1. Anti-infection
  2. HIV
    Reverse Transcriptase
  3. Lersivirine

Lersivirine (Synonyms: UK-453061)

Cat. No.: HY-14267 Purity: 98.01%
Handling Instructions

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

Lersivirine Chemical Structure

CAS No. : 473921-12-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 158 In-stock
Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
Estimated Time of Arrival: December 31
10 mg USD 240 In-stock
Estimated Time of Arrival: December 31
50 mg USD 840 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1440 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

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[1].

IC50 & Target

IC50: 119 nM (NNRT)[1]

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].

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].

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

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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (161.11 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

*All of the co-solvents are provided by MCE.
References
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Keywords:

LersivirineUK-453061UK453061UK 453061HIVReverse TranscriptaseHuman immunodeficiency virusnon-nucleoside reverse transcriptionNNRTINNRTI-resistantHIV virusresistant strainInhibitorinhibitorinhibit

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Lersivirine
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HY-14267
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