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. |