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Lersivirine

Name: Lersivirine
Brand: TargetMol
SKU: T7700
Price: 39 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T7700Cas No. 473921-12-9

Alias UK-453061, Lersivirine(UK 453061)

Lersivirine (UK-453061)(UK 453061) is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) under development for HIV infection therapy.

Lersivirine

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Purity: 98.01%

Catalog No. T7700Alias UK-453061, Lersivirine(UK 453061)Cas No. 473921-12-9

Lersivirine (UK-453061)(UK 453061) is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) under development for HIV infection therapy.

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$39	In Stock	In Stock
10 mg	$62	In Stock	In Stock
25 mg	$119	In Stock	In Stock
50 mg	$188	In Stock	In Stock
100 mg	$271	In Stock	In Stock
200 mg	$383	-	In Stock
1 mL x 10 mM (in DMSO)	$41	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:98.01%

Appearance:Solid

Color:White

Resource Download

COA HNMR LCMS

Product Introduction

Lersivirine AI Summary

Lersivirine exhibits significant antiviral activity against HIV with IC50 values of 4.0 nM and 119.0 nM in different assays. It targets multiple HIV reverse transcriptase mutants with IC95 values ranging from 40.0 nM to 100.0 nM and shows an ability to inhibit both non-competitively and competitively. The compound has low cytotoxicity toward human cells with CC30 values above 30.0 µM, and CC50 values greater than 100,000 nM in certain assays, indicating a high selectivity index. It maintains metabolic stability with a half-life of 1.217 hours in human liver microsomes and demonstrates a half-life of approximately 6.223 hours in healthy human plasma. Pharmacokinetic data shows a peak plasma concentration (Cmax) of about 4910.43 nM and an area under the curve (AUC) of 10967.32 ng.hr.mL-1. Additionally, coadministration with an antacid affects its Tmax, which is 5.0 hours compared to 2.0 hours when administered alone. Moreover, Lersivirine exhibits activity against other viral infections, including SARS-CoV-2, showing cytotoxicity inhibition in Caco-2 and VERO-6 cells at a concentration of 10 µM. It also shows inhibition percentages against SARS-CoV-2 3CL-Pro protease at 20 µM. The compound demonstrates inhibitory activity against the human HDAC6 enzyme and induces the activity of CYP3A, influencing midazolam metabolism. In addition to its antiviral properties, Lersivirine shows antitrypanocidal activity against Trypanosoma brucei and antileishmanial and antiplasmodial activities, albeit with IC50 values indicating low potency in these assays. Overall, Lersivirine presents a broad spectrum of bioactivities with notable efficacy against HIV and potential applications against other viral infections and parasitic diseases..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Lersivirine (UK-453061)(UK 453061) is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) under development for HIV infection therapy.
Targets&IC50	NNRT:119 nM (IC50)
Synonyms	UK-453061, Lersivirine(UK 453061)

Chemical Properties

Molecular Weight	310.35
Formula	C₁₇H₁₈N₄O₂
Cas No.	473921-12-9
Smiles	CCc1nn(CCO)c(CC)c1Oc1cc(cc(c1)C#N)C#N
Relative Density.	1.19

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

DMSO: 50 mg/mL (161.11 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2.5 mg/mL (8.06 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

	1mg	5mg	10mg	50mg
1 mM	3.2222 mL	16.1108 mL	32.2217 mL	161.1084 mL
5 mM	0.6444 mL	3.2222 mL	6.4443 mL	32.2217 mL
10 mM	0.3222 mL	1.6111 mL	3.2222 mL	16.1108 mL
20 mM	0.1611 mL	0.8055 mL	1.6111 mL	8.0554 mL
50 mM	0.0644 mL	0.3222 mL	0.6444 mL	3.2222 mL
100 mM	0.0322 mL	0.1611 mL	0.3222 mL	1.6111 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