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Antiviral API
- Arenavirus
- Cytomegalovirus (CMV)
- Dengue virus
- Endogenous Metabolite
- Enterovirus (EV)
- Epstein-Barr virus (EBV)
- Filovirus
- Flavivirus
- HCV Protease
- Hepatitis B Virus (HBV)
- Hepatitis C Virus (HCV)
- Herpes simplex Virus (HSV)
- HIF/HIF Prolyl-Hydroxylase
- HIV Integrase
- HIV Protease
- Human immunodeficiency Virus (HIV)
- Human papillomavirus (HPV)
- Influenza Virus
- Nipah virus
- Orthopoxvirus
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- Rabies virus (RABV)
- Respiratory syncytial Virus (RSV)
- Reverse Transcriptases (RTs)
- SARS-CoV
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- Vesicular stomatitis virus (VSV)
- Virus Protease
- West Nile virus
- Antiviral intermediates
GS-443902
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| Category | Hepatitis C Virus (HCV) |
| CAS | 1355149-45-9 |
| Description | GS-443902 is a potent inhibitor of viral RNA-dependent RNA-polymerases (RdRp), with IC50s of 1.1 µM, 5 µM for RSV RdRp and HCV RdRp, respectively. |
Product Information
| Synonyms | GS-441524 triphosphate; Remdesivir metabolite; RDV-TP |
| IUPAC Name | [[(2R,3S,4R,5R)-5-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-5-cyano-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate |
| Molecular Weight | 531.20 |
| Molecular Formula | C12H16N5O13P3 |
| Canonical SMILES | C1=C2C(=NC=NN2C(=C1)C3(C(C(C(O3)COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O)O)C#N)N |
| InChI | InChI=1S/C12H16N5O13P3/c13-4-12(8-2-1-6-11(14)15-5-16-17(6)8)10(19)9(18)7(28-12)3-27-32(23,24)30-33(25,26)29-31(20,21)22/h1-2,5,7,9-10,18-19H,3H2,(H,23,24)(H,25,26)(H2,14,15,16)(H2,20,21,22)/t7-,9-,10-,12+/m1/s1 |
| InChIKey | DFVPCNAMNAPBCX-LTGWCKQJSA-N |
| Purity | 99.87% |
| Density | 2.4±0.1 g/cm3 |
| Solubility | In Vitro: H2O : 100 mg/mL(188.25 mM;Need ultrasonic) |
| Appearance | Light yellow to yellow (Solid) |
| Application | Antiviral Agents |
| Storage | -20°C, stored under nitrogen * In solvent : -80°C 6 months -20°C 1 month (stored under nitrogen) |
| Complexity | 941 |
| Exact Mass | 530.99574658 |
| Index Of Refraction | 1.841 |
| In Vitro | GS-443902 (compound 8a), a triphosphates (TP) derivative, is a potent inhibitory activity against the enzyme TP RdRp (IC50=5.6 µM). In a continuous 72 h incubation of 1 µM GS-5734, the GS-443902 (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. 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. |
| In Vivo | GS-5734 (10 mg kg; i.v.) rapidly distributes into peripheral blood mononuclear cells (PBMCs), and efficient conversion to GS-443902 (NTP) is apparent within 2 h of dose administration in rhesus monkeys. In PBMCs, GS-443902 represents the predominant metabolite and is persistent with a t1/2 of 14 h and levels required for >50% virus inhibition for 24 hours. |
| Target | DNA/RNA Synthesis; SARS-CoV; RSV; HCV; Drug Metabolite |
| XLogP3-AA | -5.3 |
