Lersivirine | B3305

Lersivirine is a non-nucleoside, next generation reverse transcriptase inhibitor (IC50 = 118 nM for the wild-type HIV-1 enzyme). 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 displays synergistic or additive effects when used in combination with a variety of antiretroviral agents.

Lersivirine is a non-nucleoside, next generation reverse transcriptase inhibitor (IC50 = 118 nM for the wild-type HIV-1 enzyme). 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 displays synergistic or additive effects when used in combination with a variety of antiretroviral agents.

B3305 | Lersivirine DataSheet

Alternate Name/Synonyms: UK-453,061 5-[[3,5-diethyl-1-(2-hydroxyethyl)-1H-pyrazol-4-yl]oxy]-1,3-benzenedicarbonitrile

Appearance: Off-white to yellow to light brown powder

Formulation:

CAS Number: 473921-12-9

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₁₇H₁₈N₄O₂

Molecular Weight: 310.35

Cell-Permeable?: TRUE

Purity: ≥98%

Solubilities: ~30 mg/ml DMSO

Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.

Country of Origin: USA

Tag Line: A non-nucleoside reverse transcriptase inhibitor

MDL Number: MFCD16619314

PubChem CID: 16739244

SMILES: CCC1=C(C(CC)=NN1CCO)OC2=CC(C#N)=CC(C#N)=C2

InChi: 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