Referencia número: HY-18062

Pyrimethamine

(Synonyms: Pirimecidan; Pirimetamin; RP 4753)

14 Cited Publications

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Based on 14 publication(s) in Google Scholar

Pyrimethamine (Pirimecidan) is a potent, orally active dihydrofolate reductase (DHFR) inhibitor. Pyrimethamine is an antimalarial agent. Pyrimethamine affects the nucleoprotein metabolism of malarial parasites by interference in the folic–folinic acid systems and affects cell division by inhibiting the conversion of dihydrofolate to tetrahydrofolate.

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Pureza: 99.99%
No. CAS: 58-14-0
Fòrmula: C₁₂H₁₃ClN₄
Peso molecular:248.71

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Pyrimethamine Chemical Structure

No. CAS: 58-14-0

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (14)
Solvente y solubilidad
- In Vitro
- In Vivo
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Actividad biológica

Descripciòn

IC₅₀ & Target

Plasmodium

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Cellular Effect

Cell Line	Type	Value	Description	References
BC	IC₅₀	>250 μM Compound: Pyr	Cytotoxicity against human breast cancer cells. Cytotoxicity against human breast cancer cells.	[PMID: 11881993]
BC	IC₅₀	40 μM Compound: Pyrimethamine (P1)	In vitro cytotoxicity against Plasmodium falciparum infected BC cell line. In vitro cytotoxicity against Plasmodium falciparum infected BC cell line.	[PMID: 14736247]
CHO	IC₅₀	271 μM Compound: PM	Cytotoxicity against CHO cells after 48 hrs by MTT assay Cytotoxicity against CHO cells after 48 hrs by MTT assay	[PMID: 24602791]
Erythrocyte	IC₅₀	0.004 μM Compound: Pyrimethamine	Antimalarial activity against chloroquine sensitive Plasmodium falciparum 3D7 infected in human RBC assessed as parasite growth inhibition incubated for 72 hrs by SYBR Green dye based fluorescence assay Antimalarial activity against chloroquine sensitive Plasmodium falciparum 3D7 infected in human RBC assessed as parasite growth inhibition incubated for 72 hrs by SYBR Green dye based fluorescence assay	[PMID: 36561069]
HEK293	IC₅₀	4.22 nM Compound: Pyrimethamine	Cytotoxicity against HEK293 cells assessed as cell viability after 72 hrs by resazurin-based plate reader analysis Cytotoxicity against HEK293 cells assessed as cell viability after 72 hrs by resazurin-based plate reader analysis	[PMID: 26651537]
HEK293	IC₅₀	8.07 nM Compound: Pyrimethamine	Cytotoxicity against HEK293 cells by alamar blue assay Cytotoxicity against HEK293 cells by alamar blue assay	[PMID: 27212070]
HEK293	IC₅₀	4.2 μM Compound: Pyrimethamine	Growth inhibition of HEK293 cells after 72 hrs by PrestoBlue staining based fluorescence assay Growth inhibition of HEK293 cells after 72 hrs by PrestoBlue staining based fluorescence assay	[PMID: 28001067]
HEK293	IC₅₀	13.57 μM Compound: Pyrimethamine	Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay	[PMID: 28230985]
HEK293	IC₅₀	0.69 μM Compound: Pyrimethamine	Cytotoxicity against HEK293 cells after 72 hrs by resazurin dye based assay Cytotoxicity against HEK293 cells after 72 hrs by resazurin dye based assay	[PMID: 29236492]
HEK293	CC₅₀	≥20 μM Compound: Pyrimethamine	Cytotoxicity against HEK293 cells after 72 hrs by resazurin dye based assay Cytotoxicity against HEK293 cells after 72 hrs by resazurin dye based assay	[PMID: 30537832]
HEK293	IC₅₀	4.2 μM Compound: Pyrimethamine	Cytotoxicity against HEK293 cells Cytotoxicity against HEK293 cells	[PMID: 32067457]
