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ChemicalBook--->CAS DataBase List--->144217-65-2

144217-65-2

144217-65-2 Structure

144217-65-2 Structure
IdentificationBack Directory
[Name]

N1-(2,2,6,6-tetraMethylpiperidin-4-yl)-N2-p-tolyloxalaMide
[CAS]

144217-65-2
[Synonyms]

YYA-021
CS-2313
YYA-021 (YYA 021
N1-(2,2,6,6-tetraMethylpiperidin-4-yl)-N2-p-tolyloxalaMide
N-(2,2,6,6-Tetramethyl-piperidin-4-yl)-N'-p-tolyl-oxalamide
N'-(4-Methylphenyl)-N-(2,2,6,6-tetramethylpiperidin-4-yl)oxamide
N-(4-Methylphenyl)-N'-(2,2,6,6-tetramethylpiperidin-4-yl)oxalamide
N1-(4-Methylphenyl)-N2-(2,2,6,6-tetramethyl-4-piperidinyl)ethanediamide
Ethanediamide, N1-(4-methylphenyl)-N2-(2,2,6,6-tetramethyl-4-piperidinyl)-
[Molecular Formula]

C18H27N3O2
[MDL Number]

MFCD00738763
[MOL File]

144217-65-2.mol
[Molecular Weight]

317.43
Chemical PropertiesBack Directory
[density ]

1.11±0.1 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

Limited solubility
[form ]

Powder
[pka]

11.61±0.70(Predicted)
[color ]

White to off-white
Safety DataBack Directory
[Symbol(GHS) ]


GHS07,GHS09
[Signal word ]

Warning
[Hazard statements ]

H302-H315-H319-H335-H400-H410
[Precautionary statements ]

P261-P264-P270-P271-P273-P280-P301+P312-P330-P302+P352-P321-P304+P340-P305+P351+P338-P332+P313-P362+P364-P337+P313-P391-P403+P233-P405-P501
Hazard InformationBack Directory
[Uses]

YYA-021 is a small molecule CD4 mimic HIV entry inhibitor that can suppress competitively the interaction between an HIV-1 envelope glycoprotein gp120 and a cellular surface protein CD4.
[Biological Activity]

yya-021 is a small-molecule cd4 mimic that inhibits hiv entry [1].cd4 is a cell surface protein. the entry of human immunodeficiency virus type 1 (hiv-1) into target cells is initiated by the interaction of cd4 and viral envelope glycoprotein gp120. cd4 mimic inhibits the interaction between gp120 and cd4 and then inhibits hiv entry [1].yya-021 is a small-molecule cd4 mimic that inhibits hiv entry. yya-021 competitively inhibited gp120-cd4 interaction [1]. in tzm-bl cells infected with simian-human immunodeficiency virus isolate mna (shiv mna) or hiv-1 mna pseudotyped viruses, yya-021 inhibited the entry of envs of shiv mna and hiv-1. kd-247 (the anti-v3 loop mab, 50 μg) caused 50% neutralization of hiv-1 mna. however, in the presence of 20 μm of yya-021, kd-247 (<0.05 μg) caused 50% neutralization of hiv-1 mna, which suggested that the synergistic neutralization effect of yya-021 and kd-247. in the presence of yya-021, shiv mna became more sensitive to igg [2].in jcl:sd rats, the maximum tolerated dose of yya-021.hcl was 2.5 mg. when administrated by tail vein injection, yya-021 exhibited widespread tissue distribution due to its hydrophobicity. in a rhesus macaque, the maximum tolerated dose of yya-021.hcl was 35.3 mg [1].
[target]

gp120-CD4 interaction
[References]

[1]. hashimoto c, narumi t, otsuki h, et al. a cd4 mimic as an hiv entry inhibitor: pharmacokinetics. bioorg med chem, 2013, 21(24): 7884-7889.
[2]. otsuki h, hishiki t, miura t, et al. generation of a replication-competent simian-human immunodeficiency virus, the neutralization sensitivity of which can be enhanced in the presence of a small-molecule cd4 mimic. j gen virol, 2013, 94(pt 12): 2710-2716.
Spectrum DetailBack Directory
[Spectrum Detail]

N1-(2,2,6,6-tetraMethylpiperidin-4-yl)-N2-p-tolyloxalaMide(144217-65-2)1HNMR
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