| Identification | Back 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 Properties | Back 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) |
| Hazard Information | Back 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. |
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