2. Anti-infection
  3. HIV Reverse Transcriptase
  4. 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.

HIV-1-IN-85

HIV-1-IN-85 Chemical Structure

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HIV-1-IN-85 Related Antibodies

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Description

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[1].

IC50 & Target[1]

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)

In Vitro

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.

HIV-1-IN-85 Related Antibodies
In Vivo

HIV-1-IN-85 (Compound (S)-5m) (2 g/kg, p.o., single dose, 2 weeks observation) shows good in vivo safety in ICR mice[1].

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

Animal Model: ICR mice[1]
Dosage: 2 g/kg
Administration: p.o., single dose, 2 weeks observation
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.
Molecular Weight

433.48

Formula

C27H20FN5
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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HIV-1-IN-85 Related Classifications

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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.

Keywords:

HIV-1-IN-85HIVReverse TranscriptaseHuman immunodeficiency virusHIV-1 infectionNNRTIMT-4 cellsInhibitorinhibitorinhibit

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