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

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.

All Tocris products are intended for laboratory research use only.

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 solvent 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

Safety Datasheet

References

References are publications that support the products' biological activity.

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

Zimmerman et al (1987) Competitive inhibition of folate absorption by dihydrofolate reductase inhibitors, trimethoprim and pyrimethamine. 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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Keywords: inhibitors inhibits multidrug and toxin extrusion MATE transporters dihydrofolate reductase DHFR STAT3 signal transducer and activator of transcription 3 Multidrug Transporters

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