An NNRTI
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Lersivirine

Item No. 29497

Technical Information
Formal Name
5-[[3,5-diethyl-1-(2-hydroxyethyl)-1H-pyrazol-4-yl]oxy]-1,3-benzenedicarbonitrile
CAS Number
473921-12-9
Synonyms
  • UK-453,061
Molecular Formula
C17H18N4O2
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 10 mg/ml
λmax
213 nm
SMILES
CCC1=C(C(CC)=NN1CCO)OC2=CC(C#N)=CC(C#N)=C2
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
InChi Key
MCPUZZJBAHRIPO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Lersivirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI; mean IC50 = 118 nM for the wild-type HIV-1 enzyme).1 It inhibits a panel of 14 single-point mutant HIV-1 reverse transcriptases with mean IC50 values within 10-fold of the wild-type enzyme. Lersivirine inhibits HIV-1 virus replication in MT-2 cells with EC50 values of 5.04, 13.1, and 34.9 nM at multiplicities of infection (MOIs) of 0.005, 0.05, and 0.5, respectively, and exhibits synergistic or additive effects when used in combination with a variety of antiretroviral agents.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Corbau, R., Mori, J., Phillips, C., et alLersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. Antimicrob. Agents Chemother. 54(10), 4451-4463 (2010).