Pyrimethamine

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Cat.No. 3918 - Pyrimethamine | C12H13ClN4 | CAS No. 58-14-0
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)
Datasheet
Citations
Reviews
Literature (2)

Biological Activity

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

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

Technical Data

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

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

Preparing Stock Solutions

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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References

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


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View all Multidrug Transporter Inhibitors

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

Citations for Pyrimethamine

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