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| | N1-(2,2,6,6-tetraMethylpiperidin-4-yl)-N2-p-tolyloxalaMide Basic information |
| Product Name: | N1-(2,2,6,6-tetraMethylpiperidin-4-yl)-N2-p-tolyloxalaMide | | Synonyms: | N1-(2,2,6,6-tetraMethylpiperidin-4-yl)-N2-p-tolyloxalaMide;Ethanediamide, N1-(4-methylphenyl)-N2-(2,2,6,6-tetramethyl-4-piperidinyl)-;YYA-021;N1-(4-Methylphenyl)-N2-(2,2,6,6-tetramethyl-4-piperidinyl)ethanediamide;N-(4-Methylphenyl)-N'-(2,2,6,6-tetramethylpiperidin-4-yl)oxalamide;N'-(4-Methylphenyl)-N-(2,2,6,6-tetramethylpiperidin-4-yl)oxamide;N-(2,2,6,6-Tetramethyl-piperidin-4-yl)-N'-p-tolyl-oxalamide;YYA-021 (YYA 021 | | CAS: | 144217-65-2 | | MF: | C18H27N3O2 | | MW: | 317.43 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 144217-65-2.mol |  |
| | N1-(2,2,6,6-tetraMethylpiperidin-4-yl)-N2-p-tolyloxalaMide Chemical Properties |
| 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 |
| | N1-(2,2,6,6-tetraMethylpiperidin-4-yl)-N2-p-tolyloxalaMide Usage And Synthesis |
| 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. |
| | N1-(2,2,6,6-tetraMethylpiperidin-4-yl)-N2-p-tolyloxalaMide Preparation Products And Raw materials |
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