Pyrimethamine

Catalog No.S2006

Pyrimethamine is a dihydrofolate reductase(DHFR) inhibitor with an IC50 of 15.4 nM.

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In DMSO USD 130 In stock
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Pyrimethamine Chemical Structure

Pyrimethamine Chemical Structure
Molecular Weight: 248.71

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Pyrimethamine is available in the following compound libraries:

Product Information

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Product Description

Biological Activity

Pyrimethamine is a dihydrofolate reductase(DHFR) inhibitor with an IC50 of 15.4 nM. It is a medication used for protozoal infections. It is commonly used as an antimalarial drug (for both treatment and prevention of malaria), and is also used (combined with sulfadiazine) in the treatment of Toxoplasma gondii infections in immune-compromised patients, such as HIV-positive individuals. It interferes with folic acid synthesis by inhibiting the enzyme dihydrofolate reductase (DHFR). Folic acid is needed for DNA and RNA synthesis in many species, including protozoa. [1]

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km
Example

For example, to convert the dose of resveratrol used in a mouse (22.4 mg/kg) to a dose based on surface area for rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)

Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02211729 Not yet recruiting Malaria|Respiratory Infections London School of Hygiene and Tropical Medicine|Malaria Research and Training Center, Bamako, Mali|Institut de Recherche en Sciences de la Sante, Burkina Faso August 2014 Phase 3
NCT02163447 Recruiting Malaria University of California, San Francisco|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) June 2014 Phase 3
NCT01746199 Not yet recruiting Malaria in Pregnancy|HIV Infection Institut Pasteur|Institut Pasteur de Bangui December 2013 Phase 3
NCT01973933 Completed Healthy Seoul National University Hospital June 2013 Phase 1
NCT01722539 Completed Healthy Universiteit Antwerpen|Fund for Scientific Research, Flanders, Belgium|University of Kinshasa November 2012 Phase 3

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Chemical Information

Download Pyrimethamine SDF
Molecular Weight (MW) 248.71
Formula

C12H13ClN4

CAS No. 58-14-0
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms
Solubility (25°C) * In vitro DMSO 10 mg/mL (40 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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