Entecavir monohydrate (Synonyms: BMS200475 monohydrate; SQ34676 monohydrate)

Name: Entecavir monohydrate
Brand: MedChemExpress
SKU: HY-13623A
Rating: 5.0 (17 reviews)

Cat. No.: HY-13623A Purity: 99.85%: Data Sheet
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Entecavir monohydrate (BMS200475 monohydrate; SQ34676 monohydrate) is a potent and selective inhibitor of HBV, with an EC₅₀ of 3.75 nM in HepG2 cell.

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

Entecavir monohydrate Chemical Structure

CAS No. : 209216-23-9

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 61	In-stock	Estimated Time of Arrival: May 6
Solution
10 mM * 1 mL in DMSO	USD 64	In-stock	Estimated Time of Arrival: May 6
Solid
5 mg	USD 58	In-stock	Estimated Time of Arrival: May 6
10 mg	USD 104	In-stock	Estimated Time of Arrival: May 6
50 mg	USD 219	In-stock	Estimated Time of Arrival: May 6
100 mg	USD 389	In-stock	Estimated Time of Arrival: May 6
200 mg	USD 554	In-stock	Estimated Time of Arrival: May 6
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Based on 17 publication(s) in Google Scholar

Other Forms of Entecavir monohydrate:

Entecavir Get quote
Entecavir (monohydrate) (Standard) Get quote

17 Publications Citing Use of MCE Entecavir monohydrate

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Description

Entecavir monohydrate (BMS200475 monohydrate; SQ34676 monohydrate) is a potent and selective inhibitor of HBV, with an EC₅₀ of 3.75 nM in HepG2 cell.

