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Aplidine
CAS No. 137219-37-5
Aplidine ( Plitidepsin )
产品货号. M28854 CAS No. 137219-37-5
Aplidine 具有针对 SARS-CoV-2 的抗病毒活性(IC90 = 0.88 nM)。 Aplidine 是一种有效的抗癌剂,通过靶向真核翻译延伸因子 1 Alpha 2(EEF1A2,Kd = 80 nM)。
纯度: >98% (HPLC)
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规格 | 价格/人民币 | 库存 | 数量 |
5MG | ¥5897 | 有现货 |
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10MG | ¥7995 | 有现货 |
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25MG | ¥12393 | 有现货 |
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50MG | ¥16038 | 有现货 |
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100MG | 获取报价 | 有现货 |
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200MG | 获取报价 | 有现货 |
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500MG | 获取报价 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称Aplidine
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注意事项本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
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产品简述Aplidine 具有针对 SARS-CoV-2 的抗病毒活性(IC90 = 0.88 nM)。 Aplidine 是一种有效的抗癌剂,通过靶向真核翻译延伸因子 1 Alpha 2(EEF1A2,Kd = 80 nM)。
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产品描述Aplidine possesses antiviral activity against SARS-CoV-2(IC90 = 0.88 nM). Aplidine is a potent anti-cancer agent by targeting eukaryotic translation elongation factor 1 Alpha 2(EEF1A2, Kd = 80?nM).(In Vitro):In hACE2-293T cells, Aplidine exhibits anti–SARS-CoV-2 activity with an IC90 of 0.88 nM. In an established model of human pneumocyte-like cells, Aplidine inhibits SARS-CoV-2 replication with an IC90 of 3.14 nM and a selectivity index of 40.4. Aplidine (20 nM; 1 h) induces a dose-dependent decrease in VEGF secretion in MOLT-4 cells. Aplidine (20 nM; 1 h) does not result in significant inhibition of VEGF-R1 mRNA in normal endothelial cells, which do express VEGFR-1 but do not secrete VEGF.(In Vivo):In BALB/c mice expressing human ACE2, Aplidine significantly reduced SARS-CoV-2 infection. 0.3 mg/kg Aplidine group results in a reduction of nearly 2 log units in SARS-CoV-2 viral titers in the lungs, and the 1 mg/kg group leads to a reduction of 1.5 log units.
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体外实验——
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体内实验Animal Model:BALB/c mice Dosage:0.3 mg/kg; 1 mg/kg Administration:1 day QD at 1 mg/kg; 3days QD at 0.3 mg/kg Result:Showed in vivo antiviral efficacy in mouse models of SARS-CoV-2 infection.
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同义词Plitidepsin
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通路Others
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靶点Other Targets
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受体EP1
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研究领域——
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适应症——
化学信息
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CAS Number137219-37-5
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分子量1110.34
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分子式C57H87N7O15
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纯度>98% (HPLC)
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溶解度In Vitro:?DMSO : 100 mg/mL (90.06 mM)
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SMILESCC[C@@H]([C@@H]1[C@@H](O)CC(O[C@@H](C(C)C)C([C@H](C)C(N[C@@H](CC(C)C)C(N2CCC[C@H]2C(N(C)[C@@H](CC3=CC=C(OC)C=C3)C(O[C@H](C)[C@H](NC([C@H](N(C([C@@H]4CCCN4C(C(C)=O)=O)=O)C)CC(C)C)=O)C(N1)=O)=O)=O)=O)=O)=O)=O)C
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1.McKeown SC, et al. Identification of novel pyrazole acid antagonists for the EP1 receptor. Bioorg Med Chem Lett. 2006 Sep 15;16(18):4767-7Epub 2006 Jul 14.