1. Anti-infection
  2. Bacterial

Relebactam (Synonyms: MK-7655)

Cat. No.: HY-16752 Purity: 98.94%
Data Sheet SDS Handling Instructions

Relebactam is a diazabicyclooctane inhibitor with activity against a wide spectrum of β-lactamases, including class A (extended-spectrum β-lactamases [ESBLs] and KPC) and class C (AmpC) enzymes.

For research use only. We do not sell to patients.
Relebactam Chemical Structure

Relebactam Chemical Structure

CAS No. : 1174018-99-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO $383 In-stock
1 mg $150 In-stock
5 mg $500 In-stock
10 mg $800 In-stock
25 mg $1400 In-stock
50 mg $2200 In-stock
100 mg   Get quote  
200 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

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Description

Relebactam is a diazabicyclooctane inhibitor with activity against a wide spectrum of β-lactamases, including class A (extended-spectrum β-lactamases [ESBLs] and KPC) and class C (AmpC) enzymes. Target: beta-lactamase Imipenem with Relebactam is active against Escherichia coli, Klebsiella pneumoniae, and Enterobacter spp., including K. pneumoniae carbapenemase (KPC)-producing isolates. The combination of Imipenem with Relebactam demonstrated activity against KPC-producing Enterobacteriaceae and multidrug-resistant P. aeruginosa. The imipenem MIC50 and MIC90 values for the ESBL-producing isolates were 0.25 and 0.5 μg/ml, respectively; with the addition of Relebactam, the corresponding values were 0.25 and 0.25 μg/ml. Five isolates harbored blaKPC. For these 5 isolates, the imipenem MICs ranged from 0.5 to >32 μg/ml. With the addition of Relebactam, the MICs decreased to 0.12 to 0.5 μg/ml.[1] Relebactam inhibits most class A and class C β-lactamases, with selected inhibition of class D enzymes by avibactam. β-Lactamase inhibitors (BLIs) have played an important role in combatting β-lactam resistance in Gram-negative bacteria, but their effectiveness has diminished with the evolution of diverse and deleterious varieties of β-lactamases.[2]

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01506271 Merck Sharp & Dohme Corp. Intra-abdominal Infections June 2012 Phase 2
NCT01505634 Merck Sharp & Dohme Corp. Urinary Tract Infections|Pyelonephritis May 2012 Phase 2
NCT01275170 Merck Sharp & Dohme Corp. Infectious Disease January 2011 Phase 1
NCT02452047 Merck Sharp & Dohme Corp. Bacterial Infections August 21, 2015 Phase 3
NCT02493764 Merck Sharp & Dohme Corp. Bacterial Pneumonia November 24, 2015 Phase 3
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References
Molecular Weight

348.38

Formula

C₁₂H₂₀N₄O₆S

CAS No.

1174018-99-5

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
Relebactam
Cat. No.:
HY-16752
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