IC₅₀ & Target

EC50：3.75 nM (anti-HBV, HepG2 cell)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
CCRF-CEM	CC₅₀	> 100 μM Compound: Entecavir	Cytotoxicity against human CEM cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human CEM cells assessed as reduction in cell viability by MTT assay	[PMID: 33421915]
CEM-SS	EC₅₀	> 10 μM Compound: ETV	Antiviral activity against HIV1 infected in human CEM-SS cells after 10 days by MTT assay Antiviral activity against HIV1 infected in human CEM-SS cells after 10 days by MTT assay	[PMID: 18316521]
CEM-SS	EC₅₀	21 μM Compound: ETV	Cytotoxicity against human CEM-SS cells after 10 days by MTT assay Cytotoxicity against human CEM-SS cells after 10 days by MTT assay	[PMID: 18316521]
HEK293	EC₅₀	> 100 μM Compound: Entecavir	Antiviral activity against HIV1 expressing reverse transcriptase D67N/K70R/T215F/K219E/M184V mutant infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 expressing reverse transcriptase D67N/K70R/T215F/K219E/M184V mutant infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	11.7 μM Compound: Entecavir	Antiviral activity against HIV1 expressing reverse transcriptase K103N/Y181C/G190A mutant infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 expressing reverse transcriptase K103N/Y181C/G190A mutant infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	12.5 μM Compound: Entecavir	Antiviral activity against HIV1 subtype A isolate 1 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 subtype A isolate 1 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	12.6 μM Compound: Entecavir	Antiviral activity against HIV1 NL4-3 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 NL4-3 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	13.2 μM Compound: Entecavir	Antiviral activity against HIV1 subtype A isolate 2 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 subtype A isolate 2 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	13.5 μM Compound: Entecavir	Antiviral activity against HIV1 subtype B isolate 4 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 subtype B isolate 4 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	13.6 μM Compound: Entecavir	Antiviral activity against HIV1 subtype BF isolate 5 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 subtype BF isolate 5 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	15.1 μM Compound: Entecavir	Antiviral activity against HIV1 subtype B isolate 3 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 subtype B isolate 3 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	30.6 μM Compound: ETV	Antiviral activity against pseudotype HIV1 NL-Luc infected in 24 hrs pretreated HEK293 cells by phenosense assay Antiviral activity against pseudotype HIV1 NL-Luc infected in 24 hrs pretreated HEK293 cells by phenosense assay	[PMID: 18316521]
HEK293	EC₅₀	7.62 μM Compound: Entecavir	Antiviral activity against HIV1 subtype D isolate 8 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 subtype D isolate 8 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	9.51 μM Compound: Entecavir	Antiviral activity against HIV1 subtype C isolate 6 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 subtype C isolate 6 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	9.95 μM Compound: Entecavir	Antiviral activity against HIV1 subtype C isolate 7 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 subtype C isolate 7 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HeLa	EC₅₀	> 4 μM Compound: ETV	Antiviral activity against pseudotype HIV1 LAI-Luc infected in CD4-positive human HeLa cells measured on day 3 postinfection by luciferase reporter gene assay Antiviral activity against pseudotype HIV1 LAI-Luc infected in CD4-positive human HeLa cells measured on day 3 postinfection by luciferase reporter gene assay	[PMID: 18316521]
HepG2	CC₅₀	> 100 μM Compound: Entecavir	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay	[PMID: 33421915]
HepG2 2.2.15	CC₅₀	> 1 μM Compound: Entecavir	Cytotoxicity against human HepG2.2.15 cells assessed as cell viability by tetrazolium dye uptake assay Cytotoxicity against human HepG2.2.15 cells assessed as cell viability by tetrazolium dye uptake assay	[PMID: 28682067]
HepG2 2.2.15	EC₅₀	0.008 μM Compound: Entecavir	Antiviral activity against wild type Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of virus replication treated daily for 9 days by quantitative blot hybridization method Antiviral activity against wild type Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of virus replication treated daily for 9 days by quantitative blot hybridization method	[PMID: 21930377]
HepG2 2.2.15	EC₅₀	1.2 μM Compound: Entecavir	Antiviral activity against lamivudine/entecavir-resistant Hepatitis B virus harboring reverse transcriptase L180M/M204V/S202G infected in human HepG2(2.2.15) cells assessed as inhibition of virus replication treated daily for 9 days by quantitative blot h Antiviral activity against lamivudine/entecavir-resistant Hepatitis B virus harboring reverse transcriptase L180M/M204V/S202G infected in human HepG2(2.2.15) cells assessed as inhibition of virus replication treated daily for 9 days by quantitative blot h	[PMID: 21930377]
HepG2 2.2.15	EC₅₀	2.2 x 10^-6 μM Compound: ETV	Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as reduction in viral DNA levels incubated for 6 days by PCR analysis Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as reduction in viral DNA levels incubated for 6 days by PCR analysis	[PMID: 32421339]
HepG2 2.2.15	CC₅₀	28 μM Compound: Entecavir	Cytotoxicity against human HepG2(2.2.15) cells after 24 hrs by neutral red dye uptake assay Cytotoxicity against human HepG2(2.2.15) cells after 24 hrs by neutral red dye uptake assay	[PMID: 21930377]
HepG2 2.2.15	CC₅₀	30 μM Compound: Entecavir	Cytotoxicity in human HepG2.215 cells assessed as reduction in cell viability after 5 days by CCK8 assay Cytotoxicity in human HepG2.215 cells assessed as reduction in cell viability after 5 days by CCK8 assay	[PMID: 28082068]
HepG2 2.2.15	CC₅₀	30 μM Compound: ETV	Cytotoxicity against human HepG2.2.15 cells by MTT assay Cytotoxicity against human HepG2.2.15 cells by MTT assay	[PMID: 25905540]
HepG2 2.2.15	CC₅₀	52.9 μM Compound: Entecavir	Cytotoxicity against human HepG2.2.15 cells after 7 days by MTT assay Cytotoxicity against human HepG2.2.15 cells after 7 days by MTT assay	[PMID: 30613328]
MOLT-4	EC₅₀	> 38 μM Compound: ETV	Antiviral activity against HIV1 3B infected in MOLT-4/3B cells assessed as inhibition of mature virus release measured after 4 days of infection by RT assay Antiviral activity against HIV1 3B infected in MOLT-4/3B cells assessed as inhibition of mature virus release measured after 4 days of infection by RT assay	[PMID: 18316521]
MT2	EC₅₀	> 1.2 μM Compound: ETV	Antiviral activity against pseudotype HIV1 LAI-Luc infected in human MT2 cells measured on day 3 postinfection by luciferase reporter gene assay Antiviral activity against pseudotype HIV1 LAI-Luc infected in human MT2 cells measured on day 3 postinfection by luciferase reporter gene assay	[PMID: 18316521]
MT2	EC₅₀	> 10 μM Compound: ETV	Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay	[PMID: 18316521]
