Catalog No.S2006

Pyrimethamine is a dihydrofolate reductase (DHFR) inhibitor, used as an antimalarial drug.

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

Description Pyrimethamine is a dihydrofolate reductase (DHFR) inhibitor, used as an antimalarial drug.
Targets DHFR [1]
IC50 15.4 nM
In vitro Pyrimethamine has an IC50 of 5–13 μM for the Hex isozymes at pH 4.3. Pyrimethamine increases the enzyme activity and protein level of the α and β subunits of Hex A in the βR505Q/Δ16kb cell line. [1] Pyrimethamine-sulfadoxine is an inhibitor of dihydrofolate reductase(DHFR) that has been widely used to treat chloroquine-resistant Plasmodium falciparum malaria. [2] Pyrimethamine is a potent inhibitor of mouse (m)Mate1 (K(i) = 145 nM) among renal organic cation transporters mOctn1 and mOctn2 (K(i) > 30 mM), mOct1 (K(i) = 3.6 mM), and mOct2 (K(i) = 6.0 mM). Pyrimethamine inhibits the uptake of metformin by kidney brush-border membrane vesicles (BBMVs) (K(i) = 41 nM) and canalicular membrane vesicles in the presence of outward gradient of H+. Pyrimethamine treatment significantly increases the kidney-to-plasma ratio of tetraethylammonium, and both the liver- and kidney-to-plasma ratios of metformin in mice, whereas it does not affect their plasma concentrations and urinary excretion rates. Pyrimethamine is a potent inhibitor of human (h)MATE1 and hMATE2-K (K(i) = 77 and 46 nM, respectively) and H+ and organic cation exchanger in human kidney BBMVs (K(i) = 31 nM) in the presence of outward gradient of H+. [3]
In vivo

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

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
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)


[1] Maegawa GH, et al. J Biol Chem, 2007, 282(12), 9150-9161.

[2] Akao M, et al. J Am Coll Cardiol, 2002, 40(4), 803-810.

view more

Clinical Trial Information( data from, updated on 2015-06-27)

NCT Number Recruitment Conditions Sponsor
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 Active, not 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
NCT02351687 Recruiting Malnutrition Washington University School of Medicine|University of Ma  ...more Washington University School of Medicine|University of Malawi April 2014 --
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

view more

Chemical Information

Download Pyrimethamine SDF
Molecular Weight (MW) 248.71


CAS No. 58-14-0
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 10 mg/mL (40.2 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo
* <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.
Chemical Name 5-​(4-​chlorophenyl)​-​6-​ethyl-2,​4-​pyrimidinediamine

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

  • Pemetrexed Disodium Hydrate

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

  • INCB024360

    INCB024360 is a potent, competitive IDO1 (indoleamine-(2,3)-dioxygenase) inhibitor with IC50 of 67 nM. Phase 2.

  • U73122

    U73122 is a potent phospholipase C (PLC) inhibitor, which reduces agonist-induced Ca2+ increases in platelets and PMN.

  • 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 in cell-free assays, respectively.

  • Methotrexate

    Methotrexate is an antimetabolite and antifolate drug, which acts by inhibiting the metabolism of folic acid in activated peripheral T cells.

  • Pralatrexate

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

  • Sulfameter

    Sulfameter is a long-acting sulfonamide antibacterial.

  • Erastin

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

  • NLG919

    NLG919 is a potent IDO (indoleamine-(2,3)-dioxygenase) pathway inhibitor with Ki/EC50 of 7 nM/75 nM in cell-free assays. Phase 1.

  • CX-4945 (Silmitasertib)

    CX-4945 (Silmitasertib) is a potent and selective inhibitor of CK2 (casein kinase 2) with IC50 of 1 nM in a cell-free assay, less potent to Flt3, Pim1 and CDK1 (inactive in cell-based assay). Phase 1/2.

    Features:First clinical inhibitor of CK2.

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
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description
Contact Us