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Islatravir

Name: Islatravir
Brand: TargetMol
SKU: T16098
Price: 73 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T16098Cas No. 865363-93-5

Alias MK-8591

Islatravir (MK-8591) is an effective anti-HIV-1 agent. It acts as a nucleoside reverse transcriptase inhibitor (EC50s: 0.068 nM, 3.1 nM, and 0.15 nM for HIV-1 (WT), HIV-1 (M184V), HIV-1 (MDR), respectively).

Islatravir

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Purity: 98.77%

Catalog No. T16098Alias MK-8591Cas No. 865363-93-5

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$73	In Stock	In Stock
5 mg	$173	In Stock	In Stock
10 mg	$273	In Stock	In Stock
25 mg	$478	In Stock	In Stock
50 mg	$648	In Stock	In Stock
100 mg	$870	-	In Stock
200 mg	$1,170	-	In Stock
1 mL x 10 mM (in DMSO)	$191	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:98.77%

Appearance:Solid

Color:White

Resource Download

COA HNMR HPLC LCMS

Product Introduction

Islatravir AI Summary

Islatravir exhibits significant antiviral activity against various strains of HIV-1, including X4-HIV1, R5-HIV1Ba-L, and HIV1 JR-FL. It inhibits the p24 Gag protein production in human cells, with EC50 values ranging from 0.21 nM to 21.0 nM. Additionally, it demonstrates cytotoxicity in human MT4 and PHA-PBMC cells, with CC50 values of 11000.0 nM and 12000.0 nM, respectively, and a high selectivity ratio (CC50 for MT4 cells to IC50 for HIV-1 3B) of over 60000.0. The compound shows a protective effect against HIV-1 NL4-3 replication in MT4 cells, an increase in 4'-ethynyl-2-fluoro-2'-deoxyadenosine triphosphate levels, and a favorable effect on the CD4/CD8 ratio in PBMC transplanted mice. In vivo studies reveal a decrease in viral p24 antigen levels in plasma, reduced p24 expressing human CD3+ cells in spleen cells, and good pharmacokinetic properties in Sprague-Dawley rats, including high oral bioavailability (>100.0%) at a dose of 5 mg/kg. Furthermore, Islatravir also demonstrates antiviral activity against SARS-CoV-2, with an IC50 value greater than 20000.0 nM..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Islatravir (MK-8591) is an effective anti-HIV-1 agent. It acts as a nucleoside reverse transcriptase inhibitor (EC50s: 0.068 nM, 3.1 nM, and 0.15 nM for HIV-1 (WT), HIV-1 (M184V), HIV-1 (MDR), respectively).
Targets&IC50	HIV-1 (MDR):0.15 nM (EC50), HIV-1 (M184V):3.1 nM (EC50), HIV-1 (WT):0.068 nM (EC50)
Synonyms	MK-8591

Chemical Properties

Molecular Weight	293.25
Formula	C₁₂H₁₂FN₅O₃
Cas No.	865363-93-5
Smiles	Nc1nc(F)nc2n(cnc12)[C@H]1C[C@H](O)[C@@](CO)(O1)C#C
Relative Density.	1.72 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: 3 mg/mL (10.23 mM), Sonication and heating to 60℃ are recommended.

DMSO: 100 mg/mL (341.01 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (13.64 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

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	3.4101 mL	17.0503 mL	34.1006 mL	170.5030 mL
5 mM	0.6820 mL	3.4101 mL	6.8201 mL	34.1006 mL
10 mM	0.3410 mL	1.7050 mL	3.4101 mL	17.0503 mL

DMSO

	1mg	5mg	10mg	50mg
20 mM	0.1705 mL	0.8525 mL	1.7050 mL	8.5251 mL
50 mM	0.0682 mL	0.3410 mL	0.6820 mL	3.4101 mL
100 mM	0.0341 mL	0.1705 mL	0.3410 mL	1.7050 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:

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 DMSO TargetMol | 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 DMSO TargetMol | reagent stock solution to 400 μL PEG300 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 ddH₂O TargetMol | 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.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

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