Home Cart Sign in  
Chemical Structure| 58-14-0 Chemical Structure| 58-14-0
Chemical Structure| 58-14-0

*Storage: {[sel_prStorage]}

*Shipping: {[sel_prShipping]}

,{[proInfo.pro_purity]}

Pyrimethamine inhibits multidrug and toxin extrusion (MATE) transporter potently, it also inhibits dihydrofolate reductase (DHFR), used for protozoal infections and interferes with tetrahydrofolic acid synthesis from folic acid. Pyrimethamine inhibits adult polycystic kidney disease by modulating STAT signaling pathways.

Synonyms: Pirimecidan; Pirimetamin; NSC 3061

4.5 *For Research Use Only !

{[proInfo.pro_purity]}
Cat. No.: {[proInfo.prAm]} Purity: {[proInfo.pro_purity]}

Change View

Size Price VIP Price

US Stock

Global Stock

In Stock
{[ item.pr_size ]} Inquiry {[ getRatePrice(item.pr_usd,item.pr_rate,item.mem_rate,item.pr_is_large_size_no_price, item.vip_usd) ]}

US Stock: ship in 0-1 business day
Global Stock: ship in 5-7 days

  • {[ item.pr_size ]}

In Stock

- +

Please Login or Create an Account to: See VIP prices and availability

US Stock: ship in 0-1 business day
Global Stock: ship in 2 weeks

  • 1-2 Day Shipping
  • High Quality
  • Technical Support
Product Citations

Product Citations

Verónica Urdaneta-Páez ; Randy Hamchand ; Karen Anthony ; Jason Crawford ; Alan G. Sutherland ; Barbara I. Kazmierczak

Abstract: Pseudomonas aeruginosa is intrinsically resistant to many classes of antibiotics, reflecting the restrictive nature of its outer membrane and the action of its numerous efflux systems. However, the dynamics of compound uptake, retention, and efflux in this bacterium remain incompletely understood. Here, we exploited the sensor capabilities of a Z-nucleotide-sensing riboswitch to create an experimental system able to identify physicochemical and structural properties of compounds that permeate the bacterial cell, avoid efflux, and perturb the folate cycle or de novo purine synthesis. In the first step, a collection of structurally diverse compounds enriched in antifolate drugs was screened for ZTP (5-aminoimidazole-4-carboxamide riboside 5′-triphosphate) riboswitch reporter activity in efflux-deficient P. aeruginosa, allowing us to identify compounds that entered the cell and disrupted the folate pathway. These initial hits were then rescreened using isogenic efflux-proficient bacteria, allowing us to separate efflux substrates from efflux avoiders. We confirmed this categorization by measuring intracellular levels of select compounds in the efflux-deficient and -proficient strain using high-resolution liquid chromatography-mass spectrometry (LC-MS). This simple yet powerful method, optimized for high-throughput screening, enables the discovery of numerous permeable compounds that avoid efflux and paves the way for further refinement of the physicochemical and structural rules governing efflux in this multidrug-resistant Gram-negative pathogen. IMPORTANCE: Treatment of Pseudomonas aeruginosa infections has become increasingly challenging. The development of novel antibiotics against this multidrug-resistant bacterium is a priority, but many drug candidates never achieve effective concentrations in the bacterial cell due to its highly restrictive outer membrane and the action of multiple efflux pumps. Here, we develop a robust and simple reporter system in P. aeruginosa to screen chemical libraries and identify compounds that either enter the cell and remain inside or enter the cell and are exported by efflux systems. This approach enables the development of rules of compound uptake and retention in P. aeruginosa that will lead to more rational design of novel antibiotics.

Keywords: Pseudomonas aeruginosa ; antimicrobial resistance ; drug efflux

Purchased from AmBeed: ; ;

Alternative Products

Product Details of Pyrimethamine

CAS No. :58-14-0
Formula : C12H13ClN4
M.W : 248.71
SMILES Code : NC1=NC(CC)=C(C2=CC=C(Cl)C=C2)C(N)=N1
Synonyms :
Pirimecidan; Pirimetamin; NSC 3061
MDL No. :MFCD00057350
InChI Key :WKSAUQYGYAYLPV-UHFFFAOYSA-N
Pubchem ID :4993

Safety of Pyrimethamine

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335-H351-H361
Precautionary Statements:P261-P305+P351+P338

Application In Synthesis of Pyrimethamine

* All experimental methods are cited from the reference, please refer to the original source for details. We do not guarantee the accuracy of the content in the reference.

  • Downstream synthetic route of [ 58-14-0 ]
 

Historical Records

Categories