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.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
Cellular Effect
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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] |
In Vitro
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. .
In Vivo
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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