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Submit ReviewPyrimethamine
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)
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 |
| InChI Key | WKSAUQYGYAYLPV-UHFFFAOYSA-N |
| 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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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 www.P65Warnings.ca.gov
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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