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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Purity: ≥98%
Vaborbactam (formerly PX-7009; MP-7009; RPX7009; trade name: Vabomere) is novel, potent and broad spectrum non-β-lactam (cyclic boronic acid pharmacophore) β-lactamase inhibitor discovered by Rempex Pharmaceuticals and approved in 2017 for the treatment of complicated urinary tract infections and pyelonephritis. It is not effective as an antibiotic by itself, but it restores the potency of existing antibiotics by inhibiting the beta-lactamase enzymes that would otherwise degrade them. When combined with an appropriate antibiotic it can be used for the treatment of gram-negative bacterial infections. In the United States, the combination drug meropenem/vaborbactam (Vabomere) was approved by the FDA (Food and Drug Administration) on 8/29/2017 for treating complicated urinary tract infections and pyelonephritis.
ln Vitro |
Vaborbactam exhibits a wide range of β-lactamase inhibition, with a strong affinity for KPC, CTX-M, SHV, and CMY enzymes[1]. When the concentration of the inhibitor is fixed at ≥8 μg/mL, maximum potentiation is achieved (≥96.5% of isolates are inhibited at ≤2 μg/mL of SM 7338-vaborbactam). Vaborbactam restores SM 7338 activity for 72.7 to 98.1% of CPE isolates at ≤2 μg/mL. At a fixed concentration of 8 μg/mL, SM 7338-vaborbactam inhibits 93.7% of CPE isolates that show elevated SM 7338 MICs at ≤1 μg/mL (MIC50, ≤0.06 μg/mL for all organisms)[2]. Vaborbactam functions as a competitive inhibitor and prevents the b-lactamase from hydrolyzing it by creating a reversible dative bond with the blactamase[3].
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ln Vivo |
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References |
Molecular Formula |
C12H16BNO5S
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Molecular Weight |
297.13
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Exact Mass |
297.08
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Elemental Analysis |
C, 48.51; H, 5.43; B, 3.64; N, 4.71; O, 26.92; S, 10.79
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CAS # |
1360457-46-0
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Related CAS # |
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Appearance |
Solid powder
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SMILES |
O=C(O)C[C@@H]1CC[C@H](NC(CC2=CC=CS2)=O)B(O)O1
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InChi Key |
IOOWNWLVCOUUEX-WPRPVWTQSA-N
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InChi Code |
InChI=1S/C12H16BNO5S/c15-11(7-9-2-1-5-20-9)14-10-4-3-8(6-12(16)17)19-13(10)18/h1-2,5,8,10,18H,3-4,6-7H2,(H,14,15)(H,16,17)/t8-,10-/m0/s1
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Chemical Name |
2-((3R,6S)-2-hydroxy-3-(2-(thiophen-2-yl)acetamido)-1,2-oxaborinan-6-yl)acetic acid
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Synonyms |
RPX-7009; MP-7009; RPX7009; MP7009; REBO07; REBO 07; MP7; MP 7; RPX 7009; MP 7009; REBO-07; MP-7; Trade name: Vabomere
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
H2O : ~5.26 mg/mL (~17.70 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 25 mg/mL (84.14 mM) in 108 mM sodium carbonate (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
Solubility in Formulation 2: ≥ 2.62 mg/mL (8.82 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.62 mg/mL (8.82 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 27.5 mg/mL (92.55 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.3655 mL | 16.8277 mL | 33.6553 mL | |
5 mM | 0.6731 mL | 3.3655 mL | 6.7311 mL | |
10 mM | 0.3366 mL | 1.6828 mL | 3.3655 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.