Name | DHFR-IN-5 |
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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]. |
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Related Catalog | |
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 |
Molecular Formula | C18H24N4O4 |
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Molecular Weight | 360.41 |