HEK293	IC₅₀	>10 μM Compound: Pyrimethamine	Cytotoxicity against HEK293 cells assessed as inhibition of cell growth incubated for 72 hrs by alamar blue dye based fluorescence assay Cytotoxicity against HEK293 cells assessed as inhibition of cell growth incubated for 72 hrs by alamar blue dye based fluorescence assay	[PMID: 36799121]
HEL	IC₅₀	0.67 μM Compound: Pyrimethamine	The ability to inhibit [3H]- uracil incorporation by Toxoplasma gondii in cultures of HEL cells was tested The ability to inhibit [3H]- uracil incorporation by Toxoplasma gondii in cultures of HEL cells was tested	[PMID: 10090784]
HEL	IC₅₀	0.7 μM Compound: Pyrimethamine	Antimicrobial activity against Toxoplasma gondii infected in HEL cells assessed as inhibition of parasite growth by [3H]uracil incorporation assay Antimicrobial activity against Toxoplasma gondii infected in HEL cells assessed as inhibition of parasite growth by [3H]uracil incorporation assay	[PMID: 20117005]
HeLa	EC₅₀	>100 μM Compound: 32	Antiviral activity against coxsackie B4 virus infected in human HeLa cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis Antiviral activity against coxsackie B4 virus infected in human HeLa cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis	[PMID: 28477572]
HeLa	EC₅₀	>100 μM Compound: 32	Antiviral activity against vesicular stomatitis virus infected in human HeLa cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis Antiviral activity against vesicular stomatitis virus infected in human HeLa cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis	[PMID: 28477572]
HeLa	EC₅₀	0.75 μM Compound: 32	Antiviral activity against Respiratory syncytial virus infected in human HeLa cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis Antiviral activity against Respiratory syncytial virus infected in human HeLa cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis	[PMID: 28477572]
HepG2	IC₅₀	30 μM Compound: Pyrimethamine	Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 19482476]
HepG2	CC₅₀	7.1 μM Compound: Pyrimethamine	Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 21741131]
HepG2	IC₅₀	1.03 μM Compound: 76	Antimalarial activity against liver stages of Plasmodium cynomolgi infected in human HepG2 cells assessed as growth inhibition of hepatic parasite after 3 days Antimalarial activity against liver stages of Plasmodium cynomolgi infected in human HepG2 cells assessed as growth inhibition of hepatic parasite after 3 days	[PMID: 22122518]
HepG2	IC₅₀	>10 μM Compound: 92125099	HARVARD: Cytotoxicity in HepG2 cell line HARVARD: Cytotoxicity in HepG2 cell line	[PMID: 22586124]
HepG2	IC₅₀	0.0047 μM Compound: 92125099	HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells	[PMID: 22586124]
HepG2	CC₅₀	7.1 μM Compound: Pyrimethamine	Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 22608675]
HepG2	IC₅₀	<1 μM Compound: Pyrimethamine	Antimalarial activity against sporozoite stage of Plasmodium yoelii assessed as invasion of human HepG2 cells expressing CD81 incubated for 2 hrs prior to inoculation measured after 1 hr by immunofluorescence assay in presence of penicillin/streptomycin Antimalarial activity against sporozoite stage of Plasmodium yoelii assessed as invasion of human HepG2 cells expressing CD81 incubated for 2 hrs prior to inoculation measured after 1 hr by immunofluorescence assay in presence of penicillin/streptomycin	[PMID: 23927658]
HFF	EC₅₀	0.21 μM Compound: Pyrimethamine	Antiparasitic activity against Toxoplasma gondii ATCC 50839 infected in HFF cells after 72 hrs by beta-galactosidase reporter gene assay Antiparasitic activity against Toxoplasma gondii ATCC 50839 infected in HFF cells after 72 hrs by beta-galactosidase reporter gene assay	[PMID: 17698618]
