Doravirine

CAS No. 1338225-97-0

Doravirine( MK-1439 | MK1439 )

Catalog No. M11354 CAS No. 1338225-97-0

Doravirine (MK-1439, MK1439) is a novel, highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor (NNRTI) with IC50 of 12, 9.7, and 9.7 nM against WT, K103N, and Y181C reverse transcriptase (RT) mutants, respectively.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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5MG 88 In Stock
10MG 160 In Stock
25MG 318 In Stock
50MG 492 In Stock
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Biological Information

  • Product Name
    Doravirine
  • Note
    Research use only, not for human use.
  • Brief Description
    Doravirine (MK-1439, MK1439) is a novel, highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor (NNRTI) with IC50 of 12, 9.7, and 9.7 nM against WT, K103N, and Y181C reverse transcriptase (RT) mutants, respectively.
  • Description
    Doravirine (MK-1439, MK1439) is a novel, highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor (NNRTI) with IC50 of 12, 9.7, and 9.7 nM against WT, K103N, and Y181C reverse transcriptase (RT) mutants, respectively, in a biochemical assay; shows excellent potency in suppressing the replication of WT virus with EC95 of 20 nM, as well as K103N, Y181C, and K103N/Y181C mutant viruses with EC95 of 43, 27, and 55 nM, respectively.HIV Infection Phase 3 Clinical(In Vitro):Selectivity and cytotoxicity studies confirmed that Doravirine is a highly specific nonnucleoside reverse transcriptase inhibitors with minimum off-target activities. In the presence of 50% normal human serum (NHS), Doravirine shows excellent potency in suppressing the replication of WT virus, with a 95% effective concentration (EC95) of 20 nM, as well as K103N, Y181C, and K103N/Y181C mutant viruses with EC9595 of 43, 27, and 55 nM, respectively. Doravirine exhibits similar antiviral activities against 10 different HIV-1 subtype viruses (a total of 93 viruses).(In Vivo):Administration of 50 mg Doravirine with a high-fat meal is associated with slight elevations in AUC time zero to infinity and C24 h with no change in Cmax.
  • In Vitro
    Selectivity and cytotoxicity studies confirmed that Doravirine is a highly specific nonnucleoside reverse transcriptase inhibitorswith minimum off-target activities. In the presence of 50% normal human serum (NHS), Doravirine shows excellent potency in suppressing the replication of WT virus, with a 95% effective concentration (EC95) of 20 nM, as well as K103N, Y181C, and K103N/Y181C mutant viruses with EC9595 of 43, 27, and 55 nM, respectively. Doravirine exhibits similar antiviral activities against 10 different HIV-1 subtype viruses (a total of 93 viruses).
  • In Vivo
    Administration of 50 mg Doravirine with a high-fat meal is associated with slight elevations in AUC time zero to infinity and C24 h with no change in Cmax.
  • Synonyms
    MK-1439 | MK1439
  • Pathway
    Microbiology/Virology
  • Target
    HIV
  • Recptor
    HIV-1
  • Research Area
    Infection
  • Indication
    HIV Infection

Chemical Information

  • CAS Number
    1338225-97-0
  • Formula Weight
    425.7491
  • Molecular Formula
    C17H11ClF3N5O3
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: ≥ 30 mg/mL
  • SMILES
    N#CC1=CC(OC2=C(C(F)(F)F)C=CN(CC(N3C)=NNC3=O)C2=O)=CC(Cl)=C1
  • Chemical Name
    Benzonitrile, 3-chloro-5-[[1-[(4,5-dihydro-4-methyl-5-oxo-1H-1,2,4-triazol-3-yl)methyl]-1,2-dihydro-2-oxo-4-(trifluoromethyl)-3-pyridinyl]oxy]-

Shipping & Storage Information

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

Reference

1. Lai MT, et al. Antimicrob Agents Chemother. 2014;58(3):1652-63. 2. C?té B, et al. Bioorg Med Chem Lett. 2014 Feb 1;24(3):917-22. 3. Feng M, et al. Antimicrob Agents Chemother. 2015 Jan;59(1):590-8.
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