MT2	EC₅₀	> 10 μM Compound: ETV	Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay	[PMID: 18316521]
MT2	EC₅₀	> 10 μM Compound: ETV	Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay	[PMID: 18316521]
MT2	EC₅₀	> 10 μM Compound: ETV	Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay	[PMID: 18316521]
MT2	EC₅₀	> 10 μM Compound: ETV	Antiviral activity against HIV1 subtype B-NL4-3 infected in 3 hrs pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA Antiviral activity against HIV1 subtype B-NL4-3 infected in 3 hrs pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA	[PMID: 18316521]
MT2	EC₅₀	> 10 μM Compound: ETV	Antiviral activity against HIV1 NL4-3 harboring M184L mutant RT infected in human MT2 cellssmeasured after 7 passages on day 34 postinfection Antiviral activity against HIV1 NL4-3 harboring M184L mutant RT infected in human MT2 cellssmeasured after 7 passages on day 34 postinfection	[PMID: 18316521]
MT2	EC₅₀	> 100 μM Compound: ETV	Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring M184V mutant RT infected in human MT2 cells by phenosense assay Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring M184V mutant RT infected in human MT2 cells by phenosense assay	[PMID: 18316521]
MT2	EC₅₀	> 10000 μM Compound: ETV	Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA	[PMID: 18316521]
MT2	EC₅₀	> 10000 μM Compound: ETV	Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA	[PMID: 18316521]
MT2	EC₅₀	> 2.901 μM Compound: ETV	Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay	[PMID: 18316521]
MT2	EC₅₀	> 6.348 μM Compound: ETV	Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay	[PMID: 18316521]
MT2	EC₅₀	> 9.693 μM Compound: ETV	Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay	[PMID: 18316521]
MT2	EC₅₀	0.056 μM Compound: ETV	Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA	[PMID: 18316521]
MT2	EC₅₀	0.071 μM Compound: ETV	Antiviral activity against HIV1 subtype B-LAI infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA Antiviral activity against HIV1 subtype B-LAI infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA	[PMID: 18316521]
MT2	EC₅₀	0.081 μM Compound: ETV	Antiviral activity against HIV1 subtype B-3B infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA Antiviral activity against HIV1 subtype B-3B infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA	[PMID: 18316521]
MT2	EC₅₀	0.085 μM Compound: ETV	Antiviral activity against HIV1 subtype B-NL4-3 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA Antiviral activity against HIV1 subtype B-NL4-3 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA	[PMID: 18316521]
MT2	EC₅₀	0.095 μM Compound: ETV	Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA	[PMID: 18316521]
MT2	EC₅₀	0.151 μM Compound: ETV	Antiviral activity against 0.006 MOI HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA Antiviral activity against 0.006 MOI HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA	[PMID: 18316521]
MT2	EC₅₀	0.287 μM Compound: ETV	Antiviral activity against 0.006 MOI HIV1 NL4-3 infected in 1 hr-pretreated human MT2 cells measured after 5 days by RT SPA Antiviral activity against 0.006 MOI HIV1 NL4-3 infected in 1 hr-pretreated human MT2 cells measured after 5 days by RT SPA	[PMID: 18316521]
MT2	EC₅₀	0.449 μM Compound: ETV	Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA	[PMID: 18316521]
MT2	EC₅₀	0.526 μM Compound: ETV	Antiviral activity against HIV1 subtype B-SF-2 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA Antiviral activity against HIV1 subtype B-SF-2 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA	[PMID: 18316521]
MT2	EC₅₀	0.839 μM Compound: ETV	Antiviral activity against HIV1 subtype B-RF infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA Antiviral activity against HIV1 subtype B-RF infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA	[PMID: 18316521]
MT2	EC₅₀	1.03 μM Compound: ETV	Antiviral activity against HIV1 subtype B-HXB2 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA Antiviral activity against HIV1 subtype B-HXB2 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA	[PMID: 18316521]
MT2	EC₅₀	1.3 μM Compound: ETV	Antiviral activity against pseudotype HIV1 NL-RLuc infected in human MT2 cells measured on day 5 postinfection by luciferase reporter gene assay Antiviral activity against pseudotype HIV1 NL-RLuc infected in human MT2 cells measured on day 5 postinfection by luciferase reporter gene assay	[PMID: 18316521]
MT2	EC₅₀	1.364 μM Compound: ETV	Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay	[PMID: 18316521]
MT2	EC₅₀	1.4 μM Compound: ETV	Antiviral activity against HIV1 subtype B-NL4-3 infected in 2 hrs pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA Antiviral activity against HIV1 subtype B-NL4-3 infected in 2 hrs pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA	[PMID: 18316521]
MT2	EC₅₀	13.5 μM Compound: ETV	Antiviral activity against 0.006 MOI HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA Antiviral activity against 0.006 MOI HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA	[PMID: 18316521]
MT2	EC₅₀	3.62 μM Compound: ETV	Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA	[PMID: 18316521]
MT2	EC₅₀	30.6 μM Compound: ETV	Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring wild type RT infected in human MT2 cells by phenosense assay Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring wild type RT infected in human MT2 cells by phenosense assay	[PMID: 18316521]
MT2	EC₅₀	6.45 μM Compound: ETV	Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA	[PMID: 18316521]
MT2	EC₅₀	9.573 μM Compound: ETV	Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA	[PMID: 18316521]
PBMC	EC₅₀	0.026 μM Compound: ETV	Antiviral activity against HIV1 subtype B-ASM 044 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA Antiviral activity against HIV1 subtype B-ASM 044 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA	[PMID: 18316521]
PBMC	EC₅₀	0.062 μM Compound: ETV	Antiviral activity against HIV1 subtype B-92US076 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA Antiviral activity against HIV1 subtype B-92US076 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA	[PMID: 18316521]
PBMC	EC₅₀	0.109 μM Compound: ETV	Antiviral activity against HIV1 subtype B-ASM 034 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA Antiviral activity against HIV1 subtype B-ASM 034 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA	[PMID: 18316521]
PBMC	EC₅₀	1.753 μM Compound: ETV	Antiviral activity against HIV1 subtype B-93US143 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA Antiviral activity against HIV1 subtype B-93US143 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA	[PMID: 18316521]
PBMC	CC₅₀	15.7 μM Compound: Entecavir	Cytotoxicity against human PBMC cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human PBMC cells assessed as reduction in cell viability by MTT assay	[PMID: 33421915]
Vero	CC₅₀	> 100 μM Compound: Entecavir	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability by MTT assay Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability by MTT assay	[PMID: 33421915]

