Size | Price | Stock | Qty |
---|---|---|---|
1mg |
|
||
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
500mg |
|
||
Other Sizes |
|
Purity: ≥98%
Relebactam (also known as MK7655; MK-7655) is a diazabicyclooctane that acts as a potent and selective β-lactamase inhibitor. It has activity against a wide spectrum of β-lactamases, including class A (extended-spectrum β-lactamases [ESBLs] and KPC) and class C (AmpC) enzymes. Relebactam reduced imipenem MICs for Enterobacteriaceae with KPC carbapenemases from 16-64 mg/L to 0.12-1 mg/L. MK-7655 potentiated imipenem against Enterobacteriaceae with KPC carbapenemases or combinations of β-lactamase and impermeability, but not those with metallo-carbapenemases. It augmented the activity of imipenem against P. aeruginosa in general and OprD mutants in particular.
ln Vitro |
Relebactam and imipenem together show efficacy against multidrug-resistant P. aeruginosa and KPC-producing Enterobacteriaceae[1].
Relebactam has antipseudomonal activity and exhibits a limited inhibition of Class D-producing bacteria[2]. |
---|---|
References |
|
Molecular Formula |
C12H20N4O6S
|
---|---|
Molecular Weight |
348.3754
|
Exact Mass |
348.11
|
Elemental Analysis |
41.37; H, 5.79; N, 16.08; O, 27.55; S, 9.20
|
CAS # |
1174018-99-5
|
Related CAS # |
1174020-13-3 (hydrate);1174018-99-5 (free acid);1502858-91-4 (sodium);
|
Appearance |
White to off-white solid powder.
|
SMILES |
O=S(O)(ON1[C@]2([H])CC[C@@H](C(NC3CCNCC3)=O)[N@@](C2)C1=O)=O
|
InChi Key |
SMOBCLHAZXOKDQ-ZJUUUORDSA-N
|
InChi Code |
InChI=1S/C12H20N4O6S/c17-11(14-8-3-5-13-6-4-8)10-2-1-9-7-15(10)12(18)16(9)22-23(19,20)21/h8-10,13H,1-7H2,(H,14,17)(H,19,20,21)/t9-,10+/m1/s1
|
Chemical Name |
(1R,2S,5R)-7-oxo-2-(piperidin-4-ylcarbamoyl)-1,6-diazabicyclo[3.2.1]octan-6-yl hydrogen sulfate
|
Synonyms |
MK-7655; Relebactam; MK 7655; MK7655
|
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) |
DMSO : 70~125 mg/mL (200.93~358.80 mM )
H2O : ~50 mg/mL (~143.52 mM )
|
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: 25 mg/mL (71.76 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
 (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 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 | 0.2870 mL | 1.4352 mL | 2.8704 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.