HFF	EC₅₀	0.24 μM Compound: Pyrimethamine	Antiparasitic activity against artemisinin-resistant Toxoplasma gondii STL500-10A infected in HFF cells after 72 hrs by beta-galactosidase reporter gene assay Antiparasitic activity against artemisinin-resistant Toxoplasma gondii STL500-10A infected in HFF cells after 72 hrs by beta-galactosidase reporter gene assay	[PMID: 17698618]
HFF	EC₅₀	0.27 μM Compound: Pyrimethamine	Antiparasitic activity against artemisinin-resistant Toxoplasma gondii KN200-6 infected in HFF cells after 72 hrs by beta-galactosidase reporter gene assay Antiparasitic activity against artemisinin-resistant Toxoplasma gondii KN200-6 infected in HFF cells after 72 hrs by beta-galactosidase reporter gene assay	[PMID: 17698618]
HFF	EC₅₀	0.29 μM Compound: Pyrimethamine	Antiparasitic activity against artemisinin-resistant Toxoplasma gondii KN200-1 infected in HFF cells after 72 hrs by beta-galactosidase reporter gene assay Antiparasitic activity against artemisinin-resistant Toxoplasma gondii KN200-1 infected in HFF cells after 72 hrs by beta-galactosidase reporter gene assay	[PMID: 17698618]
HFF	CC₅₀	>50 μM Compound: Pyrimethamine	Cytotoxicity against human HFF cells after 72 hrs by MTT assay Cytotoxicity against human HFF cells after 72 hrs by MTT assay	[PMID: 21741131]
HFF	IC₅₀	1.1 μM Compound: Pyrimethamine	Antiparasitic activity against Toxoplasma gondii PRU tachyzoites harboring beta-Gal gene infected in human HFF cells after 72 hrs by microtiter plate based assay Antiparasitic activity against Toxoplasma gondii PRU tachyzoites harboring beta-Gal gene infected in human HFF cells after 72 hrs by microtiter plate based assay	[PMID: 21741131]
HFF	IC₅₀	0.8 μM Compound: Pyrimethamine	Antitoxoplasmic activity against Toxoplasma gondii PRU tachyzoites infected in human HFF cells assessed as beta-galactosidase activity after 72 hrs by colorimetric assay Antitoxoplasmic activity against Toxoplasma gondii PRU tachyzoites infected in human HFF cells assessed as beta-galactosidase activity after 72 hrs by colorimetric assay	[PMID: 22608675]
HFF	CC₅₀	>50 μM Compound: Pyrimethamine	Cytotoxicity against HFF assessed as cell proliferation after 96 hrs by alamar blue reduction assay Cytotoxicity against HFF assessed as cell proliferation after 96 hrs by alamar blue reduction assay	[PMID: 26479029]
Huh-7	CC₅₀	45.62 μM Compound: GNF-Pf-5586	NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7) NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)	[PMID: 18579783]
K562	IC₅₀	5 μM Compound: Pyrimethamine	Cytotoxicity against human K562 cells after 72 hrs by flow cytometry Cytotoxicity against human K562 cells after 72 hrs by flow cytometry	[PMID: 19482476]
KB	IC₅₀	109 μM Compound: Pyr	Cytotoxicity against human epidermoid carcinoma KB cell. Cytotoxicity against human epidermoid carcinoma KB cell.	[PMID: 11881993]
KB	IC₅₀	109 μM Compound: Pyrimethamine (P1)	In vitro cytotoxicity against Plasmodium falciparum infected KB cell line In vitro cytotoxicity against Plasmodium falciparum infected KB cell line	[PMID: 14736247]
MCF7	EC₅₀	11700 nM Compound: 1	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 30624926]
MCF7	IC₅₀	453 μM Compound: PYM	Antiproliferative activity in human MCF7 cells assessed as inhibition of cell viability after 72 hrs by MTS assay Antiproliferative activity in human MCF7 cells assessed as inhibition of cell viability after 72 hrs by MTS assay	[PMID: 32061484]
