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YYA-021
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
YYA-021图片
CAS NO:144217-65-2
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
YYA-021是一种抑制HIV进入的小分子CD4模拟物,具有高抗HIV活性和低细胞毒性。
Cas No.144217-65-2
Canonical SMILESCC1=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 tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation 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:
[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.