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Pyrimethamine

Catalog No. T0849   CAS 58-14-0
Synonyms: Pirimecidan, RP 4753, Pirimetamin

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

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Pyrimethamine Chemical Structure
Pyrimethamine, CAS 58-14-0
Pack Size Availability Price/USD Quantity
50 mg In stock $ 38.00
100 mg In stock $ 52.00
200 mg In stock $ 78.00
1 mL * 10 mM (in DMSO) In stock $ 50.00
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Purity: 99.74%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Pyrimethamine (Pirimecidan) is a competitive inhibitor of dihydrofolate reductase (DHFR), used as an antimalarial drug.
Targets&IC50 DHFR: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]
Synonyms Pirimecidan, RP 4753, Pirimetamin
Molecular Weight 248.71
Formula C12H13ClN4
CAS No. 58-14-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 2.5 mg/mL (10 mM)

DMSO: 24.9 mg/mL (100 mM)

TargetMolReferences and Literature

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. 3. Ito S, et al. J Pharmacol Exp Ther, 2010, 333(1), 341-350.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Parasitic Compound Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Drug-induced Liver Injury (DILI) Compound Library Anti-Aging Compound Library Target-Focused Phenotypic Screening Library NO PAINS Compound Library FDA-Approved Drug Library Metabolism Compound Library

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Keywords

Pyrimethamine 58-14-0 Cell Cycle/Checkpoint DNA Damage/DNA Repair Metabolism Microbiology/Virology DHFR Antifolate Parasite Pirimecidan RP4753 folic–folinic acid systems parasites nucleoprotein metabolism inhibit cell division RP 4753 Pirimetamin Inhibitor RP-4753 antimalarial inhibitor

 

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