[CAS NO. 1360457-46-0] Vaborbactam

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PRODUCTS SPECIFICATIONS [1360457-46-0]

Catalog

HY-19930

Brand

MCE

CAS

1360457-46-0

DESCRIPTION [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

For research use only. We do not sell to patients.

21 Publications Citing Use of MCE

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

In Vitro:

H ₂ O : 5.26 mg/mL ( 17.70 mM ; Need ultrasonic)

Preparing
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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

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.

Add each solvent one by one: 5% DMSO >> 40% PEG300 >> 5% Tween-80 >> 50% saline

Solubility: ≥ 2.62 mg/mL (8.82 mM); Clear solution
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

* All of the co-solvents are available by MCE.

References

Synonyms

1,2-Oxaborinane-6-acetic acid, 2-hydroxy-3-[[2-(2-thienyl)acetyl]amino]-, (3R,6S)-

(3R,6S)-2-Hydroxy-3-[[2-(2-thienyl)acetyl]amino]-1,2-oxaborinane-6-acetic acid

Vaborbactam

RPX 7009

2-{(3R,6S)-2-Hydroxy-3-[2-(thiophen-2-yl)acetamido]-1,2-oxaborinan-6-yl}acetic acid