In Vitro

Entecavir monohydrate (BMS200475 monohydrate; SQ34676 monohydrate) has a EC₅₀ of 3.75 nM against HBV. It is incorporated into the protein primer of HBV and subsequently inhibits the priming step of the reverse transcriptase. The antiviral activity of BMS-200475 is significantly less against the other RNA and DNA viruses^[1].
Entecavir monohydrate is more readily phosphorylated to its active metabolites than other deoxyguanosine analogs (penciclovir, ganciclovir, lobucavir, and aciclovir) or lamivudine. The intracellular half-life of entecavir is 15 h^[2].

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

In Vivo

Daily oral treatment with Entecavir monohydrate at doses ranging from 0.02 to 0.5 mg/kg of body weight for 1 to 3 months effectively reduces the level of woodchuck hepatitis virus (WHV) viremia in chronically infected woodchucks^[3].

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
NCT05550519	Janssen Pharmaceutica N.V., Belgium	Hepatitis B, Chronic	October 31, 2022	Early Phase 1
NCT01018381	The 108 Military Central Hospital\|Charles Drew University of Medicine and Science	Hepatocellular Carcinoma\|Hepatitis B	June 2006	Not Applicable
NCT05423834	Chinese University of Hong Kong	Chronic Hepatitis B	September 1, 2022
NCT04392700	Sun Yat-sen University	Hepatocellular Carcinoma Recurrent	July 25, 2019	Phase 3
NCT03640728	First Affiliated Hospital Xi´an Jiaotong University	Hepatitis B\|Virus Diseases\|Liver Failure	January 25, 2019
NCT02945956	ShuGuang Hospital\|Ruijin Hospital\|Shanghai Zhongshan Hospital\|Longhua Hospital\|Shanghai Public Health Clinical Center	Portal Hypertension	April 5, 2018	Phase 4
NCT02797522	Arrowhead Pharmaceuticals	Hepatitis B	June 2016	Phase 1
NCT03236610	Uijeongbu St. Mary Hospital	Proportion of Patients With a Sustained Virological Response (Serum HBV DNA <20 IU+mL) at Week 48	January 1, 2016	Phase 3
NCT01243281	Chulalongkorn University	Chronic Hepatitis B	March 2011	Not Applicable
NCT01242787	LG Life Sciences	Chronic Hepatitis B	August 2010	Phase 2
NCT00921180	National Taiwan University Hospital\|National Science Council, Taiwan	Hepatitis B, Chronic	February 2007	Phase 4
NCT02368288	Beijing Ditan Hospital	Chronic Hepatitis B	January 2013	Phase 4
NCT00718887	Bristol-Myers Squibb	Hepatitis B, Chronic	July 2008	Phase 4
NCT00096785	Bristol-Myers Squibb	Hepatitis B\|Chronic Disease	December 2004	Phase 3
NCT02881008	Hepatera Ltd.	Chronic Hepatitis B	November 14, 2012	Phase 1\|Phase 2
NCT03109730	Assembly Biosciences	Chronic Hepatitis B	June 15, 2017	Phase 1\|Phase 2
NCT04157257	Qilu Pharmaceutical Co., Ltd.	Chronic Hepatitis b	July 26, 2019	Phase 2
NCT02615639	Third Affiliated Hospital, Sun Yat-Sen University\|Shanghai Jiao Tong University School of Medicine	Chronic Hepatitis B	November 2015	Phase 1\|Phase 2
NCT02849132	Beijing Friendship Hospital\|Peking University People´s Hospital\|Fudan University\|Affiliated Hospital of Yanbian University\|Shanghai Public Health Clinical Center\|Beijing YouAn Hospital\|Nanfang Hospital, Southern Medical University\|Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine	Hepatitis B\|Liver Cirrhosis	January 2016	Phase 4
NCT01217632	FibroGen	Liver Fibrosis Due to Chronic Hepatitis B Infection	August 2010	Phase 2
NCT02532413	Wuhan Union Hospital, China	Chronic Hepatitis B	July 2015	Phase 4
NCT01369199	National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)\|University of Pittsburgh\|National Center for Research Resources (NCRR)	Hepatitis B	May 2012	Phase 3
NCT01765231	Peking University	Hepatitis B	January 2013	Phase 4
NCT03308890	Taipei Veterans General Hospital, Taiwan\|China Medical University Hospital\|Chang Gung Memorial Hospital\|Changhua Christian Hospital	Chronic Hepatitis B	November 1, 2017	Phase 4
NCT00412529	Novartis Pharmaceuticals\|Novartis	Hepatitis B\|Chronic Hepatitis B	December 2006	Phase 3
NCT01179594	Hoffmann-La Roche	Hepatitis B, Chronic	September 18, 2010	Phase 4
NCT02777814	Sun Yat-sen University	Colorectal Neoplasms	May 1, 2015	Phase 2
NCT02452528	Arrowhead Pharmaceuticals	Chronic Hepatitis B	August 2015	Phase 2
NCT00555334	Sun Yat-sen University	Hepatocellular Carcinoma\|Liver Cancer	November 2007	Phase 4
NCT01894269	Sun Yat-sen University	Hepatocellular Carcinoma	July 2013	Phase 4
NCT02883647	Third Affiliated Hospital, Sun Yat-Sen University	Chronic Hepatitis b	January 2014
NCT01323452	Foundation for Liver Research	Entecavir for Chronic Hepatitis B Patients	November 2010
NCT04032860	West China Hospital	HCC\|HBV Coinfection	July 1, 2017	Phase 4
NCT02327416	Tongji Hospital\|Xiamen Amoytop Biotech Co., Ltd.	Hepatitis B, Chronic	October 2014	Phase 3
NCT02360592	Tongji Hospital\|Beijing Kawin Technology Share-Holding Co., Ltd.\|Fujian Cosunter Pharmaceutical Co. Ltd	Hepatitis B, Chronic	June 2013	Phase 4
NCT03448744	Wen-hong Zhang\|Huashan Hospital	Chronic Hepatitis b	October 25, 2017	Phase 4
