DHFR-IN-5

Names

[ CAS No. ]:
1142407-81-5

[ Name ]:
DHFR-IN-5

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Infection

[In Vitro]

DHFR-IN-5 (compound p218) 对 PYR 耐药性 P. falciparum 表现出较高的活性，对野生型 P. falciparum (TM4) 和 4 突变型 P. falciparum (V1/S) 的 IC50 值分别为 4.6, 56 nM[1]。

[In Vivo]

DHFR-IN-5 (compound p218) (30 mg/kg; p.o.) 在大鼠中表现出抗疟疾活性，具有良好的口服生物利用度 (46.3%), 合理的半衰期 (7.3 h)[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.  

Chemical & Physical Properties

[ Molecular Formula ]:
C18H24N4O4

[ Molecular Weight ]:
360.41

Related Compounds