DHFR-IN-5 hydrochloride
DHFR-IN-5 hydrochloride 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 hydrochloride shows anti-malaria activity.
For research use only. We do not sell to patients.
- CAS No.: 1142407-60-0
- Formula: C18H25ClN4O4
- Molecular Weight:396.87
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
<1 μM
Compound: P218
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Antimalarial activity against sporozoite stage of Plasmodium yoelii assessed as invasion of human HepG2 cells expressing CD81 incubated for 2 hrs prior to inoculation measured after 1 hr by immunofluorescence assay in presence of penicillin/streptomycin
Antimalarial activity against sporozoite stage of Plasmodium yoelii assessed as invasion of human HepG2 cells expressing CD81 incubated for 2 hrs prior to inoculation measured after 1 hr by immunofluorescence assay in presence of penicillin/streptomycin
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[PMID: 23927658] |
DHFR-IN-5 (compound p218) hydrochloride 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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats[1]
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Dosage:30 mg/kg
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Administration:P.o.
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Result:Showed good oral bioavailability (46.3%), a reasonable half-life (7.3 h), and minimal distribution into the brain.
Chemical Information
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CAS No. 1142407-60-0
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Molecular Weight 396.87
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Formula C18H25ClN4O4
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SMILES
O=C(CCC1=C(OCCCOC2=C(CC)N=C(N)N=C2N)C=CC=C1)O.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DHFR-IN-5 hydrochloride Related Classifications
HY-153007A Related Classifications
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