1142407-81-5

1142407-81-5 structure
1142407-81-5 structure
  • Name: DHFR-IN-5
  • Chemical Name: DHFR-IN-5
  • CAS Number: 1142407-81-5
  • Molecular Formula: C18H24N4O4
  • Molecular Weight: 360.41
  • Catalog: Research Areas Infection
  • Create Date: 2023-06-24 14:47:57
  • Modify Date: 2024-01-21 21:44:59
  • 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].

Name DHFR-IN-5
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
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.  

Molecular Formula C18H24N4O4
Molecular Weight 360.41
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