Islatravir (Synonyms: MK-8591)

Name: Islatravir
Brand: MedChemExpress
SKU: HY-104012
Rating: 4.5 (1 reviews)

Cat. No.: HY-104012 Purity: 99.94%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Islatravir (MK-8591) is a potent anti-HIV-1 agent, acting as a nucleoside reverse transcriptase inhibitor, with EC₅₀s of 0.068 nM, 3.1 nM and 0.15 nM for HIV-1 (WT), HIV-1 (M184V), HIV-1 (MDR), respectively. Islatravir is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

For research use only. We do not sell to patients.

Islatravir Chemical Structure

CAS No. : 865363-93-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 385	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 385	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 550	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 960	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1300	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1750	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Islatravir:

EFdA-TP Get quote

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View All HIV Isoform Specific Products:

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HIV HIV-1 HIV-2

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

HIV-1 (WT)

0.068 nM (EC₅₀)

HIV-1 (MDR)

0.15 nM (EC₅₀)

HIV-1 (M184V)

3.1 nM (EC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
MT4	CC₅₀	> 4.2 μM Compound: MK-8591	Cytotoxicity in human MT4 cells expressing GFP assessed as reduction in cell viability incubated for 48 hrs by cell-titer-Glo luminescent cell viability assay Cytotoxicity in human MT4 cells expressing GFP assessed as reduction in cell viability incubated for 48 hrs by cell-titer-Glo luminescent cell viability assay	[PMID: 30265808]
MT4	EC₅₀	0.001 μM Compound: EFdA	Antiviral activity against X4-HIV1 NL4-3 assessed as inhibition of p24 Gag protein production in human MT4 cells by MTT assay Antiviral activity against X4-HIV1 NL4-3 assessed as inhibition of p24 Gag protein production in human MT4 cells by MTT assay	[PMID: 17548498]
MT4	IC₅₀	0.3 nM Compound: 23	Antiviral activity against HIV-1 3B infected in human MT4 cells incubated for 5 days by MTT assay Antiviral activity against HIV-1 3B infected in human MT4 cells incubated for 5 days by MTT assay	[PMID: 32031378]
MT4	CC₅₀	11 μM Compound: EFdA	Cytotoxicity against human MT4 cells by MTT assay Cytotoxicity against human MT4 cells by MTT assay	[PMID: 17548498]
PBMC	CC₅₀	12 μM Compound: EFdA	Cytotoxicity against human PHA-PBMC cells by MTT assay Cytotoxicity against human PHA-PBMC cells by MTT assay	[PMID: 17548498]

In Vitro

Islatravir (MK-8591) (4'Ed2FA) is a potent anti-HIV-1 agent, acting as a nucleoside reverse transcriptase inhibitor, with EC₅₀s of 0.068 nM, 3.1 nM and 0.15 nM for HIV-1 (WT), HIV-1 (M184V), HIV-1 (MDR), respectively^[1].

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

Clinical Trial

Molecular Weight

293.25

Formula

C₁₂H₁₂FN₅O₃

CAS No.

865363-93-5

Appearance

Solid

Color

White to off-white

SMILES

NC1=NC(F)=NC2=C1N=CN2[C@@H]3O[C@](CO)(C#C)[C@H](O)C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (341.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 3.57 mg/mL (12.17 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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: ≥ 2.08 mg/mL (7.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (7.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (7.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 4

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 1.1 mg/mL (3.75 mM); Clear solution
Protocol 5

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.1 mg/mL (3.75 mM); Clear solution

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 1.35 mg/mL (4.60 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.94%

Select Batch:

Data Sheet (273 KB) SDS (393 KB)

COA (249 KB) HNMR (223 KB) LCMS (136 KB)

Handling Instructions (2659 KB)

References

[1]. Ohrui H, et al. 2'-deoxy-4'-C-ethynyl-2-fluoroadenosine, a nucleoside reverse transcriptase inhibitor, is highly potent against all human immunodeficiency viruses type 1 and has low toxicity. Chem Rec. 2006;6(3):133-43. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	3.4101 mL	17.0503 mL	34.1006 mL	85.2515 mL
	5 mM	0.6820 mL	3.4101 mL	6.8201 mL	17.0503 mL
	10 mM	0.3410 mL	1.7050 mL	3.4101 mL	8.5251 mL
DMSO	15 mM	0.2273 mL	1.1367 mL	2.2734 mL	5.6834 mL
	20 mM	0.1705 mL	0.8525 mL	1.7050 mL	4.2626 mL
	25 mM	0.1364 mL	0.6820 mL	1.3640 mL	3.4101 mL
	30 mM	0.1137 mL	0.5683 mL	1.1367 mL	2.8417 mL
	40 mM	0.0853 mL	0.4263 mL	0.8525 mL	2.1313 mL
	50 mM	0.0682 mL	0.3410 mL	0.6820 mL	1.7050 mL
	60 mM	0.0568 mL	0.2842 mL	0.5683 mL	1.4209 mL
	80 mM	0.0426 mL	0.2131 mL	0.4263 mL	1.0656 mL
	100 mM	0.0341 mL	0.1705 mL	0.3410 mL	0.8525 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Islatravir Related Classifications

Infection

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Islatravir865363-93-5MK-8591MK8591MK 8591HIVReverse TranscriptaseHuman immunodeficiency virusInhibitorinhibitorinhibit

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Islatravir (Synonyms: MK-8591)

Customer Review

Other Forms of Islatravir:

Islatravir Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All HIV Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Islatravir Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Islatravir Related Classifications

Keywords:

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