| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
- Class A and C β-lactamases (e.g., KPC-2, CTX-M-15, TEM-1) [1,3]
|
|---|---|
| ln Vitro |
- Synergistic Activity with Imipenem: Relebactam restored imipenem activity against carbapenem-resistant Klebsiella pneumoniae and Escherichia coli isolates. For KPC-2-producing K. pneumoniae, imipenem MIC90 decreased from >32 mg/L to 1 mg/L in the presence of 4 mg/L relebactam. For CTX-M-15-expressing E. coli, imipenem MIC90 dropped from 8 mg/L to 0.5 mg/L [1]
- β-Lactamase Inhibition Profile: Relebactam potently inhibits KPC-2 (IC50 = 38 nM) and CTX-M-15 (IC50 = 5 nM), but shows no activity against metallo-β-lactamases (e.g., NDM-1) [3] |
| Enzyme Assay |
- β-Lactamase Inhibition Assay:
1. Purified KPC-2 (0.1 μM) was incubated with 0.1–10 μM relebactam in Tris buffer (pH 7.5) for 10 minutes at 37°C.
2. Residual enzyme activity was measured using imipenem (100 μM) as a substrate via spectrophotometry (λ=301 nm).
3. IC50 = 38 nM was determined by plotting percent inhibition against inhibitor concentration [3]
|
| Cell Assay |
- Bacterial Growth Inhibition:
1. K. pneumoniae (10⁶ CFU/mL) were exposed to imipenem (0.5–256 mg/L) ± relebactam (0.5–16 mg/L) in Mueller-Hinton broth.
2. MIC endpoints were read after 24-hour incubation at 37°C.
3. Relebactam reduced imipenem MIC90 for KPC-2 strains from >32 mg/L to 1 mg/L [1]
|
| ADME/Pharmacokinetics |
In humans, Relebactam exhibits linear pharmacokinetics with a steady-state volume of distribution of 18.2 L. Plasma protein binding is ~22%, and 90% of the administered dose is excreted unchanged in urine. The elimination half-life is 1.2 hours.
When administered as imipenem/cilastatin/Relebactam (500 mg/500 mg/250 mg), Relebactam achieves a peak plasma concentration (Cₘₐₓ) of 24.3 μg/mL after a 30-minute infusion, with an AUC of 50.2 μg·h/mL. |
| Toxicity/Toxicokinetics |
Common adverse reactions include diarrhea (6.9%), nausea (4.3%), headache (3.2%), and elevated liver enzymes (ALT/AST >5× upper limit of normal in 2.1% of patients).
Relebactam may reduce serum concentrations of valproic acid, increasing seizure risk; concomitant use is contraindicated |
| References |
|
| Additional Infomation |
- Mechanism of Action: Relebactam covalently binds to the active site of class A/C β-lactamases, forming a reversible acyl-enzyme intermediate. This blocks substrate access and restores β-lactam antibiotic activity [3]
- Clinical Relevance: Approved in combination with imipenem/cilastatin for treating multidrug-resistant Gram-negative infections, including complicated urinary tract and intra-abdominal infections. [3] Mechanism: Relebactam lacks intrinsic antibacterial activity but restores imipenem efficacy by inhibiting Class A/C β-lactamases (e.g., KPC, AmpC), reversing resistance in Enterobacterales and P. aeruginosa. Indications: Approved for complicated urinary tract infections (cUTI) and complicated intra-abdominal infections (cIAI) caused by susceptible Gram-negative bacteria. Resistance: 40% of carbapenem-resistant Gram-negative pathogens show resistance to imipenem-Relebactam, necessitating combination therapies (e.g., with fosfomycin). |
| Molecular Formula |
C12H19N4NAO6S
|
|---|---|
| Molecular Weight |
370.35723233223
|
| Elemental Analysis |
C, 38.92; H, 5.17; N, 15.13; Na, 6.21; O, 25.92; S, 8.66
|
| CAS # |
1502858-91-4
|
| Related CAS # |
1174018-99-5
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
S(=O)(=O)([O-])ON1C(N2C[C@H]1CC[C@H]2C(NC1CCNCC1)=O)=O.[Na+]
|
| Synonyms |
MK-7655 sodium; Relebactam sodium; Sodium relebactam; 1502858-91-4; UNII-EX0546AJ8R; EX0546AJ8R; MK 7655; sodium;[(2S,5R)-7-oxo-2-(piperidin-4-ylcarbamoyl)-1,6-diazabicyclo[3.2.1]octan-6-yl] sulfate; MK-SODIUM SALT
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7001 mL | 13.5004 mL | 27.0008 mL | |
| 5 mM | 0.5400 mL | 2.7001 mL | 5.4002 mL | |
| 10 mM | 0.2700 mL | 1.3500 mL | 2.7001 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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