VV116

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.

Product information

CAS Number: 2647442-33-7

Molecular Weight: 502.54

Formula: C24H31N5O7

Chemical Name: (2R, 3R, 4R, 5R)-2-(4-amino-5-deuteropyrrolo[2, 1-f][1, 2, 4]triazin-7-yl)-2-cyano-5-((isobutyryloxy)methyl)tetrahydrofuran-3, 4-diyl bis(2-methylpropanoate)

Smiles: [2H]C1C=C(N2N=CN=C(N)C2=1)[C@]1(C#N)O[C@H](COC(=O)C(C)C)[C@@H](OC(=O)C(C)C)[C@H]1OC(=O)C(C)C

InChiKey: RVSSLHFYCSUAHY-QXMJNOOVSA-N

InChi: InChI=1S/C24H31N5O7/c1-12(2)21(30)33-9-16-18(34-22(31)13(3)4)19(35-23(32)14(5)6)24(10-25,36-16)17-8-7-15-20(26)27-11-28-29(15)17/h7-8,11-14,16,18-19H,9H2,1-6H3,(H2,26,27,28)/t16-,18-,19-,24+/m1/s1/i7D

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: To be determined

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

References:

1. Shen Y, Ai J, Lin N, Zhang H, Li Y, Wang H, Wang S, Wang Z, Li T, Sun F, Fan Z, Li L, Lu Y, Meng X, Xiao H, Hu H, Ling Y, Li F, Li H, Xi C, Gu L, Zhang W, Fan X. An Open, Prospective Cohort Study of VV116 in Chinese Participants Infected with SARS-CoV-2 Omicron Variants. Emerg Microbes Infect. 2022 May 17:1-22. doi: 10.1080/22221751.2022.2078230. Epub ahead of print. PMID: 35579892.
2. Zhang R, Zhang Y, Zheng W, Shang W, Wu Y, Li N, Xiong J, Jiang H, Shen J, Xiao G, Xie Y, Zhang L. Oral remdesivir derivative VV116 is a potent inhibitor of respiratory syncytial virus with efficacy in mouse model. Signal Transduct Target Ther. 2022 Apr 16;7(1):123. doi: 10.1038/s41392-022-00963-7. PMID: 35429988; PMCID: PMC9012943.
3. Qian HJ, Wang Y, Zhang MQ, Xie YC, Wu QQ, Liang LY, Cao Y, Duan HQ, Tian GH, Ma J, Zhang ZB, Li N, Jia JY, Zhang J, Aisa HA, Shen JS, Yu C, Jiang HL, Zhang WH, Wang Z, Liu GY. Safety, tolerability, and pharmacokinetics of VV116, an oral nucleoside analog against SARS-CoV-2, in Chinese healthy subjects. Acta Pharmacol Sin. 2022 Mar 16:1–9. doi: 10.1038/s41401-022-00895-6. Epub ahead of print. PMID: 35296780; PMCID: PMC8924727.
4. Wu CR, Yin WC, Jiang Y, Xu HE. Structure genomics of SARS-CoV-2 and its Omicron variant: drug design templates for COVID-19. Acta Pharmacol Sin. 2022 Jan 20:1–13. doi: 10.1038/s41401-021-00851-w. Epub ahead of print. PMID: 35058587; PMCID: PMC8771608.

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