Pyrimethamine

Catalog No.S2006

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

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Pyrimethamine Chemical Structure

Pyrimethamine Chemical Structure
Molecular Weight: 248.71

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Pyrimethamine is available in the following compound libraries:

Product Information

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Product Description

Biological Activity

Description Pyrimethamine is a dihydrofolate reductase (DHFR) inhibitor, used as an antimalarial drug.
Targets DHFR [1]
IC50 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]
In vivo
Features

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[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.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2015-08-29)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02527005 Not yet recruiting Malaria|Pregnant|HIV University of Ibadan September 2015 Phase 1
NCT02524444 Not yet recruiting Malaria in Pregnant HIV + Patients ORIYOMI OMOTOYOSI AKINYOTU|University of Ibadan September 2015 Phase 1
NCT02511054 Recruiting Malaria National Institute of Allergy and Infectious Diseases (NI  ...more National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC) July 2015 Phase 1
NCT02211729 Not yet recruiting Malaria|Respiratory Infections London School of Hygiene and Tropical Medicine|Malaria Re  ...more London School of Hygiene and Tropical Medicine|Malaria Research and Training Center, Bamako, Mali|Institut de Recherche en Sciences de la Sante, Burkina Faso August 2014 Phase 3
NCT02163447 Active, not recruiting Malaria University of California, San Francisco|Eunice Kennedy Sh  ...more University of California, San Francisco|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) June 2014 Phase 3

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Chemical Information

Download Pyrimethamine SDF
Molecular Weight (MW) 248.71
Formula

C12H13ClN4

CAS No. 58-14-0
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 10 mg/mL (40.2 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 5-​(4-​chlorophenyl)​-​6-​ethyl-2,​4-​pyrimidinediamine

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