WR99210 (C007B-433100)

WR99210 is an orally active and low-toxicity dihydrofolate reductase (DHFR) inhibitor ( IC 50 <0.075 nM). WR99210 shows good antiparasitic activity and is effective against P. falciparum and P. falciparum strains (including Pyrimethamine (HY-18062)-resistant P. falciparum strains) as well as T. gondiiIn VitroWR99210 (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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Human foreskin fibroblasts ( T. gondii -infected) Concentration: 0-100 nM Incubation Time: 92 h Result: Showed marked inhibition of T. gondii , with an IC 50 value of approximately 50 nM. Cell Cytotoxicity AssayCell Line: Human foreskin fibroblasts Concentration: 0-100 nM Incubation Time: 92 h Result: Lacked of toxicity for fibroblasts.In VivoWR99210 (1.25 mg/kg; i.p.; single daily for 5 days) is highly effective against T. gondii tachyzoites in a mouse model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.Form:SolidIC50& Target:IC50: <0.075 nM (DHFR).

Specifications and Purity: ≥98%

Molecular Formula: C14H18Cl3N5O2

Molecular Weight: 394.68

PubChem CID: 121750

Isomeric SMILES: CC1(N=C(N=C(N1OCCCOC2=CC(=C(C=C2Cl)Cl)Cl)N)N)C