PeptideDB

DHFR-IN-5

CAS: 1142407-81-5 F: C18H24N4O4 W: 360.41

DHFR-IN-5 is a potent and orally active dihydrofolate reductase (DHFR) inhibitor with a Ki value of 0.54 nM for quadrupl
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Bioactivity 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].
Invitro 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:
Name DHFR-IN-5
CAS 1142407-81-5
Formula C18H24N4O4
Molar Mass 360.41
Transport Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Reference [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.