Art. -Nr.: HY-B0967

Phthalylsulfacetamide

Name: Phthalylsulfacetamide
Brand: MedChemExpress
SKU: HY-B0967
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Phthalylsulfacetamide is an orally active sulfonamide antibiotic and New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC₅₀ of 15.4 μM. Phthalylsulfacetamide stably binds to the active hydrolysis center of NDM-1, interacts with Zn²⁺, and interacts with key amino acid residues Val73 and His122 to inhibit enzyme activity. Phthalylsulfacetamide can be used for the research of Escherichia coli infection.

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Reinheit : 98.0%
CAS. Nr.: 131-69-1
Formel: C₁₆H₁₄N₂O₆S
Molecular Weight:362.36

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Phthalylsulfacetamide Chemical Structure

CAS. Nr.: 131-69-1

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Antibiotic Isoform-spezifische Produkte anzeigen :

In Vitro

Phthalylsulfacetamide (4-128 μM) potently inhibits purified recombinant NDM-1 enzyme activity with an IC₅₀ of 15.4 μM^[1].
Phthalylsulfacetamide (16 h) alone exhibits negligible intrinsic antibacterial activity against NDM-1-positive Escherichia coli with an MIC of 512 μg/mL^[1].
Phthalylsulfacetamide (16 h) acts synergistically with Meropenem (HY-13678) against NDM-1-positive Escherichia coli, reducing Meropenem's MIC by 32-fold with an FICI of 0.156^[1].
Phthalylsulfacetamide (64 μg/mL), when combined with Meropenem, rapidly eliminates NDM-1-positive Escherichia coli within 3 h, with no regrowth observed^[1].
Phthalylsulfacetamide (1-8 mg/mL; 24 h) exhibits no significant cytotoxicity toward mouse small intestinal mucosal epithelial cells^[1].

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

Cell Cytotoxicity Assay^[1]

Cell Line:

mouse small intestinal mucosal epithelial cells
Concentration:

1 mg/mL; 2 mg/mL; 4 mg/mL; 8 mg/mL
Incubation Time:

24 h
Result:

Resulted in a cell survival rate exceeding 95% at concentrations up to 8 mg/mL, with no significant reduction in cell viability (P > 0.05).

In Vivo

Phthalylsulfacetamide (5-20 mg/kg; i.g.; every 12 hours; 6 doses), when combined with Meropenem, dose-dependently reduces bacterial load, white blood cell counts, and proinflammatory cytokine levels in mice with systemic NDM-1-positive E. coli infection^[1].
Phthalylsulfacetamide (20 mg/kg; i.g.; every 12 hours; 6 doses), when combined with Meropenem, increases survival rate to 70% in mice with lethal systemic NDM-1-positive E. coli infection^[1].
Phthalylsulfacetamide (20 mg/kg; i.g.; every 12 hours; 6 doses), when combined with Meropenem, reduces bacterial load, white blood cell counts, and proinflammatory cytokine levels, and alleviates histopathological damage in mice with sublethal systemic NDM-1-positive E. coli infection, while monotherapy only reduces small intestine bacterial load^[1].

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

Animal Model:

BALB/c (female, 6-8 weeks old, 18-20 g, intraperitoneal inoculation with NDM-1-positive *E. coli*)^[1]
Dosage:

5 mg/kg; 10 mg/kg; 20 mg/kg
Administration:

i.g.; every 12 hours; 6 doses
Result:

Produced the most significant reduction in white blood cell counts, bacterial loads in liver, spleen, and small intestine tissues, and serum levels of proinflammatory cytokines TNF-α, IL-1β, and IFN-γ at 20 mg/kg when combined with Meropenem (P < 0.05).

Animal Model:

SPF BALB/c (6-8 weeks old, intraperitoneal inoculation with lethal dose of NDM-1-positive *E. coli*)^[1]
Dosage:

20 mg/kg
Administration:

i.g.; every 12 hours; 6 doses
Result:

Resulted in a 70% survival rate at 120 hours post-infection when combined with Meropenem, which was significantly higher than the 20% survival rate of infection controls (P < 0.01).
Did not significantly improve survival as monotherapy compared to infection controls.

Animal Model:

SPF BALB/c (6-8 weeks old, intraperitoneal inoculation with sublethal dose of NDM-1-positive *E. coli*)^[1]
Dosage:

20 mg/kg
Administration:

i.g.; every 12 hours; 6 doses
Result:

Significantly reduced bacterial load in the small intestine as monotherapy (P < 0.05).
Significantly reduced white blood cell counts, bacterial loads in liver, spleen, and small intestine tissues, and serum levels of proinflammatory cytokines TNF-α, IL-1β, and IFN-γ when combined with Meropenem (P < 0.05).
Significantly ameliorated histopathological damage to liver, spleen, and small intestine tissues, restoring tissue architecture to near-normal levels, and restored the integrity of small intestine villus ultrastructure with neatly arranged brush borders when combined with Meropenem.

Related Protocols :

Research Protocol for Infectious Diseases

Chemical Information

CAS. Nr. 131-69-1
Appearance Solid
Molecular Weight 362.36
Formel C₁₆H₁₄N₂O₆S
Color White to off-white
SMILES

O=C(O)C1=CC=CC=C1C(NC2=CC=C(S(=O)(NC(C)=O)=O)C=C2)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 25 mg/mL (68.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 1 mg/mL (2.76 mM; ultrasonic and warming and heat to 80°C)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7597 mL

13.7984 mL

27.5969 mL

5 mM

0.5519 mL

2.7597 mL

5.5194 mL

10 mM

0.2760 mL

1.3798 mL

2.7597 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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: ≥ 2.5 mg/mL (6.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Li X, et al. Mechanistic insights into phthalylsulfacetamide-induced restoration of meropenem bactericidal activity in NDM-1-positive Escherichia coli. BMC Microbiol. 2026;26(1):521. Published 2026 Apr 20. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	2.7597 mL	13.7984 mL	27.5969 mL	68.9922 mL
DMSO	5 mM	0.5519 mL	2.7597 mL	5.5194 mL	13.7984 mL
	10 mM	0.2760 mL	1.3798 mL	2.7597 mL	6.8992 mL
	15 mM	0.1840 mL	0.9199 mL	1.8398 mL	4.5995 mL
	20 mM	0.1380 mL	0.6899 mL	1.3798 mL	3.4496 mL
	25 mM	0.1104 mL	0.5519 mL	1.1039 mL	2.7597 mL
	30 mM	0.0920 mL	0.4599 mL	0.9199 mL	2.2997 mL
	40 mM	0.0690 mL	0.3450 mL	0.6899 mL	1.7248 mL
	50 mM	0.0552 mL	0.2760 mL	0.5519 mL	1.3798 mL
	60 mM	0.0460 mL	0.2300 mL	0.4599 mL	1.1499 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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Phthalylsulfacetamide

Alle Antibiotic Isoform-spezifische Produkte anzeigen