Lersivirine(UK 453061)

Product Name: Lersivirine(UK 453061)
CAS No.: 473921-12-9
Chemical Name: Lersivirine(UK 453061)
Synonyms: CS-628;UK 453061;UK 453061; UK453061;Lersivirine(UK 453061);5-((3,5-diethyl-1-(2-hydroxyethyl)-1H-pyrazol-4-yl)oxy)isophthalonitrile;3-Cyano-5-[[3,5-diethyl-1-(2-hydroxyethyl)-1H-pyrazol-4-yl]oxy]benzonitrile;5-[3,5-DIETHYL-1-(2-HYDROXYETHYL)PYRAZOL-4-YL]OXYBENZENE-1,3-DICARBONITRILE;1,3-Benzenedicarbonitrile, 5-[[3,5-diethyl-1-(2-hydroxyethyl)-1H-pyrazol-4-yl]oxy]-;HIV,non-nucleoside reverse transcription,Reverse Transcriptase,HIV virus,UK 453061,Inhibitor,Lersivirine,UK453061,Human immunodeficiency virus,inhibit,resistant strain,NNRTI,NNRTI-resistant
CBNumber: CB62484893
Molecular Formula: C17H18N4O2
Formula Weight: 310.35
MOL File: 473921-12-9.mol

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Lersivirine(UK 453061) Property

Boiling point:: 455.4±45.0 °C(Predicted)
Density: 1.19
storage temp.: Store at -20°C
solubility: Soluble in DMSO
form: Powder
pka: 14.34±0.10(Predicted)
color: Light yellow to khaki

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

ChemScene

Product number: CS-1191
Product name: Lersivirine
Purity: 98.01%
Packaging: 5mg
Price: $144
Updated: 2021/12/16

ApexBio Technology

Product number: A3548
Product name: Lersivirine
Packaging: 10mg
Price: $186
Updated: 2021/12/16

ChemScene

Product number: CS-1191
Product name: Lersivirine
Purity: 98.01%
Packaging: 10mg
Price: $240
Updated: 2021/12/16

American Custom Chemicals Corporation

Product number: API0006072
Product name: UK-453061
Purity: 95.00%
Packaging: 5MG
Price: $298.1
Updated: 2021/12/16

AK Scientific

Product number: 3776AH
Product name: Lersivirine
Packaging: 5mg
Price: $353
Updated: 2021/12/16

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Lersivirine(UK 453061) Chemical Properties,Usage,Production

Definition

ChEBI: Lersivirine is an aromatic ether.

Biological Activity

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].

target

reverse transcriptase

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.

Lersivirine(UK 453061) Preparation Products And Raw materials

Raw materials

Preparation Products

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Lersivirine(UK 453061) Suppliers

China 59 United States 12 Global 71

AdooQ BioScience, LLC

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NE Scientific

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View Lastest Price from Lersivirine(UK 453061) manufacturers

Career Henan Chemical Co

Product: 3-Cyano-5-[[3,5-diethyl-1-(2-hydroxyethyl)-1H-pyrazol-4-yl]oxy]benzonitrile 473921-12-9
Price: US $1.00/g
Min. Order: 1g
Purity: ≥98%
Supply Ability: g/kg/Ton
Release date: 2019-12-25

473921-12-9, Lersivirine(UK 453061)Related Search:

DIETHYLALUMINUM CHLORIDE N-NITROSODIETHYLAMINE Diethyl hydrazine Ethylenediaminetetraacetic acid

Lersivirine(UK 453061)

5-[3,5-DIETHYL-1-(2-HYDROXYETHYL)PYRAZOL-4-YL]OXYBENZENE-1,3-DICARBONITRILE

3-Cyano-5-[[3,5-diethyl-1-(2-hydroxyethyl)-1H-pyrazol-4-yl]oxy]benzonitrile

UK 453061

UK 453061; UK453061

CS-628

5-((3,5-diethyl-1-(2-hydroxyethyl)-1H-pyrazol-4-yl)oxy)isophthalonitrile

1,3-Benzenedicarbonitrile, 5-[[3,5-diethyl-1-(2-hydroxyethyl)-1H-pyrazol-4-yl]oxy]-

HIV,non-nucleoside reverse transcription,Reverse Transcriptase,HIV virus,UK 453061,Inhibitor,Lersivirine,UK453061,Human immunodeficiency virus,inhibit,resistant strain,NNRTI,NNRTI-resistant

473921-12-9