NCT04585789	Janssen Research & Development, LLC	Hepatitis B	March 11, 2021	Phase 2
NCT02650271	Guangxi Medical University	Hepatocellular Carcinoma	February 2, 2021	Phase 3
NCT01341106	RWTH Aachen University\|Hannover Medical School	Hepatitis B, Chronic\|Liver Fibrosis	April 2011	Phase 4
NCT03239353	Aucta Pharmaceuticals, Inc	HBV	October 20, 2017	Phase 1
NCT01013272	The University of Hong Kong	Hepatitis B, Chronic	June 2007	Not Applicable
NCT01037062	Bristol-Myers Squibb	Chronic Hepatitis B	December 2003	Phase 2
NCT00704106	Pacific Health Foundation\|Bristol-Myers Squibb	Hepatitis B	May 2008
NCT02499562	Shanghai Genomics, Inc.	Hepatitis B, Chronic	June 25, 2015	Phase 2
NCT03920618	Third Affiliated Hospital, Sun Yat-Sen University	Hepatitis B\|Acute-On-Chronic Liver Failure	February 1, 2019	Not Applicable
NCT01020565	Bristol-Myers Squibb	Chronic Hepatitis B	February 2003	Phase 2
NCT01724723	National Taiwan University Hospital	Hepatitis\|Tuberculosis\|hepatitisB	December 2012	Phase 4
NCT02604199	Arrowhead Pharmaceuticals	Hepatitis B	September 2015	Phase 2
NCT05391360	Sunshine Lake Pharma Co., Ltd.	Hepatitis B, Chronic	October 11, 2021	Phase 1
NCT01027065	Cytheris SA	Chronic Hepatitis B	December 2009	Phase 1\|Phase 2
NCT00940485	Hoffmann-La Roche	Hepatitis B, Chronic	April 2009	Phase 4
NCT05107778	Ascletis Pharmaceuticals Co., Ltd.	Hepatitis B, Chronic	January 10, 2022	Phase 2
NCT01589952	Bangabandhu Sheikh Mujib Medical University, Dhaka, Bangladesh	Chronic Hepatitis B	March 2012	Phase 1\|Phase 2
NCT00531167	Korea University\|GlaxoSmithKline	Chronic Hepatitis B	April 2007	Phase 4
NCT01254994	Sun Yat-sen University	Liver Failure	August 2007	Phase 2
NCT03164889	Beijing 302 Hospital	Hepatitis B, Chronic	January 2017	Not Applicable
NCT04199819	The University of Hong Kong	Occult Hepatitis B\|Liver Transplant; Complications	January 1, 2022	Not Applicable
NCT00410072	Bristol-Myers Squibb	Hepatitis B, Chronic	April 2007	Phase 3
NCT01918631	Chinese University of Hong Kong	Chronic Heptitis B	August 2013	Not Applicable
NCT00605384	Bristol-Myers Squibb	Chronic Hepatitis B	August 2008	Phase 3
NCT04501224	Third Affiliated Hospital, Sun Yat-Sen University	Chronic Hepatitis b\|Cirrhosis Due to Hepatitis B	August 3, 2020	Not Applicable
NCT01023230	Dynavax Technologies Corporation	Hepatitis B, Chronic	September 2009	Phase 1
NCT01639092	Asan Medical Center\|Samsung Medical Center\|Konkuk University Medical Center\|Korea University Guro Hospital\|Seoul National University Hospital	Chronic Viral Hepatitis B Without Delta-agent	September 28, 2012	Phase 4
NCT01599130	Sun Yat-sen University	Hepatitis B	July 2012	Not Applicable
NCT04124081	Beijing Continent Pharmaceutical Co, Ltd.	Hydronidone	May 15, 2019	Phase 1
NCT04405011	National Taiwan University Hospital	HBV+HCV Co-infection	August 1, 2018	Not Applicable
NCT00662545	University of California, San Francisco\|Bristol-Myers Squibb	HIV Infections\|Hepatitis B	April 2008	Phase 4
NCT01046799	HepNet Study House, German Liverfoundation\|Hannover Medical School	Liver Transplantation\|Hepatitis B\|Liver Disease	March 2008	Phase 3
NCT01715987	New Discovery LLC	Hepatitis B	October 2012
NCT03933384	Taichung Veterans General Hospital	Hepatitis B\|Viral Hepatitis	August 19, 2019	Phase 4
NCT01079806	Bristol-Myers Squibb	Chronic Hepatitis B Virus, Pediatric	June 30, 2010	Phase 3
NCT01711567	Korea University\|Gilead Sciences	Chronic Hepatitis B	April 2013	Phase 4
NCT03509688	The First Hospital of Jilin University\|Chinese Academy of Sciences	Hepatitis	November 2014	Not Applicable
NCT01204762	Bristol-Myers Squibb	Hepatitis B Virus	November 2010	Phase 2
NCT04536532	Sunshine Lake Pharma Co., Ltd.	Hepatitis B, Chronic	October 12, 2020	Phase 1\|Phase 2
NCT04196998	Third Affiliated Hospital, Sun Yat-Sen University	Hepatitis B\|Compensated Cirrhosis	January 1, 2019	Not Applicable
NCT01938820	Beijing Friendship Hospital\|Peking University People´s Hospital\|RenJi Hospital\|Peking University\|Shanghai Zhongshan Hospital\|Fudan University\|Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine\|Shanghai Public Health Clinical Center\|Nanfang Hospital, Southern Medical University\|Sir Run Run Shaw Hospital\|Beijing YouAn Hospital\|Peking University First Hospital\|Beijing 302 Hospital\|Peking Union Medical College Hospital\|Beijing Ditan Hospital\|Beijing Tiantan Hospital\|Huashan Hospital\|Tongji Hospital\|Tang-Du Hospital\|Fifth Hospital of Shijiazhuang City\|Logistics University of Chinese People´s Armed Police Forces\|The First Affiliated Hospital of Shanxi Medical University\|The Affiliated Hospital of Yanbian University	Liver Cirrhosis	June 2013	Phase 4
NCT02482272	Asan Medical Center	Hepatitis B, Chronic	May 2015	Phase 4
NCT04667104	Janssen Research & Development, LLC	Hepatitis B, Chronic	February 1, 2021	Phase 2
NCT01148576	Zhejiang University	Chronic Hepatitis B\|Hepatic Steatosis	June 2010	Phase 4
NCT01023217	Asan Medical Center	Hepatitis B, Chronic	November 2009	Phase 4
