HeE1-2Tyr
目录号 : GC63500
HeE1-2Tyr 是一种 pyridobenzothiazole，是一种黄病毒 RNA 依赖性 RNA 聚合酶 (RdRp) 抑制剂。HeE1-2Tyr 在体外显着抑制西尼罗河、登革热和 SARS-CoV-2 RdRps (IC50 为 27.6 µM) 的活性。
Cas No.:2245195-67-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >96.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
HeE1-2Tyr, a pyridobenzothiazole compound, is a flavivirus RNA dependent RNA polymerases (RdRp) inhibitor. HeE1-2Tyr significantly inhibits West Nile, Dengue and SARS-CoV-2 RdRps (IC50 of 27.6 µM) activity in vitro[1][2].
HeE1-2Tyr shows antiviral activity, it is able to inhibit an Ugandan strain of West Nile virus with an IC50 of 2.1 µM, as well as all the four Dengue virus (DENV) serotypes, with IC50 ranging from 6.8 to 15 µM. The cytotoxicity of HeE1-2Tyr versus Vero E6 cells is ~115 µM[1].Additionally, upon infection of human HEK 293 cells (CC50 of 50 µM), HeE1-2Tyr inhibits clinical strains of yellow fever virus with IC50 values ranging from 3.9 to 12 µM[1]. HeE1-2Tyr completely inhibits the replication of both SARS-CoV-2 and Feline coronavirus (FIPV)[2].
[1]. Delia Tarantino, et al. Targeting flavivirus RNA dependent RNA polymerase through a pyridobenzothiazole inhibitor. Antiviral Res. 2016 Oct;134:226-235.
[2]. Milan Dejmek, et al. Non-Nucleotide RNA-Dependent RNA Polymerase Inhibitor That Blocks SARS-CoV-2 Replication. Viruses. 2021 Aug 11;13(8):1585.
| Cas No. | 2245195-67-7 | SDF | |
| 分子式 | C33H30N2O6S | 分子量 | 582.67 |
| 溶解度 | DMSO : 100 mg/mL (171.62 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7162 mL | 8.5812 mL | 17.1624 mL |
| 5 mM | 0.3432 mL | 1.7162 mL | 3.4325 mL |
| 10 mM | 0.1716 mL | 0.8581 mL | 1.7162 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Non-Nucleotide RNA-Dependent RNA Polymerase Inhibitor That Blocks SARS-CoV-2 Replication
Viruses 2021 Aug 11;13(8):1585.PMID:34452451DOI:10.3390/v13081585.
SARS-CoV-2 has caused an extensive pandemic of COVID-19 all around the world. Key viral enzymes are suitable molecular targets for the development of new antivirals against SARS-CoV-2 which could represent potential treatments of the corresponding disease. With respect to its essential role in the replication of viral RNA, RNA-dependent RNA polymerase (RdRp) is one of the prime targets. HeE1-2Tyr and related derivatives were originally discovered as inhibitors of the RdRp of flaviviruses. Here, we present that these pyridobenzothiazole derivatives also significantly inhibit SARS-CoV-2 RdRp, as demonstrated using both polymerase- and cell-based antiviral assays.
Targeting flavivirus RNA dependent RNA polymerase through a pyridobenzothiazole inhibitor
Antiviral Res 2016 Oct;134:226-235.PMID:27649989DOI:10.1016/j.antiviral.2016.09.007.
RNA dependent RNA polymerases (RdRp) are essential enzymes for flavivirus replication. Starting from an in silico docking analysis we identified a pyridobenzothiazole compound, HeE1-2Tyr, able to inhibit West Nile and Dengue RdRps activity in vitro, which proved effective against different flaviviruses in cell culture. Crystallographic data show that HeE1-2Tyr binds between the fingers domain and the priming loop of Dengue virus RdRp (Site 1). Conversely, enzyme kinetics, binding studies and mutational analyses suggest that, during the catalytic cycle and assembly of the RdRp-RNA complex, HeE1-2Tyr might be hosted in a distinct binding site (Site 2). RdRp mutational studies, driven by in silico docking analysis, allowed us to locate the inhibition Site 2 in the thumb domain. Taken together, our results provide innovative concepts for optimization of a new class of anti-flavivirus compounds.