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Pyrimethamine

Pyrimethamine
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Purity:99.74%
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Pyrimethamine

Catalog No. T0849Cas No. 58-14-0
Pyrimethamine (Pirimecidan) is a competitive inhibitor of dihydrofolate reductase (DHFR), used as an antimalarial drug.
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Pack SizePriceAvailabilityQuantity
50 mg$38In Stock
100 mg$52In Stock
200 mg$78In Stock
1 mL x 10 mM (in DMSO)$50In Stock
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Product Introduction

Bioactivity
Description
Pyrimethamine (Pirimecidan) is a competitive inhibitor of dihydrofolate reductase (DHFR), used as an antimalarial drug.
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]
AliasPirimecidan, RP 4753, Pirimetamin
Chemical Properties
Molecular Weight248.71
FormulaC12H13ClN4
Cas No.58-14-0
Storage & Solubility Information
StoragePowder: -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)
Solution Preparation Table
DMSO/Ethanol
1mg5mg10mg50mg
1 mM4.0207 mL20.1037 mL40.2075 mL201.0374 mL
5 mM0.8041 mL4.0207 mL8.0415 mL40.2075 mL
DMSO
1mg5mg10mg50mg
10 mM0.4021 mL2.0104 mL4.0207 mL20.1037 mL
20 mM0.2010 mL1.0052 mL2.0104 mL10.0519 mL
50 mM0.0804 mL0.4021 mL0.8041 mL4.0207 mL
100 mM0.0402 mL0.2010 mL0.4021 mL2.0104 mL

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