[CAS NO. 1142407-81-5] DHFR-IN-5
PRODUCTS SPECIFICATIONS [1142407-81-5]
DESCRIPTION [1142407-81-5]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 360.41 |
| Molecular Formula | C18H24N4O4 |
| SMILES | O=C(CCC1=C(OCCCOC2=C(CC)N=C(N)N=C2N)C=CC=C1)O |
Summary
DHFR-IN-5 is a potent and orally active dihydrofolate reductase (DHFR) inhibitor with a K i value of 0.54 nM for quadruple mutant Plasmodium falciparum DHFR. DHFR-IN-5 shows anti-malaria activity [1] .
In Vitro
DHFR-IN-5 (compound p218) shows highly active against PYR-resistant P. falciparum with IC 50 s of 4.6, 56 nM for wild-type P. falciparum (TM4), quadruple mutant P. falciparum (V1/S), respectively [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
DHFR-IN-5 (compound p218) (30 mg/kg; p.o.) shows anti-malaria activity with good oral bioavailability (46.3%), a reasonable half-life (7.3 h) in rats [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Rats [1] |
| Dosage: | 30 mg/kg |
| Administration: | P.o. |
| Result: | Showed good oral bioavailability (46.3%), a reasonable half-life (7.3 h), and minimal distribution into the brain. |
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.