GS-443902
Based on 13 publication(s) in Google Scholar
GS-443902 (GS-441524 triphosphate) is a potent viral RNA-dependent RNA-polymerases (RdRp) inhibitor with IC50s of 1.1 µM, 5 µM for RSV RdRp and HCV RdRp, respectively. GS-443902 is the active triphosphate metabolite of Remdesivir.
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。
- CAS 番号: 1355149-45-9
- 分子式: C12H16N5O13P3
- 分子量:531.20
-
保管条件:
-20°C, stored under nitrogen
* The compound is unstable in solutions, freshly prepared is recommended.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 GS-443902
More- Cell. 2022 Nov 10;185(23):4347-4360.e17. [Abstract]
- Nat Commun. 2021 Oct 4;12(1):5811. [Abstract]
- Acta Pharm Sin B. 2021 Jun;11(6):1607-1616. [Abstract]
- J Control Release. 2025 Nov 10:387:114245. [Abstract]
- EMBO J. 2025 Jan;44(2):563-586. [Abstract]
- J Med Chem. 2025 Jun 26;68(12):12414-12433. [Abstract]
- J Med Chem. 2024 May 9;67(9):7470-7486. [Abstract]
- Int J Mol Sci. 2022 Jul 27;23(15):8302. [Abstract]
- Chem Biol Interact. 2021 Jul 1:343:109480. [Abstract]
- Sci Rep. 2022 Nov 2;12(1):18506. [Abstract]
- Research Square Preprint. 2022 May.
- Curr Res Pharmacol Drug Discov. 2021:2:100045. [Abstract]
- bioRxiv. 2021 Jul 21:2021.07.21.453274. [Abstract]
DNA/RNA Synthesis アイソフォーム固有の製品をすべて表示
More
生物活性
製品説明
IC50 & Target
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
>200 μM
Compound: 4tp
|
Inhibition of RNA polymerase 2 in human HeLa cells preincubated for 5 mins with dATP/dGTP/dTTP as substrate followed by addition of cell extract measured after 1 hr by SDS-PAGE method
Inhibition of RNA polymerase 2 in human HeLa cells preincubated for 5 mins with dATP/dGTP/dTTP as substrate followed by addition of cell extract measured after 1 hr by SDS-PAGE method
|
[PMID: 28124907] |
体外実験
In a continuous 72 h incubation of 1 µM Remdesivir (GS-5734), the GS-443902 (GS-441524 triphosphate; Remdesivir metabolite; compound 4tp) level is measured at 2, 24, 48 and 72 h, and reaches a Cmax of 300, 110, and 90 pmol/million cells in macrophages, HMVEC, and HeLa cells lines respectively[1].
GS-443902 (compound 8a) is a triphosphates (TP) derivative[2].
GS-443902 (NTP; 0.01, 0.1, 1, 10, 100 μM) inhibits RSV RdRp-catalysed RNA synthesis by incorporating into the nascent viral RNA transcript and causing its premature termination. GS-5734 selectively inhibits EBOV replication by targeting its RdRp and inhibiting viral RNA synthesis following efficient intracellular conversion to GS-443902[3].
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.
化学情報
-
CAS 番号 1355149-45-9
-
性状 Solid
-
分子量 531.20
-
分子式 C12H16N5O13P3
-
Color Light yellow to yellow
-
SMILES
O=P(OP(O)(O)=O)(O)OP(OC[C@@H](O1)[C@@H](O)[C@@H](O)[C@]1(C#N)C2=CC=C3N2N=CN=C3N)(O)=O
-
別名
GS-441524 triphosphate; Remdesivir metabolite
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
-20°C, stored under nitrogen
* The compound is unstable in solutions, freshly prepared is recommended.
