[CAS NO. 2120282-75-7] Fanotaprim
PRODUCTS SPECIFICATIONS [2120282-75-7]
DESCRIPTION [2120282-75-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 378.43 |
| Molecular Formula | C19H22N8O |
| SMILES | NC1=NC=C(N2CCN(C3=CC=CC(C4=CN=C(OC)N=C4)=C3)CC2)C(N)=N1 |
Summary
Fanotaprim is a dihydrofolate reductase (DHFR) inhibitor with IC 50 s of 1.57 and 308 nM for tg DHFR ( Toxoplasma gondii DHFR) and hDHFR (human DHFR), respectively. Fanotaprim has the potential for the research of toxoplasmosis [1] .
In Vitro
Fanotaprim shows parasiticidal and antiproliferative effects with EC
50
s of 13 and 7300 nM against the type I RH strain of
T. gondii
and MCF-7 cells, respectively
[1]
.
Fanotaprim shows ability to inhibit the growth of
T. gondii
strains in vitro with EC
50
s ranging 7.6~ 29.8 nM (GT1, ME49, CTG, RUB and VAND)
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Fanotaprim (1-10 mg/kg; p.o.; daily; beginning on day 1 through day 7) shows highly effective in control of acute infection by highly virulent strains of
T. gondii
in the murine model
[1]
.
Fanotaprim (1mg/kg; i.v; mouse) shows C
L
, V
d
, and t
1/2
values of 10.6 mL/min/kg, 1.14 L/kg, and 3.9 hours, respectively
[1]
.
Fanotaprim (0.83 mg/kg; p.o; mouse) shows F, C
max
, T
max
, and AUC
0-last
of 47.3%, 178 ng/mL, 0.05 hours and 750 ng h/mL, respectively
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | CD-1female mice (murine model of acute toxoplasmosis) [1] |
| Dosage: | 1-10 mg/kg |
| Administration: | p.o.; daily; beginning on day 1 through day 7 |
| Result: | Mice were monitored for survival for 30 days within termittent IVIS monitoring. At doses of 10 mg/kg Fanotaprim, q.d. or b.i.d. for 7 days, yielded 100% survival for 30 days. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 33.33 mg/mL ( 88.07 mM ; ultrasonic and warming and heat to 60°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.6425 mL | 13.2125 mL | 26.4250 mL |
| 5 mM | 0.5285 mL | 2.6425 mL | 5.2850 mL |
| 10 mM | 0.2642 mL | 1.3212 mL | 2.6425 mL |