MDL | - |
---|---|
Molecular Weight | 322.68 |
Molecular Formula | C9H12ClFN6O4 |
SMILES | NC(C=CN1[C@@H]2O[C@@](N=[N+]=[N-])([C@H]([C@@H]2F)O)CO)=NC1=O.[H]Cl |
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 (EC 50 s ranging from 0.03 to 6.92 nM) and HIV-2 (EC 50 s ranging from 0.018 to 0.025 nM). Azvudine hydrochloride inhibits NRTI-resistant viral strains [1] .
HIV-1 0.03-6.92 nM (EC 50 ) |
HIV-2 0.018-0.02 nM (EC 50 ) |
Azvudine (RO-0622) hydrochloride displays strong inhibition on wild-type HIV-1 IIIB and HIV-1 RF with an EC 50 ranging from 30 to 110 pM. The EC 50 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 EC 50 values of Azvudine hydrochloride against these resistant strains are 0.11, 0.14, 0.37 and 0.36 nM respectively [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
NCT Number | Sponsor | Condition | Start Date | Phase |
---|---|---|---|---|
NCT04425772 | HeNan Sincere Biotech Co., Ltd |
COVID-19
|
June 12, 2020 | Not Applicable |
NCT05621993 | Qianfoshan Hospital |
COVID-19 Respiratory Infection
|
November 22, 2022 | |
NCT05033145 | HRH Pharmaceuticals Limited|GALZU INSTITUTE OF RESEARCH, TEACHING, SCIENCE AND APPLIED TECHNOLOGY, Brazil|Clinical Research Unit + High Complexity Center (CRU+HCC) + Galzu Institute |
COVID-19
|
January 15, 2022 | Phase 3 |
NCT04303598 | HeNan Sincere Biotech Co., Ltd |
HIV-infection+Aids
|
April 1, 2020 | Phase 3 |
NCT04668235 | HRH Pharmaceuticals Limited|GALZU INSTITUTE OF RESEARCH, TEACHING, SCIENCE AND APPLIED TECHNOLOGY, Brazil|UNIVERSIDADE ESTADUAL DO NORTE FLUMINENSE (UENF), Brazil |
COVID-19
|
April 23, 2021 | Phase 3 |
Solid
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)
H 2 O : 125 mg/mL ( 387.38 mM ; Need ultrasonic)
Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 3.0990 mL | 15.4952 mL | 30.9905 mL |
5 mM | 0.6198 mL | 3.0990 mL | 6.1981 mL |
10 mM | 0.3099 mL | 1.5495 mL | 3.0990 mL |
Add each solvent one by one: PBS
Solubility: 14.29 mg/mL (44.29 mM); Clear solution; Need ultrasonic and warming and heat to 60°C