Pyrimethamine

SKU: orb1224596

Description

A synthetic derivative of ethyl-pyrimidine with potent antimalarial properties; interferes with the regeneration of tetrahydrofolic acid from dihydrofolate by competitively inhibiting DHFR; has also been found to reduce the expression of SOD1.Parasite Infection Approved(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.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 58-14-0
• MW: 248.7114
• Purity: >98% (HPLC)
• Formula: C₁₂H₁₃ClN₄
• SMILES: CCC1=C(C(=NC(=N1)N)N)C2=CC=C(C=C2)Cl
• Target: Parasite
• Solubility: 10 mM in DMSO

Bioactivity

• 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. Animal model: Female CF1 mice (18-22 g; 4-6 week of age) with T. gondii xenograft. 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.
• 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. Cell Viability Assay 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Pirimecidan | Pirimetamin | RP 4753

Quick Database Links

Gene Symbol

Parasite