HIV-1-IN-85
HIV-1-IN-85 is an orally active HIV-1 inhibitor (IC50 = 72 nM). HIV-1-IN-85 exhibits strong inhibitory activity against wild-type (WT) HIV-1 and NNRTI-resistant single mutant strains (L100I, K103N, Y181C, Y188L, E138K) and moderate efficacy against double mutant strains (F227L+V106A, RES056). HIV-1-IN-85 shows good in vivo safety in ICR mice. HIV-1-IN-85 can be used for the study of HIV-1 infection.
For research use only. We do not sell to patients.
- Formula: C27H20FN5
- Molecular Weight:433.48
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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
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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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HIV-1 72 nM (IC50) |
HIV-1 (WT) 3.7 nM (EC50) |
HIV-1 (L100I) 9.2 nM (EC50) |
HIV-1 (K103N) 5.8 nM (EC50) |
HIV-1 (Y181C) 3.7 nM (EC50) |
HIV-1 (Y188L) 231 nM (EC50) |
HIV-1 (E138K) 30 nM (EC50) |
HIV-1 (F227L+V106A) 2399 nM (EC1.5) |
HIV-1 (RES056) 277 nM (EC50) |
HIV-1-IN-85 (Compound (S)-5m) exhibits potent antiviral activity against WT HIV-1 and single mutant strains in MT-4 cells, with EC50 values of 3.7 nM (WT), 9.2 nM (L100I), 5.8 nM (K103N), 37 nM (Y181C), 231 nM (Y188L), 30 nM (E138K), 2399 nM (F227L+V106A) and 277 nM (RES056)[1].
HIV-1-IN-85 inhibits the polymerase activity of WT HIV-1 (IC50 = 72 nM) in enzyme-level assays[1].
HIV-1-IN-85 (40 μM, 24 h) has minimal effect on mitochondrial function in MT-4 cells and exhibits negligible inhibition on the hERG channel[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:ICR mice[1]
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Dosage:2 g/kg
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Administration:p.o., single dose, 2 weeks observation
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Result:Showed good in vivo safety in ICR mice, with no deaths or abnormal behaviors, no significant differences in body weight.
Showed no obvious pathological damage in brain, heart, liver, spleen, lung and kidney.
Chemical Information
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Molecular Weight 433.48
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Formula C27H20FN5
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SMILES
CC1=CC(C2=CC=C(C=C2)C#N)=CC(C)=C1[C@@H](C3=CC=NC(NC4=CC=C(C=C4)C#N)=N3)F
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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)
HIV-1-IN-85 Related Classifications
HY-175491 Related Classifications
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