GS-6620
Based on 1 Customer Validation
GS-6620 is potent and selective HCV inhibitor. GS-6620 inhibits HCV replication in genotype 1-6 subgenomic replicons and genotype 2a infectious virus, with EC50 values of 0.048-0.68 μM. GS-6620 can be used for the researches of infection and inflammation, such as Hepatitis C Virus (HCV).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 98.93%
- CAS 番号: 1350735-70-4
- 分子式: C29H37N6O9P
- 分子量:644.61
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
製品説明
IC50 & Target
[1]|
GT3a 0.048 μM (EC50) |
GT4a 0.11 μM (EC50) |
GT6a 0.11 μM (EC50) |
GT5a 0.14 μM (EC50) |
GT1a 0.18 μM (EC50) |
GT1b 0.46 μM (EC50) |
GT2a 0.68 μM (EC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | EC50 |
>20 μM
Compound: 13b
|
Antiviral activity against Ebolavirus Kikwit infected in human HeLa cells assessed as reduction in viral glycoprotein levels preincubated with cells for 2 hrs followed by viral infection measured after 48 hrs by immunostaining based assay
Antiviral activity against Ebolavirus Kikwit infected in human HeLa cells assessed as reduction in viral glycoprotein levels preincubated with cells for 2 hrs followed by viral infection measured after 48 hrs by immunostaining based assay
|
[PMID: 28124907] |
| HEp-2 | CC50 |
95 μM
Compound: 13b
|
Cytotoxicity against human Hep2 cells assessed as reduction in cell viability after 4 to 5 days by Cell-Titer Glo assay
Cytotoxicity against human Hep2 cells assessed as reduction in cell viability after 4 to 5 days by Cell-Titer Glo assay
|
[PMID: 28124907] |
| Huh-7 | CC50 |
47 μM
Compound: 16
|
Cytotoxicity against human HuH7 cells after 3 days by fluorescence assay
Cytotoxicity against human HuH7 cells after 3 days by fluorescence assay
|
[PMID: 23547794] |
| Huh-7 | CC50 |
51 μM
Compound: 13b
|
Cytotoxicity against human HuH7 cells assessed as reduction in cell viability after 3 days by calcein-AM dye based fluorescence assay
Cytotoxicity against human HuH7 cells assessed as reduction in cell viability after 3 days by calcein-AM dye based fluorescence assay
|
[PMID: 28124907] |
| Huh-7 | EC50 |
0.61 μM
Compound: 16
|
Antiviral activity against HCV genotype 1b infected in human HuH7 cells assessed as inhibition of viral replication after 3 days by luminescence assay
Antiviral activity against HCV genotype 1b infected in human HuH7 cells assessed as inhibition of viral replication after 3 days by luminescence assay
|
[PMID: 23547794] |
| MT4 | CC50 |
7.8 μM
Compound: 13b
|
Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 to 5 days by Cell-Titer Glo assay
Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 to 5 days by Cell-Titer Glo assay
|
[PMID: 28124907] |
体外実験
GS-6620 (72 h) inhibits HCV replication in genotype 1-6 subgenomic replicons and genotype 2a infectious virus, with EC50 values of 0.048-0.68 μM and shows weak activity against bovine viral diarrhea virus (BVDV, EC50 = 1.5 μM)[1].
GS-6620 (active metabolite) (0.39-1.3 μM, 70-90 mins) inhibits HCV NS5B polymerase[1].
GS-6620 (0-100 μM, 5 days) shows low cytotoxicity in Huh-7, HepG2, PC-3 and PBMCs with CC50 values of 67, 66, 40 and >100 μM[1].
GS-6620 (20-100 μM, 5-10 days) does not reduce mitochondrial DNA content in HepG2 cells or inhibit mitochondrial protein synthesis in PC-3 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1350735-70-4
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性状 Solid
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分子量 644.61
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分子式 C29H37N6O9P
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Color White to off-white
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SMILES
NC1=NC=NN2C1=CC=C2[C@@]3(C#N)[C@@](O)(C)[C@H](OC(C(C)C)=O)[C@@H](CO[P@](OC4=CC=CC=C4)(N[C@@H](C)C(OC(C)C)=O)=O)O3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : ≥ 100 mg/mL (155.13 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Joy Y Feng, et al. Inhibition of hepatitis C virus replication by GS-6620, a potent C-nucleoside monophosphate prodrug. Antimicrob Agents Chemother. 2014;58(4):1930-42. [Content Brief]
[2]. Cho A, et al. Discovery of the first C-nucleoside HCV polymerase inhibitor (GS-6620) with demonstrated antiviral response in HCV infected patients. J Med Chem. 2014 Mar 13;57(5):1812-25. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5513 mL | 7.7566 mL | 15.5133 mL | 38.7831 mL |
| 5 mM | 0.3103 mL | 1.5513 mL | 3.1027 mL | 7.7566 mL | |
| 10 mM | 0.1551 mL | 0.7757 mL | 1.5513 mL | 3.8783 mL | |
| 15 mM | 0.1034 mL | 0.5171 mL | 1.0342 mL | 2.5855 mL | |
| 20 mM | 0.0776 mL | 0.3878 mL | 0.7757 mL | 1.9392 mL | |
| 25 mM | 0.0621 mL | 0.3103 mL | 0.6205 mL | 1.5513 mL | |
| 30 mM | 0.0517 mL | 0.2586 mL | 0.5171 mL | 1.2928 mL | |
| 40 mM | 0.0388 mL | 0.1939 mL | 0.3878 mL | 0.9696 mL | |
| 50 mM | 0.0310 mL | 0.1551 mL | 0.3103 mL | 0.7757 mL | |
| 60 mM | 0.0259 mL | 0.1293 mL | 0.2586 mL | 0.6464 mL | |
| 80 mM | 0.0194 mL | 0.0970 mL | 0.1939 mL | 0.4848 mL | |
| 100 mM | 0.0155 mL | 0.0776 mL | 0.1551 mL | 0.3878 mL |