[CAS NO. 1011529-10-4] Azvudine

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PRODUCTS SPECIFICATIONS [1011529-10-4]

Catalog

HY-19314

Brand

MCE

CAS

1011529-10-4

DESCRIPTION [1011529-10-4]

Overview

MDL	-
Molecular Weight	286.22
Molecular Formula	C9H11FN6O4
SMILES	O[C@@H]1[C@](CO)(N=[N+]=[N-])O[C@@H](N2C(N=C(N)C=C2)=O)[C@H]1F

For research use only. We do not sell to patients.

Summary

Azvudine (RO-0622) is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV , HBV and HCV . Azvudine 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 inhibits NRTI-resistant viral strains ^[1] . Azvudine is a click chemistry reagent, itcontains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.

IC50 & Target

HIV-1

0.03-6.92 nM (EC ₅₀ )

HIV-2

0.018-0.02 nM (EC ₅₀ )

In Vitro

Azvudine (RO-0622) 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 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 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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT05633433	Shanghai Henlius Biotech\|Shanghai Fosun Pharmaceutical Industrial Development Co. Ltd.\|HeNan Sincere Biotech Co., Ltd	SARS-CoV-2 Infection	December 29, 2022	Phase 2\|Phase 3
NCT05642910	Southeast University, China\|Hohhot First Hospital, Hohhot, Inner Mongolia, China	SARS-CoV-2 Infection	October 18, 2022	Not Applicable
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
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
NCT05682599	Shanghai Henlius Biotech\|Huashan Hospital\|Shanghai Fosun Pharmaceutical Industrial Development Co. Ltd.\|HeNan Sincere Biotech Co., Ltd	COVID-19	January 6, 2023	Phase 2
NCT05621993	Qianfoshan Hospital	COVID-19 Respiratory Infection	November 22, 2022
NCT05675748	Shanghai Henlius Biotech\|Shanghai Fosun Pharmaceutical Industrial Development Co. Ltd.\|Huashan Hospital	COVID-19	January 15, 2023
NCT05697055	Shandong Provincial Hospital\|Central hospital Affiliated to Shandong First Medical University\|The Second Affiliated Hospital of Shandong First Medical University\|The Affiliated Hospital Of Southwest Medical University\|Gansu Provincial Hospital\|Rizhao People´s Hospital	COVID-19	January 21, 2023	Phase 4
NCT05689034	Peking Union Medical College Hospital	COVID-19 Respiratory Infection	January 20, 2023	Phase 2\|Phase 3
NCT04425772	HeNan Sincere Biotech Co., Ltd	COVID-19	June 12, 2020	Not Applicable
NCT06006611	Fifth Affiliated Hospital, Sun Yat-Sen University	COVID-19	August 5, 2023
NCT04303598	HeNan Sincere Biotech Co., Ltd	HIV-infection+Aids	April 1, 2020	Phase 3

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL ( 436.73 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.4938 mL	17.4691 mL	34.9382 mL
5 mM	0.6988 mL	3.4938 mL	6.9876 mL
10 mM	0.3494 mL	1.7469 mL	3.4938 mL

* Please refer to the solubility information to select the appropriate solvent.

References

[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.