Pyrimethamine

Catalog No.S2006

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

Price Stock Quantity  
In DMSO USD 130 In stock
USD 97 In stock
USD 310 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

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

  • Compare DHFR Inhibitors
    Compare DHFR Products
  • Research Area

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

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a 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, updated on 2014-10-16)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02211729 Not yet recruiting Malaria|Respiratory Infections London School of Hygiene and Tropical Medicine|Malaria Re  ...more 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 Sh  ...more 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, Flan  ...more Universiteit Antwerpen|Fund for Scientific Research, Flanders, Belgium|University of Kinshasa November 2012 Phase 3

view more

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.

Research Area

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.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related DHFR Products

  • AGI-6780

    AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant with IC50 of 23 nM.

  • Erastin

    Erastin is a ferroptosis activator by acting on mitochondrial VDAC, exhibiting selectivity for tumor cells bearing oncogenic RAS.

  • LB42708

    LB42708 is an orally active farnesyltransferase (FTase) inhibitor with IC50 of 0.8, 1.2, and 2.0 nM toward H-ras, N-ras, and K-ras, respectively.

  • Pemetrexed

    Pemetrexed is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively.

  • Methotrexate

    Methotrexate is an antimetabolite and antifolate drug, which acts by inhibiting the metabolism of folic acid.

  • Pralatrexate

    Pralatrexate is an antifolate, and structurally a folate analog. Its IC50 is < < 300 nM in some cell lines.

  • Tipifarnib

    Tipifarnib (R115777) is a potent and specific farnesyltransferase (FTase) inhibitor with IC50 of 0.6 nM, its anti-proliferative effects are most prominent in H-ras or N-ras mutant cells. Phase 3.

    Features:A potent and selective farnesyl protein transferase inhibitor with significant antitumor effects.

  • FK866 (APO866, Daporinad)

    FK866 (APO866, Daporinad) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase) with IC50 of 0.09 nM. Phase 1/2.

  • Abiraterone

    Abiraterone is a potent CYP17 inhibitor with IC50 of 2 nM.

    Features:Approved for the treatment of docetaxel-treated castration-resistant prostate cancer.

  • Roflumilast

    Roflumilast is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM.

Recently Viewed Items

Tags: buy Pyrimethamine | Pyrimethamine ic50 | Pyrimethamine price | Pyrimethamine cost | Pyrimethamine solubility dmso | Pyrimethamine purchase | Pyrimethamine manufacturer | Pyrimethamine research buy | Pyrimethamine order | Pyrimethamine mouse | Pyrimethamine chemical structure | Pyrimethamine mw | Pyrimethamine molecular weight | Pyrimethamine datasheet | Pyrimethamine supplier | Pyrimethamine in vitro | Pyrimethamine cell line | Pyrimethamine concentration | Pyrimethamine nmr
Contact Us