Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Lersivirine (formerly UK-453061; UK453061) is a novel next-generation and potent non-nucleoside reverse transcriptase inhibitor (NNRTI) with IC50 of 119 nM and a unique resistance profile. It exhibits potent antiretroviral activity against wild-type human immunodeficiency virus and clinically relevant NNRTI-resistant strains. Lersivirine was under development for HIV infection therapy. It binds reverse transcriptase in a distinct way leading to a unique resistance profile. In February 2013, ViiV Healthcare announced the development of lersivirine was disconinued.
ln Vitro |
In line with the promising results seen against isolated RT enzymes, lerivirine shows outstanding efficacy against a variety of drug-resistant and wild-type HIV strains [1].
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ln Vivo |
Lersivirine causes skeletal variations in mated Crl:CD1(ICR) mice, which are linked to developmental delays and reduced fetal ossification. Lersivirine (oral gavage; 0, 150, 350, and 500 mg/kg; once daily; days 6 to 17 of gestation, followed by caesarean section on day 18 of gestation) induces hepatic metabolic enzymes at 250 mg for the first 2 days/ kg, followed by increasing the dose to 500 mg/kg/day.
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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.
[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. |
Molecular Formula |
C17H18N4O2
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Molecular Weight |
310.3504
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CAS # |
473921-12-9
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Related CAS # |
147362-57-0 (Loviride); 16837-52-8 (Oxymatrine)
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SMILES |
N#CC1=CC(OC2=C(CC)N(CCO)N=C2CC)=CC(C#N)=C1
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InChi Key |
MCPUZZJBAHRIPO-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C17H18N4O2/c1-3-15-17(16(4-2)21(20-15)5-6-22)23-14-8-12(10-18)7-13(9-14)11-19/h7-9,22H,3-6H2,1-2H3
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Chemical Name |
5-((3,5-diethyl-1-(2-hydroxyethyl)-1H-pyrazol-4-yl)oxy)isophthalonitrile
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Synonyms |
UK 453061; UK-453061; UK-453,061; UK453,061; UK453061; UK 453,061
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~50 mg/mL (~161.11 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (9.67 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.