NCT02738008	Arrowhead Pharmaceuticals	Hepatitis B	March 2016	Phase 2
NCT01341743	Nanfang Hospital, Southern Medical University\|JiangSu Chia-Tai Tianqin Pharmacy Co.Ltd	Hepatitis B	December 2010	Phase 4
NCT02973646	Third Affiliated Hospital, Sun Yat-Sen University	Chronic Hepatitis b	January 2016	Phase 4
NCT00625339	Yonsei University\|Pusan National University Hospital	Hepatitis B, Chronic	February 2008	Phase 4
NCT02075294	Ying-Jie Ji\|Beijing 302 Hospital	Hepatitis B, Chronic	January 2010
NCT01022801	Bristol-Myers Squibb	Chronic Hepatitis B	August 2003	Phase 2
NCT04160897	Qing XIe\|Shanghai MedSci Healthcare Co. Ltd\|Ruijin Hospital	Hepatitis B, Chronic\|Hepatocellular Carcinoma\|Compensated Cirrhosis	October 22, 2019
NCT01720238	Beijing Friendship Hospital\|Peking University First Hospital\|Peking University People´s Hospital\|Beijing YouAn Hospital\|Beijing Tiantan Hospital\|Beijing Ditan Hospital\|Peking Union Medical College Hospital\|Beijing 302 Hospital	Liver Cirrhosis\|Hepatitis B	March 2012
NCT01037166	Bristol-Myers Squibb	Chronic Hepatitis B	December 2002	Phase 2
NCT02589652	Huashan Hospital	Chronic Hepatitis B	October 2015
NCT01914744	Fudan University	Non-Hodgkin Lymphoma\|Hepatitis B Reactivation	February 2013	Phase 2
NCT00922207	Hoffmann-La Roche	Hepatitis B, Chronic	May 7, 2010	Phase 4
NCT03680183	Affiliated Cancer Hospital & Institute of Guangzhou Medical University	Non Small Cell Lung Cancer\|Hepatitis B	May 22, 2018
NCT05793268	E-DA Hospital	Chronic Hepatitis b	December 20, 2022	Not Applicable
NCT04365933	Enyo Pharma	Hepatitis B, Chronic	May 25, 2020	Phase 2
NCT03018821	Xi´an Traditional Medicine Hospital	Hepatitis B? Chronic	January 2017	Not Applicable
NCT04431245	The University of Hong Kong	Chronic Hepatitis b	June 1, 2021
NCT00877760	Foundation for Liver Research	Chronic Hepatitis B	August 2009	Phase 4
NCT02560649	Ruijin Hospital	Chronic Hepatitis B	May 2015	Phase 4
NCT01768195	Peking University	Hepatitis B	January 2013	Phase 4
NCT01694264	Seoul National University Hospital\|Konkuk University Medical Center\|Kyungpook National University Hospital\|Kyunghee University Medical Center\|Kyung Hee University Hospital at Gangdong\|Gachon University Gil Medical Center\|Daegu Catholic University Medical Center\|Eulji University Hospital\|SMG-SNU Boramae Medical Center\|The Catholic University of Korea\|Severance Hospital\|Ajou University School of Medicine\|Ewha Womans University Mokdong Hospital\|Inha University Hospital\|Chonnam National University Hospital\|Chonbuk National University Hospital\|Chungnam National University Hospital\|Hallym University Medical Center\|Hanyang University\|Dong-A University\|Korea University Guro Hospital	Chronic Hepatitis B\|Rheumatoid Arthritis\|Ankylosing Spondylitis\|Psoriatic Arthritis\|Juvenile Idiopathic Arthritis	September 1, 2012	Phase 3
NCT01926288	Chia Tai Tianqing Pharmaceutical Group Co., Ltd.	Chronic Hepatitis B	October 2008	Phase 4
NCT00371150	Bristol-Myers Squibb	Hepatitis B Infection	November 2006	Phase 4
NCT00637663	Pusan National University Hospital\|Yonsei University	Hepatitis B, Chronic	February 2008	Phase 4
NCT01456312	Gangnam Severance Hospital\|Roche Pharma AG	Hepatitis B, Chronic	September 2012	Phase 4
NCT03332329	Qin Ning\|Tongji Hospital	Chronic Hepatitis b	December 1, 2015	Phase 4
NCT00663182	Shanghai Changzheng Hospital	Hepatitis B Virus\|Decompensated Cirrhosis	January 2008	Phase 4
NCT05453448	Xiangya Hospital of Central South University	Antiviral Drugs	May 1, 2022	Not Applicable
NCT01220596	Hanyang University\|Roche Pharma AG	Hepatitis B, Chronic	June 2010	Phase 3
NCT01270178	Taipei Veterans General Hospital, Taiwan	Chronic Hepatitis B\|Hepatocellular Carcinoma	January 2011
NCT01266005	Bukwang Pharmaceutical	Chronic Hepatitis B	August 2009	Phase 4
NCT03349008	Cttq	Chronic Hepatitis b\|Liver Inflammation	November 25, 2017	Phase 4
NCT01139203	Shanghai Jiao Tong University School of Medicine\|Zhejiang University	Liver Transplantation\|Hepatitis B	August 2009	Not Applicable
NCT01580202	Seoul National University Hospital	Malignancy\|Hepatitis B	April 2012	Phase 3
NCT00597259	National Taiwan University Hospital\|Bristol-Myers Squibb	Chronic Hepatitis B	January 2008	Phase 4
NCT05382351	Sun Yat-sen University	Chronic Hepatitis B Virus Infection	May 10, 2022	Phase 2
NCT03568578	Peking University First Hospital	Hepatitis B\|Liver Fibrosis	January 28, 2018	Not Applicable
NCT03345498	Sanjay Gandhi Postgraduate Institute of Medical Sciences	Hepatitis B\|Liver Cirrhosis	January 1, 2017
NCT02829359	Guangxi Medical University	Liver Cancer	July 2012	Phase 2\|Phase 3
NCT04182321	Fu-Sheng Wang\|Jinan Military General Hospital\|Beijing 302 Hospital	Chronic Hepatitis B	March 13, 2020	Not Applicable
NCT02263079	Hoffmann-La Roche	Pediatric Immuno-Tolerant Chronic Hepatitis B	June 16, 2014	Phase 3
NCT00625560	Yonsei University\|Pusan National University Hospital	Hepatitis B, Chronic	February 2008	Phase 4