Publications (13)
-
Journal Impact Factor
-
Most Recent
-
Cell
A mechanism for SARS-CoV-2 RNA capping and its inhibition by nucleotide analog inhibitors. [Abstract]2022 Nov 10;185(23):4347-4360.e17. PMID: 36335936 -
Nat Commun
2021 Oct 4;12(1):5811. PMID: 34608151 -
Acta Pharm Sin B
Can remdesivir and its parent nucleoside GS-441524 be potential oral drugs? An in vitro and in vivo DMPK assessment. [Abstract]2021 Jun;11(6):1607-1616. PMID: 34221871 -
J Control Release
A general nanoplatform for nucleotide drug delivery: From molecular binding to antiviral therapy. [Abstract]2025 Nov 10:387:114245. PMID: 40975176 -
EMBO J
2025 Jan;44(2):563-586. PMID: 39739115 -
J Med Chem
Identification of 4'-Thiouridine as an Orally Available Antiviral Agent Targeting Both RdRp and NiRAN Functions of SARS-CoV-2 Nsp12. [Abstract]2025 Jun 26;68(12):12414-12433. PMID: 40512093 -
J Med Chem
Differential Bioactivation Profiles of Different GS-441524 Prodrugs in Cell and Mouse Models: ProTide Prodrugs with High Cell Permeability and Susceptibility to Cathepsin A Are More Efficient in Delivering Antiviral Active Metabolites to the Lung. [Abstract]2024 May 9;67(9):7470-7486. PMID: 38690769 -
Int J Mol Sci
A Systematic Study on the Optimal Nucleotide Analogue Concentration and Rate Limiting Nucleotide of the SARS-CoV-2 RNA-Dependent RNA Polymerase. [Abstract]2022 Jul 27;23(15):8302. PMID: 35955442 -
Chem Biol Interact
2021 Jul 1:343:109480. PMID: 33887223 -
Sci Rep
Discovery of SARS-CoV-2 antiviral synergy between remdesivir and approved drugs in human lung cells. [Abstract]2022 Nov 2;12(1):18506. PMID: 36323770 -
-
Curr Res Pharmacol Drug Discov
Comparison of anti-SARS-CoV-2 activity and intracellular metabolism of remdesivir and its parent nucleoside. [Abstract]2021:2:100045. PMID: 34870151 -
bioRxiv
Combination of Antiviral Drugs to Inhibit SARS-CoV-2 Polymerase and Exonuclease as Potential COVID-19 Therapeutics. [Abstract]2021 Jul 21:2021.07.21.453274. PMID: 34312622
溶剤 & 溶解度
体外:
H2O : 100 mg/mL (188.25 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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
-
データシート (277 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
取扱説明書 (2659 KB)
参考文献
[1]. Siegel D, et al. Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses. Med Chem. 2017 Mar 9;60(5):1648-1661. [Content Brief]
[2]. Cho A, et al. Synthesis and antiviral activity of a series of 1'-substituted 4-aza-7,9-dideazaadenosine C-nucleosides. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2705-7. [Content Brief]
[3]. Warren TK, et al. Therapeutic efficacy of the small molecule GS-5734 against Ebola virus in rhesus monkeys. Nature. 2016 Mar 17;531(7594):381-5. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 1.8825 mL | 9.4127 mL | 18.8253 mL | 47.0633 mL |
| 5 mM | 0.3765 mL | 1.8825 mL | 3.7651 mL | 9.4127 mL | |
| 10 mM | 0.1883 mL | 0.9413 mL | 1.8825 mL | 4.7063 mL | |
| 15 mM | 0.1255 mL | 0.6275 mL | 1.2550 mL | 3.1376 mL | |
| 20 mM | 0.0941 mL | 0.4706 mL | 0.9413 mL | 2.3532 mL | |
| 25 mM | 0.0753 mL | 0.3765 mL | 0.7530 mL | 1.8825 mL | |
| 30 mM | 0.0628 mL | 0.3138 mL | 0.6275 mL | 1.5688 mL | |
| 40 mM | 0.0471 mL | 0.2353 mL | 0.4706 mL | 1.1766 mL | |
| 50 mM | 0.0377 mL | 0.1883 mL | 0.3765 mL | 0.9413 mL | |
| 60 mM | 0.0314 mL | 0.1569 mL | 0.3138 mL | 0.7844 mL | |
| 80 mM | 0.0235 mL | 0.1177 mL | 0.2353 mL | 0.5883 mL | |
| 100 mM | 0.0188 mL | 0.0941 mL | 0.1883 mL | 0.4706 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
GS-443902 関連分類
HY-126303 関連分類
Powered by Bioz