve the efficacy against resistant bacteria (such as Pseudomonas aeruginosa and Klebsiella pneumoniae)[3, 4]. Relebactam can reduce the MIC of multiple cephalosporins and carbapenems against Mycobacterium abscessus[5].
References:
[1] Alfei S, Schito A M. β-lactam antibiotics and β-lactamase enzymes inhibitors, part 2: our limited resources[J]. Pharmaceuticals, 2022, 15(4): 476.
[2] Tooke C L, Hinchliffe P, Lang P A, et al. Molecular basis of class A β-lactamase inhibition by relebactam[J]. Antimicrobial agents and chemotherapy, 2019, 63(10): 10.1128/aac. 00564-19.
[3] McCarthy M W. Clinical Pharmacokinetics and Pharmacodynamics of Imipenem–Cilastatin/Relebactam Combination Therapy[J]. Clinical Pharmacokinetics, 2020, 59(5): 567-573.
[4] Young K, Painter R E, Raghoobar S L, et al. In vitro studies evaluating the activity of imipenem in combination with relebactam against Pseudomonas aeruginosa[J]. BMC microbiology, 2019, 19: 1-14.
[5] Kaushik A, Ammerman N C, Parrish N M, et al. New β-lactamase inhibitors nacubactam and zidebactam improve the in vitro activity of β-lactam antibiotics against Mycobacterium abscessus complex clinical isolates[J]. Antimicrobial agents and chemotherapy, 2019, 63(9): 10.1128/aac. 00733-19.
| Cas No. | 1174018-99-5 | SDF | |
| Canonical SMILES | O=S(ON1[C@]2([H])CC[C@@H](C(NC3CCNCC3)=O)[N@@](C2)C1=O)(O)=O | ||
| Formula | C12H20N4O6S | M.Wt | 348.38 |
| Solubility | Water : 72 mg/mL (206.67 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.8704 mL | 14.3521 mL | 28.7043 mL |
| 5 mM | 0.5741 mL | 2.8704 mL | 5.7409 mL |
| 10 mM | 0.287 mL | 1.4352 mL | 2.8704 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 5 reference(s) in Google Scholar.)
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