NCT00410202	Bristol-Myers Squibb	Hepatitis B, Chronic	March 2008	Phase 3
NCT05494528	National Taiwan University Hospital\|PharmaEssentia	Chronic Hepatitis B Virus Infection	May 4, 2021	Not Applicable
NCT01906580	Beijing 302 Hospital	Chronic Hepatitis B	July 2011	Phase 4
NCT02417207	Third Affiliated Hospital, Sun Yat-Sen University	Hepatitis B\|Liver Transplantation	April 2015	Phase 4
NCT01834508	Nanfang Hospital, Southern Medical University\|Major Science and Technology Special Project of China 12th Five-year	Chronic Hepatitis B	March 2013	Phase 4
NCT01938781	Beijing Friendship Hospital\|Peking University People´s Hospital\|RenJi Hospital\|Peking University\|Shanghai Zhongshan Hospital\|Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine\|Shanghai Public Health Clinical Center\|Nanfang Hospital, Southern Medical University\|Sir Run Run Shaw Hospital\|Beijing YouAn Hospital\|Peking University First Hospital\|Beijing 302 Hospital\|Peking Union Medical College Hospital\|Beijing Ditan Hospital\|Beijing Tiantan Hospital\|Huashan Hospital\|Tongji Hospital\|Tang-Du Hospital\|Fifth Hospital of Shijiazhuang City\|Logistics University of Chinese People´s Armed Police Forces\|The First Affiliated Hospital of Shanxi Medical University\|The Affiliated Hospital of Yanbian University	Liver Fibrosis	June 2013	Phase 4
NCT03847246	Chia Tai Tianqing Pharmaceutical Group Co., Ltd.	Chronic Hepatitis b	December 4, 2018	Not Applicable
NCT00614471	Hoffmann-La Roche	Hepatitis B, Chronic	August 2007	Phase 4
NCT01833611	National Cheng-Kung University Hospital	Chronic Hepatitis	September 2008	Phase 4
NCT03032536	Alios Biopharma Inc.	Hepatitis B\|Chronic Hepatitis B\|Viral Hepatitis B	January 31, 2017	Phase 1
NCT05687409	First Affiliated Hospital of Zhejiang University	Cirrhosis, Liver\|Metagonimiasis	November 24, 2019	Phase 4
NCT01813487	Genexine, Inc.	Chronic Hepatitis B	February 2013	Not Applicable
NCT03062813	Guangdong Provincial People´s Hospital	Hepatitis B Virus Associated Nephrotic Syndrome	February 1, 2017	Phase 4
NCT04195074	Third Affiliated Hospital, Sun Yat-Sen University	Chronic Hepatitis b	January 1, 2019	Not Applicable
NCT01627223	Taichung Veterans General Hospital\|GlaxoSmithKline	Chronic Hepatitis B	July 2012	Phase 4
NCT05275023	Janssen Research & Development, LLC	Hepatitis B, Chronic	June 30, 2022	Phase 2
NCT00931229	National Health Research Institutes, Taiwan\|National Taiwan University Hospital\|Mackay Memorial Hospital\|China Medical University Hospital\|Chi Mei Medical Hospital\|Taichung Veterans General Hospital\|Kaohsiung Veterans General Hospital.\|Kaohsiung Medical University	Non-Hodgkin´s Lymphoma	June 2009	Not Applicable
NCT01639066	Asan Medical Center\|Samsung Medical Center\|Konkuk University Medical Center\|Korea University Guro Hospital\|Seoul National University Hospital	Chronic Viral Hepatitis B Without Delta-agent	September 25, 2012	Phase 4
NCT02391805	Hoffmann-La Roche	Hepatitis B, Chronic	May 17, 2015	Phase 2
NCT00395018	Bristol-Myers Squibb	Hepatitis B, Chronic	April 2007	Phase 3
NCT02726789	Replicor Inc.	Hepatitis B, Chronic	October 2012	Phase 2
NCT01943617	Beijing Friendship Hospital\|Peking University People´s Hospital\|RenJi Hospital\|Peking University\|Shanghai Zhongshan Hospital\|Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine\|Shanghai Public Health Clinical Center\|Nanfang Hospital, Southern Medical University\|Sir Run Run Shaw Hospital\|Beijing YouAn Hospital\|Peking University First Hospital\|Beijing 302 Hospital\|Peking Union Medical College Hospital\|Beijing Ditan Hospital\|Beijing Tiantan Hospital\|Huashan Hospital\|Tongji Hospital\|Tang-Du Hospital\|Fifth Hospital of Shijiazhuang City\|Logistics University of Chinese People´s Armed Police Forces\|The First Affiliated Hospital of Shanxi Medical University\|The Affiliated Hospital of Yanbian University	Liver Cirrhosis	June 2013	Phase 4
NCT04536337	Aligos Therapeutics	Chronic Hepatitis B	October 22, 2020	Phase 1
NCT00035633	Bristol-Myers Squibb	Chronic Hepatitis B	December 2001	Phase 3
NCT01595685	Asan Medical Center	Chronic Viral Hepatitis B Without Delta-agent	May 2012	Phase 3
NCT02097004	Seoul National University Hospital	Hepatitis B, Chronic	April 2014	Phase 4
NCT03357822	Tongji Hospital	Chronic Hepatitis B	January 25, 2018	Phase 4
NCT01594905	Yonsei University\|Bristol-Myers Squibb\|Seoul St. Mary´s Hospital\|The Catholic University of Korea	Chronic Hepatitis B	August 2012	Phase 4
NCT00823550	Yonsei University\|Severance Hospital\|Kangbuk Samsung Hospital\|Konkuk University Hospital\|Chung-Ang University\|Ajou University\|Inha University Hospital\|Soonchunhyang University Hospital\|The Catholic University of Korea\|Hallym University Medical Center\|Kyungpook National University Hospital\|Keimyung University\|Korea University Anam Hospital\|Korea University\|Hanyang University\|Inje University\|Pusan National University Hospital\|Bristol-Myers Squibb	Hepatitis B, Chronic	January 2009	Phase 4
