| CAS NO: | 144217-65-2 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| Cas No. | 144217-65-2 |
| Canonical SMILES | CC1=CC=C(C=C1)NC(=O)C(=O)NC2CC(NC(C2)(C)C)(C)C |
| 分子式 | C18H27N3O2 |
| 分子量 | 317.43 |
| 溶解度 | DMF: 12 mg/ml,DMF:PBS (pH7.2) (1:30): 0.03 mg/ml,DMSO: 5 mg/ml,Ethanol: 0.125 mg/ml |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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]. References: |
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