- Emtricitabine
- Lamivudine
- Delavirdine mesylate
- Nevirapine
- Tenofovir
- Zalcitabine
| LersivirineNNRT inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Description | Lersivirine (UK-453061) is a next-generation non-nucleoside inhibitor of reverse transcriptase under development for the treatment of HIV-1 infection. | |||||
| Targets | reverse transcriptase | |||||
| IC50 | ||||||
Lersivirine Dilution Calculator
calculate
Lersivirine Molarity Calculator
calculate
| Cas No. | 473921-12-9 | SDF | Download SDF |
| Synonyms | UK-453061;UK453061;UK 453061 | ||
| Chemical Name | 5-[3,5-diethyl-1-(2-hydroxyethyl)pyrazol-4-yl]oxybenzene-1,3-dicarbonitrile | ||
| Canonical SMILES | CCC1=C(C(=NN1CCO)CC)OC2=CC(=CC(=C2)C#N)C#N | ||
| Formula | C17H18N4O2 | M.Wt | 310.35 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Lersivirine (UK-453061) is a next-generation non-nucleoside reverse transcriptase inhibitor (NNRTI)for human immunodeficincy virus (HIV) infection with IC50 value of 119 nM [1].
HIV is a retro virus that causes HIV infection and acquired immunodeficiency syndrome (AIDS). It may infect vital cells of human immune system such as helper T cells and dendritic cells. HIV transcriptase plays an important role in the infection process. HIV carries a reverse transcriptase which can transcript single-stranded virus RNA into double-stranded DNA. When the virus anchor to the target cell surface, the reverse transcriptase will be injected into host cell, there it may complete the transcription. And the transcribed DNA is able to integrate into host genome to complete infection and viral replication.
Lersivirine (UK-453061) is a NNRTI with a unique resistance profile that exhibits potent antiretroviral activity against wild-type HIV and clinically relevant NNRTI-resistant strains. When lersivirine was tested with a panel of isolated wild-type and drug-resistant HIV reverse transcriptase, it exhibited excellent inhibitory activity, which confirmed the high potency of it as the next-generation anti-HIV NNRTI. The compound also has good aqueous solubility and formulation characteristics which enable further in vivo evaluation [2].
Mated Crl:CD1 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. Exposure of lersivirine did not cause any increases in external, visceral, or skeletal malformation, which demonstrated lersivirine is not teratogenic in mice [3].
References:[1] Mowbray C E et al., Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate. Bioorg Med Chem Lett. 2009, 19(20):5857-60.[2] Davis J et al., The effect of lersivirine, a next-generation NNRTI, on the pharmacokinetics of midazolam and oral contraceptives in healthy subjects. Eur J Clin Pharmacol. 2012, 68(11):1567-1572.[3]Cappon G D et al., Developmental toxicity study of lersivirine in mice. Birth Defects Res B Dev Reprod Toxicol. 2012, 95(3):225-30.
