| YYA-021Competitive gp120-CD4 interaction inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Description | YYA-021 is a competitive inhibitor of the gp120-CD4 interaction. | |||||
| Targets | gp120-CD4 interaction | |||||
| IC50 | ||||||
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| Cas No. | 144217-65-2 | SDF | Download SDF |
| Canonical SMILES | CC1=CC=C(C=C1)NC(=O)C(=O)NC2CC(NC(C2)(C)C)(C)C | ||
| Formula | C18 H27 N3 O2 | M.Wt | 317.43 |
| Solubility | Limited solubility | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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="">
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.
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请赐教！
荚膜（capsule）是某些细菌在生长繁殖过程中分泌的一层黏液性物质，包围在细胞壁外，通常这种黏液层厚度小于0.2μm，成分是多糖或多肽，只有在营养丰富时或在动物体内，细菌才产生这种半抗原性质的黏液性物质。它具有保护菌体免受巨噬细胞等的捕捉和吞噬，因而具有抗吞噬抗消化、侵袭力强、与致病性关系密切等特点。像肺炎球菌、炭疽杆菌等都有这类荚膜。有些细菌的荚膜层较薄，小于0.2μm，称为微荚。
像链球菌的M蛋白、伤寒杆菌的Vi抗原、大肠杆菌的K抗原等都属于这类微荚膜。
颗粒型抗原,除了有细菌、红细胞、螺旋体等天然颗粒型抗原,还有吸附有可溶性抗原的非免疫相关颗粒.
颗粒性抗原光镜下可见，比如细菌性抗原、红细胞抗原等；而可溶性抗原在光镜下不可见，如组织浸出液、细菌毒素、蛋白质分子等。
它们不等同于完全抗原和不完全抗原。完全抗原具有免疫原性和抗原性，而不完全抗原只具有抗原性。完全抗原可以是颗粒性抗原，亦可是可溶性抗原，而不完全抗原一般只能是可溶性抗原，不会是颗粒性抗原。
若已进入细胞内。则先由巨噬细胞吞噬降解。并形成抗原-MHC复合体传送到表面。被辅助性T淋巴细胞识别和效应T淋巴细胞识别后。效应T淋巴细胞被激活。分解靶细胞。然后再由效应B细胞分泌的抗体进一步消灭病毒。
还有不清楚的么？
