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[CAS NO. 1360457-46-0] Vaborbactam
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-19930 |
| Brand: | MCE |
| CAS: | 1360457-46-0 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 297.14 |
| Molecular Formula | C12H16BNO5S |
| SMILES | O=C(O)C[C@@H]1CC[C@H](NC(CC2=CC=CS2)=O)B(O)O1 |
21 Publications Citing Use of MCE
- [1]J Med Chem. 2021 Jul 31.
- [2]J Clin Microbiol. 2020 Aug 24;58(9):e00932-20.
- [3]J Antimicrob Chemother. 2021 May 6;dkab141.
- [4]J Antimicrob Chemother. 2021 Feb 11;76(3):653-658.
- [5]Antimicrob Agents Chemother. 2020 Nov 17;64(12):e00297-20.
- [6]Antimicrob Agents Chemother. 2020 Sep 21;64(10):e00409-20.
- [7]Antimicrob Agents Chemother. 2020 Mar 24;64(4):e02255-19.
- [8]Antimicrob Agents Chemother. 2019 Feb 26;63(3). pii: e02623-18.
- [9]Antimicrob Agents Chemother. 2018 Jul 27;62(8). pii: e00414-18.
- [10]Int J Antimicrob Agents. 2021 Sep 18;106439.
- [11]ACS Infect Dis. 2022 Feb 3.
- [12]ACS Infect Dis. 2021 Mar 16.
- [13]Antibiotics (Basel). 2021, 10(11), 1341.
- [14]Antibiotics (Basel). 2021 Sep 14;10(9):1110.
- [15]Open Forum Infect Di. 2020 Jan 4;7(1):ofz545.
- [16]Spectrochim Acta A Mol Biomol Spectrosc. 2020 Apr 5;230:118066.
- [17]Int J Infect Dis. 2021 Apr 14;S1201-9712(21)00346-5.
- [18]Bioorg Med Chem. 11 August 2021, 116343.
- [19]Infect Drug Resist. 2021 Jun 30;14:2499-2507.
- [20]MedChemComm. 2020 Apr 1; 11(4): 491-496.
- [21]bioRxiv. 2021 Mar 13.
Summary
Vaborbactam (RPX7009) is a cyclic boronic acid pharmacophore β-lactamase inhibitor.
In Vitro
Vaborbactam is a broad spectrum of inhibition of β-lactamases, with particularly potent activity against KPC, CTX-M, SHV, and CMY enzymes [1] . Vaborbactam restores SM 7338 activity for 72.7 to 98.1% of CPE isolates at ≤2 μg/mL, and maximum potentiation is achieved with fixed concentrations of ≥8 μg/mL of the inhibitor (≥96.5% of isolates are inhibited at ≤2 μg/mL of SM 7338-vaborbactam). SM 7338-vaborbactam with a fixed concentration of 8 μg/mL of the inhibitor (MIC50, ≤0.06 μg/mL for all organisms) inhibits 93.7% of the CPE isolates displaying elevated SM 7338 MICs at ≤1 μg/mL [2] . By forming a reversible dative bond with the blactamase, vaborbactam acts as a competitive inhibitor and is not hydrolyzed by the b-lactamase [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Vaborbactam is well tolerated and has a half-life of 1.23 h, and steadystate volume of distribution of 21.0 L in subjects [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02073812 | Rempex Pharmaceuticals (a wholly owned subsidiary of The Medicines Company) |
Healthy Subjects
|
February 2014 | Phase 1 |
| NCT01897779 | Rempex Pharmaceuticals (a wholly owned subsidiary of The Medicines Company) |
Healthy Volunteers|Bacterial Infections
|
July 2013 | Phase 1 |
| NCT01772836 | Rempex Pharmaceuticals (a wholly owned subsidiary of The Medicines Company) |
Healthy Volunteers|Bacterial Infections
|
March 2013 | Phase 1 |
| NCT01751269 | Rempex Pharmaceuticals (a wholly owned subsidiary of The Medicines Company) |
Healthy Volunteers|Bacterial Infections
|
December 2012 | Phase 1 |
| NCT02020434 | Rempex Pharmaceuticals (a wholly owned subsidiary of The Medicines Company) |
Subjects With Varying Degrees of Renal Insufficiency and|Subjects With Normal Renal Function
|
January 2014 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
H 2 O : 5.26 mg/mL ( 17.70 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.3654 mL | 16.8271 mL | 33.6542 mL |
| 5 mM | 0.6731 mL | 3.3654 mL | 6.7308 mL |
| 10 mM | 0.3365 mL | 1.6827 mL | 3.3654 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 27.5 mg/mL (92.55 mM); Clear solution; Need ultrasonic
-
2.
Add each solvent one by one: 108 mM sodium carbonate
Solubility: 25 mg/mL (84.14 mM); Clear solution; Need ultrasonic
-
3.
-
4.
Add each solvent one by one: 5% DMSO >> 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.62 mg/mL (8.82 mM); Clear solution
References
- [1] Hecker SJ, et al. Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. J Med Chem. 2015 May 14;58(9):3682-92.
- [2] Castanheira M, et al. Effect of the β-Lactamase Inhibitor Vaborbactam Combined with SM 7338 against Serine Carbapenemase-Producing Enterobacteriaceae. Antimicrob Agents Chemother. 2016 Aug 22;60(9):5454-8.
- [3] Wong D, et al. Novel Beta-Lactamase Inhibitors: Unlocking Their Potential in Therapy.
Synonyms
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