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    Pyrimethamine
    Pyrimethamine

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0849
    CAS #: 58-14-0Purity ≥98%

    Description: Pyrimethamine (Pirimecidan; Pirimetamin; RP 4753) is a potent dihydrofolate reductase (DHFR) inhibitor which is used as an antimalarial and antiprotozoal drug. 

    References: J Biol Chem. 2007 Mar 23;282(12):9150-61; J Am Coll Cardiol. 2002 Aug 21;40(4):803-10.

    Related CAS #: 14720-95-7 (isethionate); 19085-09-7 (HCl); 7681-25-6 (phosphate); 58-14-0 (free base); 53640-38-3 (sulfate);


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    Molecular Weight (MW)248.71
    FormulaC12H13ClN4
    CAS No.58-14-0
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 10 mg/mL (40.2 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other info

    Chemical Name: 5-(4-chlorophenyl)-6-ethylpyrimidine-2,4-diamine

    InChi Key: WKSAUQYGYAYLPV-UHFFFAOYSA-N

    InChi Code: InChI=1S/C12H13ClN4/c1-2-9-10(11(14)17-12(15)16-9)7-3-5-8(13)6-4-7/h3-6H,2H2,1H3,(H4,14,15,16,17)

    SMILES Code: CCC1=C(C(=NC(=N1)N)N)C2=CC=C(C=C2)Cl

    SynonymsMalocid; Khloridin; BW 50-63; BW-50-63; BW50-63; Pyrimethamine; Daraprim; NCI-C01683; NSC 3061; Tindurin; WR 297; Chloridine; Ethylpyrimidine; Aventis Brand of Pyrimethamine; Chloridin; Daraprim; Glaxo Wellcome Brand of Pyrimethamine; GlaxoSmithKline Brand of Pyrimethamine; Pirimecidan; Malocide; Pirimetamin; RP 4753; Pyrimethamine; Tindurine; Wellcome Brand of Pyrimethamine;


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    In Vitro

    In vitro activity: 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. Pyrimethamine-sulfadoxine is an inhibitor of dihydrofolate reductase(DHFR) that has been widely used to treat chloroquine-resistant Plasmodium falciparum malaria. 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+.


    Cell Assay: In a PC12 cell-based assay, no compounds reduced SOD1 promoter activity without concomitant cytotoxicity. Additionally,pyrimethamine failed to repress levels of SOD1 protein in HeLa cells or homogenates of liver, spinal cord and brain of wild-type mice.

    In Vivo(131)I-Pyrimethamine (specific activity: 7.08 MBq/ mol) was injected intravenously into the tail vein of the control and infected rats. Static whole body images of the rats were acquired under the gamma camera at 5 min, 45 min, 2 h, 6 h, and 24 h following the intravenous administration of the radioactivity (3.7 MBq/rat). The 10-day treatment with 10mg/kg/day of fluconazole combined with 40/1mg/kg/day sulfadiazine and pyrimethamine resulted in 93% survival of CF1 mice acutely infected with the highly virulent T. gondii RH strain, versus 36% of mice treated with just sulfadiazine and pyrimethamine
    Animal modelRats
    Formulation & Dosage7.08 MBq/ mol; i.v.
    References

    J Biol Chem. 2007 Mar 23;282(12):9150-61; J Am Coll Cardiol. 2002 Aug 21;40(4):803-10.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Pyrimethamine
    PYR enhances Hex A enzyme levels in some TSD patient cell lines. J Biol Chem. 2007 Mar 23;282(12):9150-61.
     
    Pyrimethamine
    TSD or α-mutants cell lines which responded to PYR and NGT. J Biol Chem. 2007 Mar 23;282(12):9150-61.


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