MDA-MB-231	IC₅₀	238 μM Compound: PYM	Antiproliferative activity in human MDA-MB-231 cells assessed as inhibition of cell viability after 72 hrs by MTS assay Antiproliferative activity in human MDA-MB-231 cells assessed as inhibition of cell viability after 72 hrs by MTS assay	[PMID: 32061484]
MDCK	CC₅₀	41 μM Compound: 32	Cytotoxicity against dog MDCK cells assessed as reduction in cell viability measured after 5 to 6 days by MTS assay Cytotoxicity against dog MDCK cells assessed as reduction in cell viability measured after 5 to 6 days by MTS assay	[PMID: 28477572]
MRC5	IC₅₀	0.07 mg/L Compound: Pyrimethamine	Antimicrobial activity against Toxoplasma gondii isolate RMS-1994-LEF harboring DHPS Ex2, E474D/Ex4, R560K/Ex5, 580 sil Gly; A597E/627 sil Glu mutant gene and DHFR Ex3, 204 sil Ala mutant gene infected in human MRC-5 cells after 72 hrs by ELISA Antimicrobial activity against Toxoplasma gondii isolate RMS-1994-LEF harboring DHPS Ex2, E474D/Ex4, R560K/Ex5, 580 sil Gly; A597E/627 sil Glu mutant gene and DHFR Ex3, 204 sil Ala mutant gene infected in human MRC-5 cells after 72 hrs by ELISA	[PMID: 18212105]
MRC5	IC₅₀	0.09 mg/L Compound: Pyrimethamine	Antimicrobial activity against Toxoplasma gondii isolate RMS-2003-DJO infected in human MRC-5 cells after 72 hrs by ELISA Antimicrobial activity against Toxoplasma gondii isolate RMS-2003-DJO infected in human MRC-5 cells after 72 hrs by ELISA	[PMID: 18212105]
MRC5	IC₅₀	0.09 mg/L Compound: Pyrimethamine	Antimicrobial activity against Toxoplasma gondii ME49 infected in human MRC-5 cells infected in human MRC-5 cells after 72 hrs by ELISA Antimicrobial activity against Toxoplasma gondii ME49 infected in human MRC-5 cells infected in human MRC-5 cells after 72 hrs by ELISA	[PMID: 18212105]
MRC5	IC₅₀	0.1 mg/L Compound: Pyrimethamine	Antimicrobial activity against Toxoplasma gondii RH harboring DHPS Ex2, E474D/Ex4, R560K/Ex5, 580 sil Gly; A597E/627 sil Glu mutant gene and DHFR Ex3, 156 sil Leu mutant gene infected in human MRC-5 cells after 72 hrs by ELISA Antimicrobial activity against Toxoplasma gondii RH harboring DHPS Ex2, E474D/Ex4, R560K/Ex5, 580 sil Gly; A597E/627 sil Glu mutant gene and DHFR Ex3, 156 sil Leu mutant gene infected in human MRC-5 cells after 72 hrs by ELISA	[PMID: 18212105]
MRC5	IC₅₀	0.11 mg/L Compound: Pyrimethamine	Antimicrobial activity against Toxoplasma gondii isolate GRE-1995-MAE infected in human MRC-5 cells after 72 hrs by ELISA Antimicrobial activity against Toxoplasma gondii isolate GRE-1995-MAE infected in human MRC-5 cells after 72 hrs by ELISA	[PMID: 18212105]
MRC5	IC₅₀	0.11 mg/L Compound: Pyrimethamine	Antimicrobial activity against Toxoplasma gondii isolate RMS-2005-HAG infected in human MRC-5 cells after 72 hrs by ELISA Antimicrobial activity against Toxoplasma gondii isolate RMS-2005-HAG infected in human MRC-5 cells after 72 hrs by ELISA	[PMID: 18212105]
MRC5	IC₅₀	0.12 mg/L Compound: Pyrimethamine	Antimicrobial activity against Toxoplasma gondii isolate RMS-2001-MAU infected in human MRC-5 cells after 72 hrs by ELISA Antimicrobial activity against Toxoplasma gondii isolate RMS-2001-MAU infected in human MRC-5 cells after 72 hrs by ELISA	[PMID: 18212105]
MRC5	IC₅₀	0.14 mg/L Compound: Pyrimethamine	Antimicrobial activity against Toxoplasma gondii isolate PSP-2005-MUP infected in human MRC-5 cells after 72 hrs by ELISA Antimicrobial activity against Toxoplasma gondii isolate PSP-2005-MUP infected in human MRC-5 cells after 72 hrs by ELISA	[PMID: 18212105]
