1. Anti-infection
  2. HIV
    Reverse Transcriptase

Lersivirine (Synonyms: UK-453061; UK453061; UK 453061)

Cat. No.: HY-14267
Handling Instructions

Lersivirine(UK-453061) is a next-generation non-nucleoside reverse transcriptase inhibitor (NNRTI, IC50=119 nM) with a unique resistance profile that exhibits potent antiretroviral activity against wild-type human immunodeficiency 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 $132 In-stock
5 mg $120 In-stock
10 mg $200 In-stock
50 mg $700 In-stock
100 mg $1200 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Description

Lersivirine(UK-453061) is a next-generation non-nucleoside reverse transcriptase inhibitor (NNRTI, IC50=119 nM) with a unique resistance profile that exhibits potent antiretroviral activity against wild-type human immunodeficiency virus and clinically relevant NNRTI-resistant strains. IC50 value: 0.119 uM [1] Target: NNRTI UK-453061(Compound 5) demonstrated excellent activity against large panels of wild type and drug-resistant HIV consistent with the encouraging profile demonstrated against the isolated RT enzymes. Compound 5 can be readily prepared in multi-gram quantities by virtue of the efficient and concise synthetic route. The compound also has good aqueous solubility and formulation characteristics which enable further in vivo evaluation. Clinical trials evaluating the potential of 5 (UK-453,061, lersivirine) to treat HIV infection are proceeding and further progress will be reported in due course [1]. At clinically relevant lersivirine doses (500-1,000 mg total daily dose), the mean plasma exposure of midazolam was reduced in a dose-dependent manner by 20-36 %. Co-administration of lersivirine 1,000 mg QD with OCs had minor PK effects, increasing ethinylestradiol exposure by 10 % and reducing levonorgestrel exposure by 13 % [2]. Mated Crl:CD1(ICR) mice were administered 0, 150, 350, and 500 mg/kg lersivirine once daily by oral gavage on gestation days 6 to 17, followed by cesarean section on gestation day 18. The first 2 days of dosing for the high-dose group were done at 250 mg/kg to allow induction of hepatic metabolizing enzymes, after which the dose was increased to 500 mg/kg/day [3].

Clinical Trial
Sponsor Condition Start Date Phase
Pfizer Inc HIV-1 infection 2009-02-28 Phase 2
Pfizer Inc HIV-1 infection 2009-03-31 Phase 2
Pfizer Inc HIV-1 infection 2011-02-28 Phase 2
Pfizer Inc HIV infection 2006-02-28 Phase 2
Pfizer Inc 2012-06-30 Phase 1
Preparing Stock Solutions
Concentration Volume (DMSO) 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
M.Wt

310.35

Formula

C₁₇H₁₈N₄O₂

CAS No.

473921-12-9

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

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

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Lersivirine
Cat. No.:
HY-14267
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