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

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.

For research use only. We do not sell to patients.

DHFR-IN-5 Chemical Structure

DHFR-IN-5 Chemical Structure

CAS No. : 1142407-81-5

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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].

In Vitro

DHFR-IN-5 (compound p218) shows highly active against PYR-resistant P. falciparum with IC50s of 4.6, 56 nM for wild-type P. falciparum (TM4), quadruple mutant P. falciparum (V1/S), respectively[1].

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

In Vivo

DHFR-IN-5 (compound p218) (30 mg/kg; p.o.) shows anti-malaria activity with good oral bioavailability (46.3%), a reasonable half-life (7.3 h) in rats[1].

MedChemExpress (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.
Molecular Weight

360.41

Formula

C18H24N4O4

CAS No.
Appearance

Solid

Color

Off-white to gray

SMILES

O=C(CCC1=C(OCCCOC2=C(CC)N=C(N)N=C2N)C=CC=C1)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Purity & Documentation
References
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  • 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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Product Name:
DHFR-IN-5
Cat. No.:
HY-153007
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