
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)






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Biological Information
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Product NameDoravirine
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NoteResearch use only, not for human use.
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Brief DescriptionDoravirine (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.
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DescriptionDoravirine (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.
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In VitroSelectivity 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).
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In VivoAdministration 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.
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SynonymsMK-1439 | MK1439
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PathwayMicrobiology/Virology
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TargetHIV
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RecptorHIV-1
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Research AreaInfection
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IndicationHIV Infection
Chemical Information
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CAS Number1338225-97-0
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Formula Weight425.7491
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Molecular FormulaC17H11ClF3N5O3
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Purity>98% (HPLC)
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SolubilityDMSO: ≥ 30 mg/mL
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SMILESN#CC1=CC(OC2=C(C(F)(F)F)C=CN(CC(N3C)=NNC3=O)C2=O)=CC(Cl)=C1
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Chemical NameBenzonitrile, 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
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Storage(-20℃)
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ShippingWith Ice Pack
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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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