| Identification | Back Directory | [Name]
INDEX NAME NOT YET ASSIGNED | [CAS]
2647442-13-3 | [Synonyms]
GS-621763
SARS-CoV,GS-621763,GS 621763,Inhibitor,SARS coronavirus,inhibit,GS621763 | [Molecular Formula]
C24H31N5O7 | [MOL File]
2647442-13-3.mol | [Molecular Weight]
501.54 |
| Chemical Properties | Back Directory | [density ]
1.37±0.1 g/cm3(Predicted) | [storage temp. ]
4°C, away from moisture and light | [solubility ]
DMSO: 2mg/mL, clear | [form ]
Solid | [pka]
4.11±0.30(Predicted) | [color ]
White to off-white | [InChIKey]
RVSSLHFYCSUAHY-BSVPRABPNA-N | [SMILES]
C([C@@]1(C2=CC=C3C(=NC=NN23)N)O[C@H](COC(=O)C(C)C)[C@@H](OC(=O)C(C)C)[C@H]1OC(=O)C(C)C)#N |&1:1,13,21,28,r| |
| Hazard Information | Back Directory | [Uses]
GS-621763 is an orally available precursor to GS-441524 that exhibits anti-SARS-CoV-2 viral activity in mice. GS-621763 reduces viral load to undetectable levels in ferrets infected with SARS-CoV-2[1][2]. | [Biological Activity]
GS-621763 is an orally bioavailable analog of remdesivirwhich is efficiently converted in plasma to active metabolite GS-441524or in lungs to the bioactive triphosphate GS-443902. GS-621763 effectively reduces SARS-CoV-2 burden to near-undetectable levels in ferrets. | [in vivo]
GS-621763 (30 and 60 mg/kg p.o., twice daily for 4 days) shows potent antiviral activity in SARS-CoV-2 infected BALB/c mouse model[1].
GS-621763 (10 mg/kg, p.o., twice daily for 4 days) shows significant antiviral activity in SARS-CoV-2-infected ferret model[2]. | Animal Model: | SARS-CoV-2 infected BALB/c mouse model[1] | | Dosage: | 30 mg/kg and 60 mg/kg | | Administration: | Oral gavage (p.o.), twice daily for 4 days | | Result: | Significantly reduced lung infectious virus levels (30 mg/kg);
Further reduced ung infectious virus levels (60 mg/kg). |
| Animal Model: | SARS-CoV-2-infected ferret model[2] | | Dosage: | 10 mg/kg | | Administration: | Oral gavage (p.o.), twice daily for 4 days | | Result: | Significantly reduced SARS-CoV-2 shedding, with virus undetectable in nasal lavages. |
| [References]
[1] Sch?fer A, et al. Therapeutic efficacy of an oral nucleoside analog of remdesivir against SARS-CoV-2 pathogenesis in mice. bioRxiv [Preprint]. 2021 Sep 17:2021.09.13.460111. DOI:10.1101/2021.09.13.460111
[2] Cox RM, et al. Oral prodrug of remdesivir parent GS-441524 is efficacious against SARS-CoV-2 in ferrets. Nat Commun. 2021 Nov 5;12(1):6415. DOI:10.1038/s41467-021-26760-4 |
|
|