| Identification | Back Directory | [Name]
Benzenepropanoic acid, 2-[3-[(2,4-diamino-6-ethyl-5-pyrimidinyl)oxy]propoxy]- | [CAS]
1142407-81-5 | [Synonyms]
DHFR-IN-5
Benzenepropanoic acid, 2-[3-[(2,4-diamino-6-ethyl-5-pyrimidinyl)oxy]propoxy]- | [Molecular Formula]
C18 H24 N4 O4 | [MOL File]
1142407-81-5.mol | [Molecular Weight]
360.41 |
| Hazard Information | Back Directory | [Uses]
DHFR-IN-5 is a potent and orally active dihydrofolate reductase (DHFR) inhibitor with a Ki value of 0.54 nM for quadruple mutant Plasmodium falciparum DHFR. DHFR-IN-5 shows anti-malaria activity[1]. | [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]. | 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. |
| [References]
[1] Yuthavong Y, et al. Malarial dihydrofolate reductase as a paradigm for drug development against a resistance-compromised target. Proc Natl Acad Sci U S A. 2012 Oct 16;109(42):16823-8. DOI:10.1073/pnas.1204556109 |
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