ChemicalBook > CAS DataBase List > Lersivirine(UK 453061)

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

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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