1. Anti-infection
  2. HIV
  3. Reverse transcriptase-IN-1

Reverse transcriptase-IN-1 

Cat. No.: HY-130241
Handling Instructions

Reverse transcriptase-IN-1 (Compound 12z) is a diarylbenzopyrimidine (DABP) analogue and a potent, oral bioavailability HIV-1 nonnucleoside reverse transcriptase inhibitor. Reverse transcriptase-IN-1 has antiviral activity with EC50 values of 3.4 nM, 4.3 nM and 3.6 nM for HIV-1 IIIB, E138K and K103N mutants, respectively. And also has an IC50 value of 13.7 nM against HIV-1 mutant RT enzyme.

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

Reverse transcriptase-IN-1 Chemical Structure

Reverse transcriptase-IN-1 Chemical Structure

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Description

Reverse transcriptase-IN-1 (Compound 12z) is a diarylbenzopyrimidine (DABP) analogue and a potent, oral bioavailability HIV-1 nonnucleoside reverse transcriptase inhibitor. Reverse transcriptase-IN-1 has antiviral activity with EC50 values of 3.4 nM, 4.3 nM and 3.6 nM for HIV-1 IIIB, E138K and K103N mutants, respectively. And also has an IC50 value of 13.7 nM against HIV-1 mutant RT enzyme[1].

IC50 & Target

HIV-1

 

In Vivo

The oral bioavailability of Reverse transcriptase-IN-1 (Compound 12z) is significantly improved to 16.5% at a dose of 5 mg/kg in rats. The intrinsic rat microsome clearance of Reverse transcriptase-IN-1 is 33.2 μL/min/mg proteins. The PK study and safety assessment of Reverse transcriptase-IN-1 shows that it was absorbed with mean residence times (MRTs) of 11.8 hours (5 mg/kg, p.o.) and 11.4 hours (1 mg/kg, i.v.) at these two doses. The Cmax of Reverse transcriptase-IN-1 is 39.9 ng/mL at a dose of 5 mg/kg. A single-dose toxicity test of Reverse transcriptase-IN-1 in rats shows no mortality, and there is no abnormal body weight decrease in the animals in the week following an intragastrical dose at 293 mg/kg body weigh. The above results indicate that Reverse transcriptase-IN-1 could be an orally bioavailable candidate for treating human HIV-1 infection[1].

Molecular Weight

447.45

Formula

C₂₅H₁₇N₇O₂

SMILES

N#CC1=CC=C(NC2=NC(NC3=C([N+]([O-])=O)C=C(/C=C/C#N)C=C3C)=C4C=CC=CC4=N2)C=C1

Shipping

Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Reverse transcriptase-IN-1
Cat. No.:
HY-130241
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