WR99210

SKU: orb1218005

Description

WR99210 is effective against the most pyrimethamine-resistant Plasmodium falciparum strains. WR99210 is an effective inhibitor of dihydrofolate reductase (IC50:<0.075 nM).

Key Properties

• CAS Number: 47326-86-3
• MW: 394.68
• Purity: >98% (HPLC)
• Formula: C₁₄H₁₈Cl₃N₅O₂
• SMILES: CC1(N=C(N=C(N1OCCCOC2=C(C=C(C(Cl)=C2)Cl)Cl)N)N)C
• Target: DHFR
• Solubility: DMSO : 5 mg/mL (12.67 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  WR99210 (1.25 mg/kg; i.p.; single daily for 5 days) is highly effective against T. gondii tachyzoites in a mouse model. Animal model: Male mice (T. gondii-infected). Dosage: 1.25 mg/kg. Administration: Intraperitoneal injection; single daily for 5 days. Result: Exhibited intraperitoneal parasite numbers were 2 logs less in mice on the day 5.
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• In Vitro:
  WR99210 (0-100 nM; 92 h) is highly effective against T. gondii tachyzoites in tissue culture. WR99210 (0-100 nM; 92 h) shows low cytotoxicity to human foreskin fibroblasts. Cell Viability Assay Cell line: Human foreskin fibroblasts (T. gondii-infected) Concentration: 0-100 nM. Incubation time: 92 h. Result: Showed marked inhibition of T. gondii, with an IC50 value of approximately 50 nM. Cell Cytotoxicity Assay Cell line: Human foreskin fibroblasts. Concentration: 0-100 nM. Incubation time: 92 h. Result: Lacked of toxicity for fibroblasts.
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Storage & Handling

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

Quick Database Links

Gene Symbol

DHFR