Azvudine hydrochloride  (Synonyms: RO-0622 hydrochloride; FNC hydrochloride)

Azvudine (RO-0622) hydrochloride is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine hydrochloride exerts highly potent inhibition on HIV-1 (EC₅₀s ranging from 0.03 to 6.92 nM) and HIV-2 (EC₅₀s ranging from 0.018 to 0.025 nM). Azvudine hydrochloride inhibits NRTI-resistant viral strains^[1]. Azvudine (hydrochloride) is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

Azvudine (RO-0622) hydrochloride displays strong inhibition on wild-type HIV-1_IIIB and HIV-1_RF with an EC₅₀ ranging from 30 to 110 pM. The EC₅₀ values of Azvudine hydrochloride against HIV-1_KM018, HIV-1_TC-1 and HIV-1_{WAN T69N} are 6.92, 0.34 and 0.45 nM, respectively. Azvudine is sensitive to NRTIs-resistant strain HIV-1_74V, PIs-resistant strains HIV-1_{L10R/M46I/L63P/V82T/I84V} and HIV-1_{RF V82F/184V}, and FIs-resistant strain pNL4-3_{gp41 (36G) V38A/N42T}. The EC₅₀ values of Azvudine hydrochloride against these resistant strains are 0.11, 0.14, 0.37 and 0.36 nM respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

322.68

C₉H₁₂ClFN₆O₄

1333126-31-0

Solid

Light yellow to khaki

O[C@@H]1[C@](CO)(N=[N+]=[N-])O[C@@H](N2C(N=C(N)C=C2)=O)[C@H]1F.Cl

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Wang RR, et al. Azvudine, a novel nucleoside reverse transcriptase inhibitor showed good drug combination features and better inhibition on drug-resistant strains than lamivudine in vitro. PLoS One. 2014 Aug 21;9(8):e105617.  [Content Brief]