Fanotaprim

SKU: orb1303929

Description

Fanotaprim is a potent and selective dihydrofolate reductase (DHFR) inhibitor, exhibiting strong activity against Toxoplasma gondii (TgDHFR IC50 = 1.57 nM) with high selectivity over human DHFR (196-fold). This makes it a valuable chemical tool for studying parasitic infections in both in vitro and in vivo experimental models.

Research Area

Cell Biology, Metabolism Research, Molecular Biology

Key Properties

• CAS Number: 2120282-75-7
• MW: 378.43
• Purity: 97.37% (May vary between batches)
• Formula: C₁₉H₂₂N₈O
• SMILES: COc1ncc(cn1)-c1cccc(c1)N1CCN(CC1)c1cnc(N)nc1N
• Target: Antifolate,DHFR
• Solubility: DMSO:25 mg/mL (66.06 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.28 mM)

Bioactivity

• Target IC50:
  TgDHFR:1.57 ± 0.11 nM(Toxoplasma gondii)|DHFR (human):308 ± 71 nM(human)
• In Vivo:
  Fanotaprim (1-10 mg/kg; p.o.; daily; beginning on day 1 through day 7) is highly effective in controlling acute infection by highly virulent strains of T. gondii in the murine model. In mice, Fanotaprim (1 mg/kg; i.v.) shows CL, Vd, and t1/2 values of 10.6 mL/min/kg, 1.14 L/kg, and 3.9 hours, respectively. When administered orally at 0.83 mg/kg, Fanotaprim exhibits F, Cmax, Tmax, and AUC0-last values of 47.3%, 178 ng/mL, 0.05 hours, and 750 ng h/mL, respectively.
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• In Vitro:
  Fanotaprim exhibits parasiticidal and antiproliferative effects with EC50s of 13 and 7300 nM against the type I RH strain of T. gondii and MCF-7 cells, respectively. It also inhibits the growth of T. gondii strains in vitro with EC50s ranging from 7.6 to 29.8 nM (GT1, ME49, CTG, RUB, and VAND).
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Storage & Handling

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

Alternative Names

toxoplasmosis, survival, VYR 006, VYR006, VYR-006, reductase, DHFR, dhydrofolate, CD-1, Antifolate, Fanotaprim, Inhibitor, inhibit, mice

Compound Identifiers

PubChem CID

134812633