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Pyrimethamine

Catalog No. T0849 CAS 58-14-0

Synonyms: 乙胺嘧啶, RP 4753, Pirimetamin, Pirimecidan

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

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Pyrimethamine, CAS 58-14-0

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Pyrimethamine 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	乙胺嘧啶, RP 4753, Pirimetamin, Pirimecidan
Molecular Weight	248.71
Formula	C12H13ClN4
CAS No.	58-14-0

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

Ethanol: 2.5 mg/mL (10 mM)

DMSO: 24.9 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References 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-Cancer Compound Library Anti-Cancer Metabolism Compound Library Inhibitor Library DNA Damage & Repair Compound Library Immunology/Inflammation Compound Library Anti-Metabolism Disease Compound Library Cell Cycle Compound Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library FDA-Approved Drug Library

Related Products

Related compounds with same targets

Metoprine Aminopterin Calcium N5-methyltetrahydrofolate Levomefolate calcium Pemetrexed disodium hemipenta hydrate Pralatrexate Proguanil hydrochloride Diaveridine

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Keywords

Pyrimethamine 58-14-0 DNA损伤和修复代谢微生物学细胞周期 Antifolate DHFR Parasite Pirimecidan folic–folinic acid systems Pirimetamin parasites nucleoprotein metabolism RP-4753 inhibit cell division RP4753 RP 4753 Inhibitor antimalarial inhibitor

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