Shopping Cart

Your shopping cart is currently empty

PF-04753299

Name: PF-04753299
Brand: TargetMol
SKU: T41275
Price: 397 USD
Availability: InStock
Rating: 5 (10 reviews)

Copy Product Info

🥰Excellent

Catalog No. T41275Cas No. 1289620-49-0

PF-04753299 is a potent and selective inhibitor of UDP-3-O-(R-3-hydroxymyristol)-N-acetylglucosamine deacetylase (LpxC), demonstrating bactericidal effects against gonococcal isolates and exhibiting inhibitory activity against E. coli, P. aeruginosa, and K. pneumoniae, with minimum inhibitory concentration (MIC) 90 values of 2 μg/ml, 4 μg/ml, and 16 μg/ml, respectively. This compound is utilized in researching gram-negative bacterial infections [1].

PF-04753299

Copy Product Info

🥰Excellent

Purity: 99.88%

Catalog No. T41275Cas No. 1289620-49-0

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$68	In Stock	In Stock
2 mg	$105	In Stock	In Stock
5 mg	$165	In Stock	In Stock
10 mg	$238	In Stock	In Stock
25 mg	$397	In Stock	In Stock
50 mg	Preferential	In Stock	In Stock

Add to Cart

Add to Quotation

In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Questions

Batch Information

Select Batch

Purity:99.88%

Appearance:Solid

Color:White

Resource Download

COA HNMR LCMS

Product Introduction

PF-04753299 AI Summary

PF-04753299 exhibits potent antibacterial properties with strong inhibition of Pseudomonas aeruginosa LpxC enzyme (IC50 of 1.37 nM). It also shows considerable antibacterial activity against various bacterial strains, with MIC values ranging from 0.008 to 64.0 ug/mL, and specific activity against quinolone-resistant Pseudomonas aeruginosa PA3060 and PA7 with an MIC of 1.0 ug/mL. The compound displays moderate inhibition of human MMP12 (Ki of 1350.0 nM) and MMP13 (Ki of 7730.0 nM), as well as inhibition of the human norepinephrine transporter (IC50 of 340.0 nM, Ki of 250.0 nM). Pharmacokinetically, it has moderate solubility, moderate clearance, and volume of distribution in rats, along with a moderate half-life and free AUC in rat plasma. It also has a low fraction unbound in both rat and human plasma, and lipophilicity with a log D value of 2.24. These properties suggest that PF-04753299 has strong antibacterial efficacy and favorable pharmacokinetic characteristics..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description

In vivo

Rats were subjected to intraperitoneal challenge with Pseudomonas aeruginosa strain UC12120, a penicillin-resistant, quinolone-susceptible clinical isolate (1a Minimum Inhibitory Concentration MIC = 0.25 μg/mL), at 0.5 hr and 4 hr post-treatment with PF-04753299 (Subcutaneous Dose; Vehicle: 40% β-cyclodextrin dissolved in water). At 24 h post-infection, animals were necropsied and the bacterial load on the spleen was subsequently determined. The dose of compound required to reduce the bacterial load by 50% (ED50) was determined to be 35 mg/kg compared to untreated animals [2].

Chemical Properties

Molecular Weight	347.43
Formula	C₁₈H₂₁NO₄S
Cas No.	1289620-49-0
Smiles	C(C[C@](C(NO)=O)(S(C)(=O)=O)C)C1=CC=C(C=C1)C2=CC=CC=C2

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 70 mg/mL (201.48 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.8783 mL	14.3914 mL	28.7828 mL	143.9139 mL
5 mM	0.5757 mL	2.8783 mL	5.7566 mL	28.7828 mL
10 mM	0.2878 mL	1.4391 mL	2.8783 mL	14.3914 mL
20 mM	0.1439 mL	0.7196 mL	1.4391 mL	7.1957 mL
50 mM	0.0576 mL	0.2878 mL	0.5757 mL	2.8783 mL
100 mM	0.0288 mL	0.1439 mL	0.2878 mL	1.4391 mL

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc