1. Metabolic Enzyme/Protease
  2. Dihydrofolate reductase (DHFR)
  3. DHFR-IN-5

DHFR-IN-5 是一种有效且具有口服活性的二氢叶酸还原酶 (DHFR) 抑制剂,对 Plasmodium falciparum 突变体的 Ki 值为 0.54 nM。DHFR-IN-5显示抗疟疾活性 [1]

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DHFR-IN-5 Chemical Structure

DHFR-IN-5 Chemical Structure

CAS No. : 1142407-81-5

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(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]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(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]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
分子量

360.41

Formula

C18H24N4O4

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
DHFR-IN-5
目录号:
HY-153007
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