D-Altrononitrile, 2-C-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-2,5-anhydro-, 3,4,6-tris(2-methylpropanoate)

Product NameD-Altrononitrile, 2-C-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-2,5-anhydro-, 3,4,6-tris(2-methylpropanoate)
CAS2647442-13-3
MFC24H31N5O7
MW501.53
EINECS
MOL File2647442-13-3.mol

Chemical Properties

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\|

Safety Information

WGK Germany	WGK 3
Storage Class	11 - Combustible Solids

Usage And Synthesis

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 remdesivir, which is efficiently converted in plasma to active metabolite GS-441524, or 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] Schfer 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

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