Reverse transcriptase-IN-1

CAS No. 2380001-43-2

Reverse transcriptase-IN-1( —— )

Catalog No. M26414 CAS No. 2380001-43-2

Reverse transcriptase-IN-1 is a diarylbenzopyrimidine (DABP) analogue and a potent inhibitor of HIV-1 nonnucleoside reverse transcriptase with an IC50of 13.7 nM.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    Reverse transcriptase-IN-1
  • Note
    Research use only, not for human use.
  • Brief Description
    Reverse transcriptase-IN-1 is a diarylbenzopyrimidine (DABP) analogue and a potent inhibitor of HIV-1 nonnucleoside reverse transcriptase with an IC50of 13.7 nM.
  • Description
    Reverse transcriptase-IN-1 is a diarylbenzopyrimidine (DABP) analogue and a potent inhibitor of HIV-1 nonnucleoside reverse transcriptase with an IC50of 13.7 nM. (In Vitro):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.(In Vivo):The PK study and safety assessment of Reverse transcriptase-IN-1 shows that it is 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. The oral bioavailability of Reverse transcriptase-IN-1 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.
  • In Vitro
    ——
  • 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 is 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 human HIV-1 infection research.
  • Synonyms
    ——
  • Pathway
    Microbiology/Virology
  • Target
    HIV
  • Recptor
    ——
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2380001-43-2
  • Formula Weight
    447.458
  • Molecular Formula
    C25H17N7O2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 12.5 mg/mL (27.94 mM)
  • SMILES
    Cc1cc(\C=C\C#N)cc(c1Nc1nc(Nc2ccc(cc2)C#N)nc2ccccc12)[N+]([O-])=O
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Atta-ur-Rahman, et, al. Antifungal aryltetralin lignans from leaves of Podophyllum hexandrum. Phytochemistry. 1995 Sep; 40(2): 427-431.
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