Glecaprevir
(Synonyms: 格来普韦,ABT-493) 目录号 : GC19165
An HCV NS3/4A protease inhibitor
Cas No.:1365970-03-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | The activity of Glecaprevir, paritaprevir or grazoprevir is determined against nine cell lines each stably transfected with an HCV subgenomic replicon containing NS3 protease from a different HCV genotype using a luciferase reporter assay as described previously. All replicon constructs are bicistronic subgenomic replicons, and the replicon cell lines are generated by introducing these constructs into a Huh-7 human hepatoma-derived cell line. The inhibitory effect of Glecaprevir on HCV replication in replicon cells is determined in Dulbecco's modified eagle medium containing 5% fetal bovine serum with or without 40% human plasma. The EC50 values are determined using nonlinear regression curve[1]. |
References: [1]. Ng TI, et al. In Vitro Antiviral Activity and Resistance Profile of the Next-Generation Hepatitis C Virus NS3/4A Protease Inhibitor Glecaprevir. Antimicrob Agents Chemother. 2017 Oct 30. pii: AAC.01620-17. | |
Glecaprevir is a novel HCV NS3/4A protease inhibitor, with IC50 values ranging from 3.5 to 11.3 nM.
Glecaprevir inhibits the enzymatic activity of HCV genotype 1-6 NS3/4A proteases with half maximal inhibitory concentration (IC50) values ranging from 3.5 to 11.3 nM in a biochemical assay. Glecaprevir inhibites HCV subgenomic stable replicons containing proteases from HCV genotypes 1a, 1b, 2a, 2b, 3a, 4a, 5a, 6a and 6e in Huh-7 cells with 50% effective concentration (EC50) values ranging from 0.21 to 4.6 nM. Glecaprevir is active against a replicon containing protease from genotype 3, the most difficult-to-treat HCV genotype, with an EC50 value of 1.9 nM, which is 10- and 44-fold lower than those for paritaprevir and grazoprevir, respectively. The median Glecaprevir EC50 values against replicons containing these genotype 1a, 1b, 2a, 2b, 3a, 4a, 4d, and 5a clinical samples are 0.08, 0.29, 1.6, 2.2, 2.3, 0.41, 0.17, and 0.12 nM, respectively, with an overall median EC50 value of 0.30 nM (range=0.05~3.8 nM)[1].
References:
[1]. Ng TI, et al. In Vitro Antiviral Activity and Resistance Profile of the Next-Generation Hepatitis C Virus NS3/4A Protease Inhibitor Glecaprevir. Antimicrob Agents Chemother. 2017 Oct 30. pii: AAC.01620-17.
| Cas No. | 1365970-03-1 | SDF | |
| 别名 | 格来普韦,ABT-493 | ||
| Canonical SMILES | O=C([C@H]1N(C([C@@H](NC(O[C@@]2([H])[C@@]3([H])CCC2)=O)C(C)(C)C)=O)C[C@@](OC4=NC5=CC=CC=C5N=C4C(F)(/C=C/CO3)F)([H])C1)N[C@]6([C@H](C(F)F)C6)C(NS(=O)(C7(CC7)C)=O)=O | ||
| 分子式 | C38H46F4N6O9S | 分子量 | 838.87 |
| 溶解度 | DMSO : ≥ 83.3 mg/mL (99.30 mM);Water : < 0.1 mg/mL (insoluble) | 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 | 1.1921 mL | 5.9604 mL | 11.9208 mL |
| 5 mM | 0.2384 mL | 1.1921 mL | 2.3842 mL |
| 10 mM | 0.1192 mL | 0.596 mL | 1.1921 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。