Lersivirine (Synonyms: UK-453061)

Cat. No.: HY-14267 Purity: 98.38%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Lersivirine (UK-453061) is potent and selective non-nucleoside reverse transcription inhibitor (NNRTI; IC₅₀=119 nM) with excellent efficacy against NNRTI-resistant viruses. Lersivirine exhibits potent antiretroviral activity against wild-type HIV virus and clinically relevant NNRTI-resistant strains.

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

Lersivirine Chemical Structure

CAS No. : 473921-12-9

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 124	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 124	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 113	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 182	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 345	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 540	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 119 nM (NNRT)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
MRC5	IC₅₀	> 64 μM Compound: Lersivirine	Trypanocidal activity against nifurtimox-sensitive Trypanosoma cruzi Tulahuen CL2 infected in human MRC5 SV2 cells assessed as parasite growth inhibition after 168 hrs by beta-galactosidase assay Trypanocidal activity against nifurtimox-sensitive Trypanosoma cruzi Tulahuen CL2 infected in human MRC5 SV2 cells assessed as parasite growth inhibition after 168 hrs by beta-galactosidase assay	[PMID: 25199582]
MT2	EC₅₀	0.005 nM Compound: Lersivirine, UK-453061	Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.005 multiplicities of infection after 6 days Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.005 multiplicities of infection after 6 days	[PMID: 20660667]
MT2	EC₅₀	0.05 nM Compound: Lersivirine, UK-453061	Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.05 multiplicities of infection after 6 days Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.05 multiplicities of infection after 6 days	[PMID: 20660667]
MT2	EC₅₀	0.5 nM Compound: Lersivirine, UK-453061	Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.5 multiplicities of infection after 6 days Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.5 multiplicities of infection after 6 days	[PMID: 20660667]
TZM	CC₅₀	> 100 μM Compound: Lersivirine	Cytotoxicity against human TZM-bl cells assessed as cell viability after 48 hrs by WST1 assay Cytotoxicity against human TZM-bl cells assessed as cell viability after 48 hrs by WST1 assay	[PMID: 25199582]

In Vitro

Lersivirine demonstrates excellent activity against large panels of wild type and drug-resistant HIV consistent with the encouraging profile demonstrated against the isolated RT enzymes^[1].

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

In Vivo

Lersivirine (oral gavage; 0, 150, 350, and 500 mg/kg; once daily; gestation days 6 to 17, followed by cesarean section on gestation day 18. ) allows induction of hepatic metabolizing enzymes at the first 2 days at 250 mg/kg, after which the dose is increased to 500 mg/kg/day in Mated Crl:CD1(ICR) mice. Lersivirine leads to skeletal variations which related to delayed development and decreased fetal ossifications^[1].

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

Clinical Trial

Molecular Weight

310.35

Formula

C₁₇H₁₈N₄O₂

CAS No.

473921-12-9

Appearance

Solid

Color

Light yellow to khaki

SMILES

CCC1=NN(CCO)C(CC)=C1OC2=CC(C#N)=CC(C#N)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (161.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.2222 mL	16.1108 mL	32.2217 mL
5 mM	0.6444 mL	3.2222 mL	6.4443 mL
10 mM	0.3222 mL	1.6111 mL	3.2222 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, 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.

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: ≥ 3 mg/mL (9.67 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

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: 98.38%

Select Batch:

Data Sheet (277 KB) SDS (251 KB)

COA (255 KB) RP-HPLC (245 KB)

Handling Instructions (2659 KB)

References

[1]. Mowbray CE, et al. Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate. Bioorg Med Chem Lett. 2009 Oct 15;19(20):5857-60. [Content Brief]

[2]. Gregg D Cappon, et al. Developmental toxicity study of lersivirine in mice. Birth Defects Res B Dev Reprod Toxicol. 2012 Jun;95(3):225-30. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	3.2222 mL	16.1108 mL	32.2217 mL	80.5542 mL
	5 mM	0.6444 mL	3.2222 mL	6.4443 mL	16.1108 mL
	10 mM	0.3222 mL	1.6111 mL	3.2222 mL	8.0554 mL
	15 mM	0.2148 mL	1.0741 mL	2.1481 mL	5.3703 mL
	20 mM	0.1611 mL	0.8055 mL	1.6111 mL	4.0277 mL
	25 mM	0.1289 mL	0.6444 mL	1.2889 mL	3.2222 mL
	30 mM	0.1074 mL	0.5370 mL	1.0741 mL	2.6851 mL
	40 mM	0.0806 mL	0.4028 mL	0.8055 mL	2.0139 mL
	50 mM	0.0644 mL	0.3222 mL	0.6444 mL	1.6111 mL
	60 mM	0.0537 mL	0.2685 mL	0.5370 mL	1.3426 mL
	80 mM	0.0403 mL	0.2014 mL	0.4028 mL	1.0069 mL
	100 mM	0.0322 mL	0.1611 mL	0.3222 mL	0.8055 mL

Lersivirine 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:

Lersivirine473921-12-9UK-453061UK453061UK 453061HIVReverse TranscriptaseHuman immunodeficiency virusnon-nucleoside reverse transcriptionNNRTINNRTI-resistantHIV virusresistant strainInhibitorinhibitorinhibit

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