MRC5	IC₅₀	0.15 mg/L Compound: Pyrimethamine	Antimicrobial activity against Toxoplasma gondii isolate TOU-1998-TRI infected in human MRC-5 cells after 72 hrs by ELISA Antimicrobial activity against Toxoplasma gondii isolate TOU-1998-TRI infected in human MRC-5 cells after 72 hrs by ELISA	[PMID: 18212105]
MRC5	IC₅₀	0.17 mg/L Compound: Pyrimethamine	Antimicrobial activity against Toxoplasma gondii isolate RMS-1995-ABE harboring DHPS Ex5, A587V mutant gene infected in human MRC-5 cells after 72 hrs by ELISA Antimicrobial activity against Toxoplasma gondii isolate RMS-1995-ABE harboring DHPS Ex5, A587V mutant gene infected in human MRC-5 cells after 72 hrs by ELISA	[PMID: 18212105]
MRC5	IC₅₀	0.18 mg/L Compound: Pyrimethamine	Antimicrobial activity against Toxoplasma gondii isolate TRS-2004-REV infected in human MRC-5 cells after 72 hrs by ELISA Antimicrobial activity against Toxoplasma gondii isolate TRS-2004-REV infected in human MRC-5 cells after 72 hrs by ELISA	[PMID: 18212105]
MRC5	IC₅₀	0.19 mg/L Compound: Pyrimethamine	Antimicrobial activity against Toxoplasma gondii NED infected in human MRC-5 cells after 72 hrs by ELISA Antimicrobial activity against Toxoplasma gondii NED infected in human MRC-5 cells after 72 hrs by ELISA	[PMID: 18212105]
MRC5	IC₅₀	0.25 mg/L Compound: Pyrimethamine	Antimicrobial activity against Toxoplasma gondii isolate GUY-2003-MEL harboring DHPS Ex2, E474D/Ex4, R560K/Ex5, 580 sil Gly/ A597E/627 sil Glu mutant gene and DHFR Ex2, 145 sil Val mutant gene infected in human MRC-5 cells after 72 hrs by ELISA Antimicrobial activity against Toxoplasma gondii isolate GUY-2003-MEL harboring DHPS Ex2, E474D/Ex4, R560K/Ex5, 580 sil Gly/ A597E/627 sil Glu mutant gene and DHFR Ex2, 145 sil Val mutant gene infected in human MRC-5 cells after 72 hrs by ELISA	[PMID: 18212105]
MRC5	IC₅₀	0.34 mg/L Compound: Pyrimethamine	Antimicrobial activity against Toxoplasma gondii ENT harboring DHPS Ex2, E474D/Ex3, 156 sil Leu/Ex4, R560K/Ex5, 580 sil Gly/A597E/627 sil Glu mutant gene and DHFR Ex3, 156 sil Leu mutant gene infected in human MRC-5 cells after 72 hrs by ELISA Antimicrobial activity against Toxoplasma gondii ENT harboring DHPS Ex2, E474D/Ex3, 156 sil Leu/Ex4, R560K/Ex5, 580 sil Gly/A597E/627 sil Glu mutant gene and DHFR Ex3, 156 sil Leu mutant gene infected in human MRC-5 cells after 72 hrs by ELISA	[PMID: 18212105]
MRC5	IC₅₀	0.35 mg/L Compound: Pyrimethamine	Antimicrobial activity against Toxoplasma gondii B1 harboring DHPS Ex2, E474D/Ex4, R560K/Ex5, 580 sil Gly/ A597E/627 sil Glu mutant gene and DHFR Ex3, 156 sil Leu mutant gene infected in human MRC-5 cells after 72 hrs by ELISA Antimicrobial activity against Toxoplasma gondii B1 harboring DHPS Ex2, E474D/Ex4, R560K/Ex5, 580 sil Gly/ A597E/627 sil Glu mutant gene and DHFR Ex3, 156 sil Leu mutant gene infected in human MRC-5 cells after 72 hrs by ELISA	[PMID: 18212105]
MRC5	IC₅₀	0.39 mg/L Compound: Pyrimethamine	Antimicrobial activity against Toxoplasma gondii isolate GRE-1998-TRA infected in human MRC-5 cells after 72 hrs by ELISA Antimicrobial activity against Toxoplasma gondii isolate GRE-1998-TRA infected in human MRC-5 cells after 72 hrs by ELISA	[PMID: 18212105]
MRC5	ED₅₀	16.23 μg/mL Compound: 1	Cytotoxicity against human MRC5 cells after 72 hrs by Alamar blue assay Cytotoxicity against human MRC5 cells after 72 hrs by Alamar blue assay	[PMID: 21126022]
MRC5	ED₅₀	16.2 μg/mL Compound: PYR	Toxicity against human MRC5 cells assessed as growth inhibition Toxicity against human MRC5 cells assessed as growth inhibition	[PMID: 22946585]
