Art. -Nr.: HY-16767

Doravirine

(Synonyms: MK-1439)

14 Cited Publications

Kundenbewertung

Based on 14 publication(s) in Google Scholar

Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC₅₀s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181C reverse transcriptase mutants, respectively.

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Reinheit: 99.79%
CAS. Nr.: 1338225-97-0
Formel: C₁₇H₁₁ClF₃N₅O₃
Molecular Weight:425.75

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Doravirine Chemical Structure

CAS. Nr.: 1338225-97-0

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (14)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

HIV-1

Alle HIV Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MT4	CC₅₀	>293 μM Compound: DOR	Cytotoxicity against human MT4 cells Cytotoxicity against human MT4 cells	[PMID: 35061384]
MT4	CC₅₀	>294 μM Compound: 6; DOR	Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay	[PMID: 30606670]
MT4	CC₅₀	>294 μM Compound: DOR	Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay	[PMID: 34496571]
MT4	CC₅₀	>294 μM Compound: DOR	Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay	[PMID: 38613773]
MT4	CC₅₀	293.24 μM Compound: DOR	Cytotoxicity against human MT4 cells assessed as reduction on cell growth by MTT assay Cytotoxicity against human MT4 cells assessed as reduction on cell growth by MTT assay	[PMID: 35797898]

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)^[1].

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

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 C_max^[2].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1338225-97-0
Appearance Solid
Molecular Weight 425.75
Formel C₁₇H₁₁ClF₃N₅O₃
Color White to off-white
SMILES

N#CC1=CC(OC2=C(C(F)(F)F)C=CN(CC(N3C)=NNC3=O)C2=O)=CC(Cl)=C1
Synonyms

MK-1439
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (14)

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Journal Impact Factor

Sci Adv

GRL-142 binds to and impairs HIV-1 integrase nuclear localization signal and potently suppresses highly INSTI-resistant HIV-1 variants. [Abstract]

2023 Jul 14;9(28):eadg2955. PMID: 37436982
J Photochem Photobiol A Chem

2025 Nov 15;473:116930.
Molecules

Targeting HIV-1 Reverse Transcriptase Using a Fragment-Based Approach. [Abstract]

2023 Mar 30;28(7):3103. PMID: 37049868
Int J Antimicrob Agents

Residual phenotypic susceptibility to doravirine in multidrug resistant HIV-1 from subjects enrolled in the PRESTIGIO Registry. [Abstract]

2023 Mar;61(3):106737. PMID: 36708743
Int J Antimicrob Agents

Efficacy of antiretroviral compounds against Toxoplasma gondii in vitro. [Abstract]

2019 Dec;54(6):814-819. PMID: 31479744
J Infect Dis

Prevalence and phenotypic susceptibility to doravirine of the HIV-1 reverse transcriptase V106I polymorphism in B and non-B subtypes. [Abstract]

2024 Jun 14;229(6):1796-1802. PMID: 38206187
J Antimicrob Chemother

Variable antiviral activity of islatravir against M184I/V mutant HIV-1 selected during antiretroviral therapy. [Abstract]

2024 Feb 1;79(2):370-374. PMID: 38153245
J Antimicrob Chemother

Placental transfer of doravirine, a recent HIV-1 NNRTI in the ex vivo human cotyledon perfusion model. [Abstract]

2021 Aug 12;76(9):2364-2367. PMID: 34151361
J Antimicrob Chemother

In vitro cross-resistance to doravirine in a panel of HIV-1 clones harbouring multiple NNRTI resistance mutations. [Abstract]

2021 Jan 1;76(1):130-134. PMID: 32974670
Viruses

Analysis and Molecular Determinants of HIV RNase H Cleavage Specificity at the PPT/U3 Junction. [Abstract]

2021 Jan 18;13(1):131. PMID: 33477685
Toxicol Lett

Discovery of non-steroidal aldo-keto reductase 1D1 inhibitors through automated screening and in vitro evaluation. [Abstract]

2025 Apr:406:31-37. PMID: 39988211
J Chromatogr B Analyt Technol Biomed Life Sci

Development, validation and clinical implementation of a HPLC-MS/MS method for the simultaneous quantification of bictegravir, emtricitabine, doravirine, cabotegravir, lenacapavir, fostemsavir, tenofovir alafenamide and the corresponding metabolites temsavir and tenofovir, in human plasma. [Abstract]

2025 Dec 15:1267:124803. PMID: 41072339
bioRxiv

Structural and Mechanistic Basis of F227C-Mediated Hypersusceptibility to Islatravir in HIV-1 Reverse Transcriptase. [Abstract]

2026 Jun 10:2026.06.08.730881. PMID: 42327331
Preprints

2024 Aug 30.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (234.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3488 mL

11.7440 mL

23.4880 mL

5 mM

0.4698 mL

2.3488 mL

4.6976 mL

10 mM

0.2349 mL

1.1744 mL

2.3488 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.5 mg/mL (5.87 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.87 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Lai MT et al. In vitro characterization of MK-1439, a novel HIV-1 nonnucleoside reverse transcriptase inhibitor. Antimicrob Agents Chemother. 2014;58(3):1652-63. [Content Brief]

[2]. Anderson MS et al. Safety, tolerability and pharmacokinetics of doravirine, a novel HIV non-nucleoside reverse transcriptase inhibitor, after single and multiple doses in healthy subjects. Antivir Ther. 2015;20(4):397-405. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3488 mL	11.7440 mL	23.4880 mL	58.7199 mL
	5 mM	0.4698 mL	2.3488 mL	4.6976 mL	11.7440 mL
	10 mM	0.2349 mL	1.1744 mL	2.3488 mL	5.8720 mL
	15 mM	0.1566 mL	0.7829 mL	1.5659 mL	3.9147 mL
	20 mM	0.1174 mL	0.5872 mL	1.1744 mL	2.9360 mL
	25 mM	0.0940 mL	0.4698 mL	0.9395 mL	2.3488 mL
	30 mM	0.0783 mL	0.3915 mL	0.7829 mL	1.9573 mL
	40 mM	0.0587 mL	0.2936 mL	0.5872 mL	1.4680 mL
	50 mM	0.0470 mL	0.2349 mL	0.4698 mL	1.1744 mL
	60 mM	0.0391 mL	0.1957 mL	0.3915 mL	0.9787 mL
	80 mM	0.0294 mL	0.1468 mL	0.2936 mL	0.7340 mL
	100 mM	0.0235 mL	0.1174 mL	0.2349 mL	0.5872 mL

Keywords

Doravirine

14 Cited Publications

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Doravirine

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Publications Citing Use of MedChemExpress (MCE) Doravirine

Alle HIV Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Doravirine

Anti-Infection Compound Library

Immunology/Inflammation Compound Library

FDA-Approved Drug Library

Antiviral Compound Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Drug-Induced Liver Injury (DILI) Compound Library

Rare Diseases Drug Library

Pediatric Drug Library

EMA-Approved Drug Library

Human Metabolite Library

Mitochondrial Toxicity Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Classic FDA-Approved Drug Library

Publications Citing Use of MedChemExpress (MCE) Doravirine

Alle HIV Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Doravirine Related Classifications

HY-16767 Related Classifications