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Doravirine

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Catalog No. T3632Cas No. 1338225-97-0
Alias MK-1439

Doravirine (MK-1439) is a non-nucleoside reverse transcriptase inhibitor used for the treatment of HIV/AIDS.

Doravirine

Doravirine

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Purity: 99.79%
Catalog No. T3632Alias MK-1439Cas No. 1338225-97-0
Doravirine (MK-1439) is a non-nucleoside reverse transcriptase inhibitor used for the treatment of HIV/AIDS.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$45In StockIn Stock
2 mg$63In StockIn Stock
5 mg$98In StockIn Stock
10 mg$178In StockIn Stock
25 mg$353In StockIn Stock
50 mg$547In StockIn Stock
100 mg$789In StockIn Stock
500 mg$1,630InquiryInquiry
1 mL x 10 mM (in DMSO)$133In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.79%
Color:White
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Product Introduction

Bioactivity
Description
Doravirine (MK-1439) is a non-nucleoside reverse transcriptase inhibitor used for the treatment of HIV/AIDS.
Targets&IC50
Y181C:31nM, K103N/Y181C:33 nM, K103N:21nM, Virus (WT):12nM
In vitro
Doravirine exhibits potent antiviral activity against wild-type virus and K103N, Y181C, and K103N/Y181C mutant viruses, with IC50 value of 12, 21, 31, and 33 nM, respectively. [1]? MK-1439 exhibited similar antiviral activities against 10 different HIV-1 subtype viruses (a total of 93 viruses).[2]
In vivo
Administration of 50 mg doravirine with a high-fat meal is associated with slight elevations in AUC time zero to infinity (AUC0-∞) and C24 h with no change in Cmax. Midazolam AUC0-∞ is slightly reduced by coadministration of doravirine (geometric mean ratio 0.82, 90% CI 0.70, 0.97). [3]
Kinase Assay
FS-3 substrate is solubilized in assay buffer at 500 μM and frozen at -20°C in single-use aliquots for up to 4 weeks. Recombinant autotaxin is diluted in Tris-buffered saline (140 mM NaCl, 5 mM KCl, 1 mM CaCl2, 1 mM MgCl2, 50 mM Tris, pH 8.0) and incubated with compound in DMSO or DMSO alone (final 1% DMSO) for 15 min at 37°C, and the reaction is started with the addition of FS-3 at a final concentration of 1 μM. The reaction is allowed to proceed at 37°C for 30 min and monitored at 520 nm until the uninhibited control compared with a no-enzyme control gave a Z′≥0.5. IC50s are determined in triplicate by using a four-parameter fit[1].
SynonymsMK-1439
Chemical Properties
Molecular Weight425.75
FormulaC17H11ClF3N5O3
Cas No.1338225-97-0
SmilesCn1c(Cn2ccc(c(Oc3cc(Cl)cc(c3)C#N)c2=O)C(F)(F)F)n[nH]c1=O
Relative Density.1.56 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 100 mg/mL (234.88 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+90% Corn Oil: 2 mg/mL (4.7 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.3488 mL11.7440 mL23.4880 mL117.4398 mL
5 mM0.4698 mL2.3488 mL4.6976 mL23.4880 mL
10 mM0.2349 mL1.1744 mL2.3488 mL11.7440 mL
20 mM0.1174 mL0.5872 mL1.1744 mL5.8720 mL
50 mM0.0470 mL0.2349 mL0.4698 mL2.3488 mL
100 mM0.0235 mL0.1174 mL0.2349 mL1.1744 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
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Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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