Vero	IC₅₀	32 μM Compound: Pyr	Cytotoxicity by the selective inhibition against African green monkey kidney fibroblast (vero cells). Cytotoxicity by the selective inhibition against African green monkey kidney fibroblast (vero cells).	[PMID: 11881993]
Vero	IC₅₀	32 μM Compound: Pyrimethamine (P1)	In vitro cytotoxicity against Plasmodium falciparum infected vero cell line. In vitro cytotoxicity against Plasmodium falciparum infected vero cell line.	[PMID: 14736247]
Vero	IC₅₀	>62.5 μg/mL Compound: Pyrimethamine	Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay	[PMID: 23352268]
Vero	IC₅₀	18.2 μM Compound: 2	Cytotoxicity against african green monkey Vero cells after 48 hrs by neutral red assay Cytotoxicity against african green monkey Vero cells after 48 hrs by neutral red assay	[PMID: 24900509]
Vero	CC₅₀	122 μM Compound: Pyr	Cytotoxicity against African green monkey Vero cells after 24 hrs by MTT assay Cytotoxicity against African green monkey Vero cells after 24 hrs by MTT assay	[PMID: 25899334]
Vero	EC₅₀	>100 μM Compound: 32	Antiviral activity against Punta Toro virus infected in African green monkey Vero cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis Antiviral activity against Punta Toro virus infected in African green monkey Vero cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis	[PMID: 28477572]
Vero	EC₅₀	>100 μM Compound: 32	Antiviral activity against Yellow fever virus infected in African green monkey Vero cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis Antiviral activity against Yellow fever virus infected in African green monkey Vero cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis	[PMID: 28477572]
Vero	EC₅₀	20 μM Compound: 32	Antiviral activity against para influenza 3 virus infected in African green monkey Vero cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis Antiviral activity against para influenza 3 virus infected in African green monkey Vero cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis	[PMID: 28477572]
Vero	EC₅₀	46 μM Compound: 32	Antiviral activity against Coxsackie B4 virus infected in African green monkey Vero cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis Antiviral activity against Coxsackie B4 virus infected in African green monkey Vero cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis	[PMID: 28477572]
Vero	EC₅₀	5.4 μM Compound: 32	Antiviral activity against Reovirus 1 infected in African green monkey Vero cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis Antiviral activity against Reovirus 1 infected in African green monkey Vero cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis	[PMID: 28477572]
Vero	EC₅₀	8.9 μM Compound: 32	Antiviral activity against Sindbis virus infected in African green monkey Vero cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis Antiviral activity against Sindbis virus infected in African green monkey Vero cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis	[PMID: 28477572]
Vero	IC₅₀	>6.25 μg/mL Compound: Pyrimethamine	Cytotoxicity against monkey Vero cells assessed as decrease in cell viability after 72 hrs by MTT assay Cytotoxicity against monkey Vero cells assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 28552337]
Vero	IC₅₀	32 μM Compound: PYR	Cytotoxicity against African green monkey Vero cells by sulforhodamine B assay Cytotoxicity against African green monkey Vero cells by sulforhodamine B assay	[PMID: 31685330]
Vero	CC₅₀	18.12 μM Compound: Pyrimethamine	Cytotoxicity against African green monkey Vero cells Cytotoxicity against African green monkey Vero cells	[PMID: 37163950]

