Nacubactam (Synonyms: OP0595 free acid)

Name: Nacubactam
Brand: MedChemExpress
SKU: HY-109008
Rating: 5.0 (2 reviews)

Cat. No.: HY-109008 Purity: 99.06%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

Nacubactam (OP0595 free acid) is a potent non-β-lactam-β-lactamase inhibitor with activity against class A and C β-lactamases. Nacubactam acts as a penicillin binding protein (PBP) 2-active antibacterial, and gives β-lactamase-independent potentiation of β-lactams targeting other PBPs. Nacubactam potentiates the antimicrobial activities of Piperacillin (HY-B1923), Cefepime (HY-B0692), and Meropenem (HY-13678) against CTX-M-15-positive Escherichia coli and KPC-positive Klebsiella pneumoniae.

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Nacubactam 화학구조

CAS No. : 1452458-86-4

사이즈	재고	수량
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

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This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 2 publication(s) in Google Scholar

Other Forms of Nacubactam:

Nacubactam (Standard) 견적 받기

2 Publications Citing Use of MCE Nacubactam

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•Related Screening Libraries:

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View All Beta-lactamase Isoform Specific Products:

View All Isoforms

Metallo-β-lactamase (MBL) Serine β-lactamase (SBL)

Biological Activity
순도&문서
References
고객리뷰

제품 설명

IC₅₀ & Target

non-β-lactam-β-lactamase^[1]

In Vitro

Nacubactam (4 μg/mL) can reduce the minimum inhibitory concentrations (MICs) of Piperacillin (HY-B1923), Cefepime (HY-B0692), and Meropenem (HY-13678) against CTX-M-15-positive Escherichia coli and KPC-positive Klebsiella pneumoniae, enhancing the antibacterial activity^[1].
Nacubactam shows MICs ranging from 1 to >256 μg/mL against 11 Gram-negative isolates^[2].
Nacubactam (8 μg/mL) can reduce the MIC₅₀ of Meropenem by 8-fold, making all isolates susceptible or intermediately susceptible to Meropenem^[4].
Nacubactam can inhibit Carbapenem-resistant Klebsiella pneumoniae producing KPC and restore the antibacterial activity of Meropenem^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Nacubactam (2.5 mg/kg; s.c.; administered once at 1, 3, and 5 h after infection), when combined with Cefepime, can significantly reduce the bacterial load of CTX-M-15-positive Escherichia coli and KPC-positive Klebsiella pneumoniae in a neutropenic murine thigh infection model^[1].
Nacubactam (10-80 mg/kg; s.c.; administered every 8 h), when combined with Meropenem, shows the greatest in-vivo efficacy against 9 out of 10 Gram-negative isolates in a neutropenic murine complicated urinary tract infection model, reducing the bacterial load by 3 log from the 48-h control^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

분자량

324.31

화학식

C₉H₁₆N₄O₇S

CAS No.

1452458-86-4

Appearance

Solid

Color

White to light brown

SMILES

O=S(ON1[C@]2([H])CC[C@@H](C(NOCCN)=O)[N@@](C2)C1=O)(O)=O

선적

Room temperature in continental US; may vary elsewhere.

보관

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

용액&용해도

In Vitro:

DMSO : 250 mg/mL (770.87 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 50 mg/mL (154.17 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.0835 mL	15.4173 mL	30.8347 mL
5 mM	0.6167 mL	3.0835 mL	6.1669 mL
10 mM	0.3083 mL	1.5417 mL	3.0835 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

몰농도 계산기
농도 희석 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (6.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 100 mg/mL (308.35 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

순도&문서

Purity: 99.06%

Select Batch:

Data Sheet (276 KB) SDS (392 KB)

COA (249 KB) HNMR (202 KB) LCMS (382 KB)

Handling Instructions (2659 KB)

References

[1]. Morinaka A, et al. In Vitro and In Vivo Activities of OP0595, a New Diazabicyclooctane, against CTX-M-15-Positive Escherichia coli and KPC-Positive Klebsiella pneumoniae. Antimicrob Agents Chemother. 2016 Apr 22;60(5):3001-6. [Content Brief]

[2]. Monogue ML, et al. In Vivo Efficacy of Meropenem with a Novel Non-β-Lactam-β-Lactamase Inhibitor, Nacubactam, against Gram-Negative Organisms Exhibiting Various Resistance Mechanisms in a Murine Complicated Urinary Tract Infection Model. Antimicrob Agents Chemother. 2018 Aug 27;62(9):e02596-17. [Content Brief]

[3]. Misawa K, et al. In vitro effects of diazabicyclooctane β-lactamase inhibitors relebactam and nacubactam against three subspecies of Mycobacterium abscessus complex. Int J Antimicrob Agents. 2022 Nov-Dec;60(5-6):106669. [Content Brief]

[4]. Kaushik A, et al. New β-Lactamase Inhibitors Nacubactam and Zidebactam Improve the In Vitro Activity of β-Lactam Antibiotics against Mycobacterium abscessus Complex Clinical Isolates. Antimicrob Agents Chemother. 2019 Aug 23;63(9):e00733-19. [Content Brief]

[5]. Barnes MD, et al. Nacubactam Enhances Meropenem Activity against Carbapenem-Resistant Klebsiella pneumoniae Producing KPC. Antimicrob Agents Chemother. 2019 Jul 25;63(8):e00432-19. [Content Brief]

[6]. Livermore DM, et al. Activity of OP0595/β-lactam combinations against Gram-negative bacteria with extended-spectrum, AmpC and carbapenem-hydrolysing β-lactamases. J Antimicrob Chemother. 2015 Nov;70(11):3032-41. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	3.0835 mL	15.4173 mL	30.8347 mL	77.0867 mL
	5 mM	0.6167 mL	3.0835 mL	6.1669 mL	15.4173 mL
	10 mM	0.3083 mL	1.5417 mL	3.0835 mL	7.7087 mL
	15 mM	0.2056 mL	1.0278 mL	2.0556 mL	5.1391 mL
	20 mM	0.1542 mL	0.7709 mL	1.5417 mL	3.8543 mL
	25 mM	0.1233 mL	0.6167 mL	1.2334 mL	3.0835 mL
	30 mM	0.1028 mL	0.5139 mL	1.0278 mL	2.5696 mL
	40 mM	0.0771 mL	0.3854 mL	0.7709 mL	1.9272 mL
	50 mM	0.0617 mL	0.3083 mL	0.6167 mL	1.5417 mL
	60 mM	0.0514 mL	0.2570 mL	0.5139 mL	1.2848 mL
	80 mM	0.0385 mL	0.1927 mL	0.3854 mL	0.9636 mL
	100 mM	0.0308 mL	0.1542 mL	0.3083 mL	0.7709 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Nacubactam Related Classifications

Infection

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Nacubactam1452458-86-4OP0595OP 0595OP-0595Beta-lactamaseBacterialβ-lactamaseKlebsiella pneumoniaeEscherichia colineutropenicmiceGram-negativeInhibitorinhibitorinhibit

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Nacubactam (Synonyms: OP0595 free acid)

고객리뷰

Other Forms of Nacubactam:

Nacubactam Related Antibodies

2 Publications Citing Use of MCE Nacubactam

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Beta-lactamase Isoform Specific Products:

Biological Activity

순도&문서

References

고객리뷰

Nacubactam Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

Nacubactam Related Classifications

Keywords:

최근 본 상품:

고객리뷰

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report