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Description: Potent inhibitor of multidrug and toxin extrusion (MATE) transporters; also DHFR and STAT3 inhibitor
Chemical Name: 5-(4-Chlorophenyl)-6-ethyl-2,4-pyrimidinediamine
Purity: ≥99% (HPLC)
Citations (1)
Literature (1)

Biological Activity for Pyrimethamine

Pyrimethamine is a potent inhibitor of multidrug and toxin extrusion (MATE) transporters (Ki values are 46 and 77 nM for human MATE2-K-HEK293 and MATE1-HEK293 cells respectively). Also inhibits dihydrofolate reductase (DHFR) and STAT3. Decreases proliferation of human autosomal dominant polycystic kidney disease cells.

Compound Libraries for Pyrimethamine

Pyrimethamine is also offered as part of the Tocriscreen Antiviral Library and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.

Technical Data for Pyrimethamine

M. Wt 248.71
Formula C12H13ClN4
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 58-14-0
PubChem ID 4993
Smiles ClC1=CC=C(C2=C(N)N=C(N)N=C2CC)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Pyrimethamine

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 24.87 100
ethanol 2.49 10

Preparing Stock Solutions for Pyrimethamine

The following data is based on the product molecular weight 248.71. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 4.02 mL 20.1 mL 40.21 mL
5 mM 0.8 mL 4.02 mL 8.04 mL
10 mM 0.4 mL 2.01 mL 4.02 mL
50 mM 0.08 mL 0.4 mL 0.8 mL

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Product Datasheets for Pyrimethamine

References for Pyrimethamine

References are publications that support the biological activity of the product.

Ito et al (2010) Potent and specific inhibition of mMate1-mediated efflux of type I organic cations in the liver and kidney by pyrimeth. J.Pharmacol.Exp.Ther. 333 341 PMID: 20065018

Zimmerman et al (1987) Competitive inhibition of folate absorption by dihydrofolate reductase inhibitors, trimeth. and pyrimeth. Am.J.Clin.Nutr. 46 518 PMID: 3630970

Takakura et al (2011) Pyrimethamine inhibits adult polycystic kidney disease by modulating STAT signaling pathways. Hum.Mol.Genet. 20 4143 PMID: 21821671

If you know of a relevant reference for Pyrimethamine, please let us know.

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Keywords: Pyrimethamine, Pyrimethamine supplier, inhibitors, inhibits, multidrug, and, toxin, extrusion, MATE, transporters, dihydrofolate, reductase, DHFR, STAT3, signal, transducer, activator, of, transcription, 3, Multidrug, Transporters, Dihydrofolate, Reductase, STAT, 3918, Tocris Bioscience

⚠ WARNING: This product can expose you to chemicals including Pyrimethamine, which is known to the State of California to cause reproductive toxicity with developmental effects. For more information, go to

1 Citation for Pyrimethamine

Citations are publications that use Tocris products. Selected citations for Pyrimethamine include:

Hui et al (2020) Simultaneous Control of Endogenous and User-Defined Genetic Pathways Using Unique ecDHFR Pharmacological Chaperones. Cell Chem Biol 27 622-634.e6 PMID: 32330442

Do you know of a great paper that uses Pyrimethamine from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

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