2. Anti-infection
  3. Beta-lactamase Bacterial
  4. Nacubactam

Nacubactam  (Synonyms: OP0595 free acid)

製品番号: HY-109008 純度: 99.06%
COA 取扱説明書 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

Nacubactam 構造式

CAS 番号 : 1452458-86-4

容量 価格（税別） 在庫状況 数量
5 mg $160 在庫あり
10 mg $265 在庫あり
50 mg $930 在庫あり
100 mg $1490 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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

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Based on 2 publication(s) in Google Scholar

Other Forms of Nacubactam:

Nacubactam 関連抗体

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Beta-lactamase アイソフォーム固有の製品をすべて表示:

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

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製品説明

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[1][2][3][4][5][6].

IC50 & Target

non-β-lactam-β-lactamase[1]
体外実験

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.

Nacubactam 関連抗体
体内実験

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.
臨床実験
分子量

324.31

分子式

C9H16N4O7S
CAS 番号
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

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

DMSO : 100 mg/mL (308.35 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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.

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)

g

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).
純度とドキュメンテーション

純度: 99.06%

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

取扱説明書 (2659 KB)
参考文献

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.

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.

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Nacubactam Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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  • 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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