VV116
- Product Name
- VV116
- CAS No.
- 2647442-33-7
- Chemical Name
- VV116
- Synonyms
- VV116;Remindevir-d1;Mindeudesivir;VV116, 10 mM in DMSO;D-Altrononitrile, 2-C-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl-5-d)-2,5-anhydro-, 3,4,6-tris(2-methylpropanoate) (;(3R,4R,5R)-2-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl-5-d)-2-cyano-5-((isobutyryloxy)methyl)tetrahydrofuran-3,4-diyl bis(2-methylpropanoate)
- CBNumber
- CB49734801
- Molecular Formula
- C24H30DN5O7
- Formula Weight
- 502.54
- MOL File
- 2647442-33-7.mol
VV116 Property
- Density
- 1.375±0.14 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted)
- solubility
- DMF: 20 mg/ml; DMSO: 12 mg/ml; Ethanol: Slightly soluble
- form
- A solid
- pka
- 4.110±0.30(predicted)
- color
- White to off-white
- InChIKey
- RVSSLHFYCSUAHY-QXMJNOOVSA-N
- SMILES
- C([C@@]1(C2=CC([2H])=C3C(=NC=NN23)N)O[C@@H]([C@H]([C@H]1OC(=O)C(C)C)OC(=O)C(C)C)COC(=O)C(C)C)#N
VV116 Chemical Properties,Usage,Production
Description
VV116, also known as JT001, is an oral drug candidate of nucleoside analog against SARS-CoV-2. VV116 is a deuterated, tri-isobutyrate ester prodrug of the RDV parent nucleoside, and is rapidly metabolized into the parent nucleoside (116-N1) in the body. 116-N1 is intracellularly converted to the nucleoside triphosphate active form, which would interfere with the function of RNA-dependent RNA polymerase of SARS-CoV-2, thus exerting antiviral effects (Fig. 1). VV116 showed potent activity against a panel of SARS-CoV-2 variants (alpha, beta, delta, and omicron) and excellent therapeutic efficacy in the mice model.
Uses
GS-621763-d1 is the deuterium labeled GS-621763 (HY-145119)[1]. GS-621763, an orally bioavailable proagent of GS-441524, shows antiviral activity against SARS-CoV-2 pathogenesis in mice[2].
References
[1] Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. DOI:10.1177/1060028018797110
[2] 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
VV116 Preparation Products And Raw materials
Raw materials
Preparation Products
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