In Vitro

Pyrimethamine (Pirimecidan; 4 nM-4 μM; 24 h; LLC-MK2 cells with T. gondii) combination of Fluconazole (FLZ) (HY-B0101) inhibits T. gondii activity with IC₅₀ values of 0.23, 0.19, 0.23, 0.34, 0.14, and 0.19 μM for FLZ concentration at 0, 0.05, 0.1, 0.5, 1.0, and 3.0 μM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

LLC-MK2 cells with T. gondii
Concentration:

4 nM-4 μM
Incubation Time:

24 hours
Result:

Inhibited T. gondii activity and decreased parasite proliferation index.

In Vivo

Pyrimethamine (Pirimecidan; 1 mg/kg; i.g.; daily, for 10 d; female CF1 mice with T. gondii xenograft) combination of Fluconazole (HY-B0101) and Sulfadiazine (HY-B0273) increases protection from death^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female CF1 mice (18-22 g; 4-6 week of age) with T. gondii xenograft^[1]
Dosage:

Oral gavage; daily, for 10 days
Administration:

1 mg/kg; 10 mg/kg (Fluconazole (HY-B0101)), 40 mg/kg (Sulfadiazine (HY-B0273))
Result:

Increased mouse survival compared to treatment with SDZ/PYR alone.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 58-14-0
Appearance Solid
Peso molecular 248.71
Fòrmula C₁₂H₁₃ClN₄
Color White to off-white
SMILES

NC1=NC(N)=C(C2=CC=C(Cl)C=C2)C(CC)=N1
Synonyms

Pirimecidan; Pirimetamin; RP 4753
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (14)

All Cell Proliferation/Viability AssayIF

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Journal Impact Factor

EMBO Mol Med

A novel model of glioblastoma recurrence to identify therapeutic vulnerabilities. [Abstract]

2025 Jun;17(6):1325-1354. PMID: 40295888

Pyrimethamine purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2025 Jun;17(6):1325-1354. [Abstract]

Cell viability assay of patient-derived GICs and GICRs, treated with increasing concentrations of Pyrimethamine.
Biomolecules

Activity Evaluation and Mode of Action of ICA Against Toxoplasma gondii In Vitro. [Abstract]

2025 Feb 1;15(2):202. PMID: 40001505

Pyrimethamine purchased from MedChemExpress. Usage Cited in: Biomolecules. 2025 Feb 1;15(2):202. [Abstract]

Antiproliferative effect of Pyrimethamine (PYR: 10 μM) on intracellular Toxoplasma gondii, cellular immunofluorescence image.
J Mol Med (Berl)

Combination of PARP inhibitor and temozolomide to suppress chordoma progression. [Abstract]

2019 Aug;97(8):1183-1193. PMID: 31201471
Int J Antimicrob Agents

Efficacy of antiretroviral compounds against Toxoplasma gondii in vitro. [Abstract]

2019 Dec;54(6):814-819. PMID: 31479744
J Lipid Res

Toxoplasma gondii sustains survival by regulating cholesterol biosynthesis and uptake via SREBP2 activation. [Abstract]

2024 Oct 25:100684. PMID: 39490926

Pyrimethamine purchased from MedChemExpress. Usage Cited in: J Lipid Res. 2024 Oct 25:100684. [Abstract]

H-RFP were cultured in the presence of AY9944 (5 μM) or Pyrimethamine (PYR: 10 μM) in 96-well plates for 24 h.
ACS Infect Dis

Integral Solvent-Induced Protein Precipitation for Target-Engagement Studies in Plasmodium falciparum. [Abstract]

2024 Dec 13;10(12):4073-4086. PMID: 39631773
Drug Metab Dispos

Identification of selective substrates and inhibitors of the major human renal uptake transporters. [Abstract]

2025 Mar;53(3):100046. PMID: 40024137
PLoS Negl Trop Dis

Identification of anti-flaviviral drugs with mosquitocidal and anti-Zika virus activity in Aedes aegypti. [Abstract]

2019 Aug 20;13(8):e0007681. PMID: 31430351
Mol Carcinog

Pyroptosis-related gene GSDMC indicates poor prognosis and promotes tumor progression by activating the AKT/mTOR pathway in lung squamous cell carcinoma. [Abstract]

2024 Nov;63(11):2218-2236. PMID: 39136610
J Appl Toxicol

Inhibitory effect of flavonoids on multidrug and toxin extrusion protein 1 function: Implications for food/herb-drug interaction and drug-induced kidney injury. [Abstract]

2024 May 17. PMID: 38760888
J Oral Pathol Med

Pyrimethamine Triggers the Apoptotic Pathway in Mucoepidermoid Carcinoma in Cell-Based Models. [Abstract]

2025 Aug 6. PMID: 40765495
bioRxiv

Cortisol Drives Pregnancy-Associated Induction of Hepatic OAT2, NTCP, and OCT1 in HepaRG cells Through GR-, HNF1α-, and HNF4α-Dependent Signaling. [Abstract]

2026 Jun 19:2026.06.15.732466. PMID: 42367899
Pathog Dis

Pyp25α is required for male gametocyte exflagellation. [Abstract]

2022 Nov 12;80(1):ftac043. PMID: 36316012
Research Square Preprint

2022 Jun.

Solvente y solubilidad

In Vitro:

DMSO : 20 mg/mL (80.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.0207 mL

20.1037 mL

40.2075 mL

5 mM

0.8041 mL

4.0207 mL

8.0415 mL

10 mM

0.4021 mL

2.0104 mL

4.0207 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (10.05 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (10.05 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% PBS

Solubility: 25 mg/mL (100.52 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (278 KB)
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Aikawa M, et, al. Studies on nuclear division of a malarial parasite under pyrimethamine treatment. J Cell Biol. 1968 Dec;39(3):749-54. [Content Brief]

[2]. Martins-Duarte ÉS, et, al. Toxoplasma gondii: the effect of fluconazole combined with sulfadiazine and pyrimethamine against acute toxoplasmosis in murine model. Exp Parasitol. 2013 Mar;133(3):294-9. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	4.0207 mL	20.1037 mL	40.2075 mL	100.5187 mL
	5 mM	0.8041 mL	4.0207 mL	8.0415 mL	20.1037 mL
	10 mM	0.4021 mL	2.0104 mL	4.0207 mL	10.0519 mL
	15 mM	0.2680 mL	1.3402 mL	2.6805 mL	6.7012 mL
	20 mM	0.2010 mL	1.0052 mL	2.0104 mL	5.0259 mL
	25 mM	0.1608 mL	0.8041 mL	1.6083 mL	4.0207 mL
	30 mM	0.1340 mL	0.6701 mL	1.3402 mL	3.3506 mL
	40 mM	0.1005 mL	0.5026 mL	1.0052 mL	2.5130 mL
	50 mM	0.0804 mL	0.4021 mL	0.8041 mL	2.0104 mL
	60 mM	0.0670 mL	0.3351 mL	0.6701 mL	1.6753 mL
	80 mM	0.0503 mL	0.2513 mL	0.5026 mL	1.2565 mL

Keywords

Pyrimethamine

14 Cited Publications

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Pyrimethamine

Anti-Infection Compound Library

Cell Cycle/DNA Damage Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Drug-Induced Liver Injury (DILI) Compound Library

Antiparasitic Compound library

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FDA-Approved Anticancer Drug Library

Human Metabolite Library

Heterocyclic Compound Library

Off-patent Drug Library

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FDA-Approved Drug Library Plus

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Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Nephrotoxicity Compound Library

Publications Citing Use of MedChemExpress (MCE) Pyrimethamine

Ver todos los productos específicos de isoformas Parasite

Actividad biológica

Chemical Information

Publications (14)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Pyrimethamine

Anti-Infection Compound Library

Cell Cycle/DNA Damage Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Drug-Induced Liver Injury (DILI) Compound Library

Antiparasitic Compound library

Anti-Cancer Metabolism Compound Library

Rare Diseases Drug Library

Pediatric Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Heterocyclic Compound Library

Off-patent Drug Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Nephrotoxicity Compound Library

Publications Citing Use of MedChemExpress (MCE) Pyrimethamine

Ver todos los productos específicos de isoformas Parasite

Actividad biológica

Chemical Information

Publications (14)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Pyrimethamine Related Classifications

HY-18062 Related Classifications