NCT00926757	Taipei Veterans General Hospital, Taiwan\|Bristol-Myers Squibb	Non Hodgkin´s Lymphoma\|Hepatitis B	April 2009	Phase 4
NCT00975091	Bristol-Myers Squibb	Chronic Hepatitis B Virus	May 2004	Phase 3
NCT02577029	Arrowhead Pharmaceuticals	Hepatitis B\|Hepatitis D	December 2015	Phase 2
NCT02604212	Arrowhead Pharmaceuticals	Hepatitis B	November 2015	Phase 2
NCT04568265	Ascentage Pharma Group Inc.	Hepatitis B\|Chronic Hep B\|HBV	June 3, 2020	Phase 2
NCT01368497	National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)	Hepatitis B	September 2012	Phase 3
NCT01588912	Pusan National University Yangsan Hospital	Chronic Hepatitis B	April 2012	Phase 4
NCT05423106	Janssen Research & Development, LLC	Healthy\|Hepatitis B, Chronic	July 4, 2022	Phase 1
NCT05453435	Sun Yat-sen University	Resolved Hepatitis B\|CD20 Positive B-cell Lymphoma	July 15, 2022	Phase 2
NCT00994773	Bader, Ted, M.D.	Hepatitis B	December 2009	Phase 1
NCT04069858	Korea University	Chronic Hepatitis B	December 1, 2016	Phase 4
NCT02365402	Beijing Ditan Hospital	Chronic Hepatitis B	January 2013	Phase 4
NCT01892241	Third Affiliated Hospital, Sun Yat-Sen University	Antiviral Treatment of Chronic Hepatitis B	January 2010	Phase 3
NCT00051038	Bristol-Myers Squibb	Hepatitis B	September 2002	Phase 2\|Phase 3
NCT00065507	Bristol-Myers Squibb	Hepatitis B	August 2003	Phase 3
NCT00388674	Bristol-Myers Squibb	Chronic Hepatitis B	December 18, 2006
NCT04942886	Dong-Gun Lee\|Seoul St. Mary´s Hospital	Hepatitis B Reactivation\|Hematopoietic Stem Cell Transplantation\|Antiviral Drug\|HBV	August 21, 2021	Not Applicable
NCT00298363	Gilead Sciences	Chronic Hepatitis B	April 2006	Phase 2
NCT02505009	Chang Gung Memorial Hospital	Chronic Hepatitis B	May 1, 2015	Phase 4
NCT01438424	Bristol-Myers Squibb	Hepatitis B Virus\|HBV	January 2001	Phase 2
NCT00423891	Bristol-Myers Squibb	Hepatitis B, Chronic	June 30, 2007	Phase 1\|Phase 2
NCT00036608	Bristol-Myers Squibb	Chronic Hepatitis B	January 2002	Phase 3
NCT04535544	Janssen Research & Development, LLC	Hepatitis D, Chronic	September 17, 2020	Phase 2
NCT02241590	ShuGuang Hospital\|Shanghai Zhongshan Hospital\|Guangxi Ruikang Hospital\|Hubei Hospital of Traditional Chinese Medicine\|The First Affiliated Hospital of Hunan University of Traditional Chinese Medicine\|Huai´an No. 4 People´s Hospital\|Ruijin Hospital\|Shenzhen Third People´s Hospital\|Beijing Ditan Hospital\|Beijing YouAn Hospital\|China-Japan Friendship Hospital\|Tongji Hospital\|Wenzhou Central Hospital\|Jingmen No.1 People´s Hospital\|Shandong University of Traditional Chinese Medicine\|The Ninth Hospital of Nanchang\|The People´s Hospital of Ningxia\|Fifth Hospital of Shijiazhuang City\|The Fifth People´s Hospital of Suzhou\|The Fifth People´s Hospital of Anyang	Liver Cirrhosis Due to Hepatitis B Virus	September 2014	Phase 4
NCT05017116	Suzhou Ribo Life Science Co. Ltd.	Chronic Hepatitis b	August 9, 2021	Phase 1
NCT04638439	PharmaEssentia	Chronic Hepatitis B Infection\|Chronic Hepatitis D Infection	December 2021	Phase 1
NCT02908191	Assembly Biosciences	Chronic Hepatitis B	November 2016	Phase 1
NCT00096811	Bristol-Myers Squibb	Hepatitis B\|Chronic Disease	September 2003
NCT01326546	Chongqing Jiachen Biotechnology Ltd.\|Third Military Medical University	Chronic Hepatitis B	June 2010	Phase 2
NCT01063036	Bristol-Myers Squibb	Chronic Hepatitis B	May 2010	Phase 3
NCT04129554	Janssen Sciences Ireland UC	Hepatitis B, Chronic	November 6, 2019	Phase 2
NCT03469583	Enyo Pharma\|CPR Pharma Services Pty Ltd, Australia	Hepatitis B, Chronic	February 12, 2018	Phase 1
NCT04180150	Chia Tai Tianqing Pharmaceutical Group Co., Ltd.	Chronic Hepatitis B	November 18, 2019	Phase 2
NCT04539119	Ruijin Hospital	B-cell Lymphoma\|HBV	July 3, 2020	Phase 3
NCT00035789	Bristol-Myers Squibb	Chronic Hepatitis B	November 2001	Phase 3
NCT02777801	Sun Yat-sen University	Stomach Neoplasms	June 2015	Phase 2
NCT02065336	Arrowhead Pharmaceuticals\|ICON Clinical Research	Hepatitis B, Chronic	March 2014	Phase 2
NCT03272009	Enyo Pharma\|CPR Pharma Services Pty Ltd, Australia	Hepatitis B, Chronic	September 21, 2017	Phase 1
NCT01907230	Taipei Veterans General Hospital, Taiwan	Rheumatoid Arthritis\|Hepatitis B Reactivation\|Exposure to Hepatitis B Virus	September 10, 2013	Phase 4
NCT00986778	Bristol-Myers Squibb	Hepatitis B, Chronic	December 2009	Phase 4
NCT03887702	SWOG Cancer Research Network\|National Cancer Institute (NCI)	Hepatitis B Infection\|Malignant Solid Neoplasm	January 17, 2020	Phase 3
NCT00824707	Eastern Hepatobiliary Surgery Hospital	Primary Liver Cancer	December 2008	Not Applicable
NCT06000657	Daewoong Pharmaceutical Co. LTD.	Hepatitis B, Chronic	July 28, 2023	Phase 4
NCT00393484	Bristol-Myers Squibb	Chronic Hepatitis B	February 2007	Phase 4
NCT04398134	Assembly Biosciences	Chronic Hepatitis B	August 28, 2020	Phase 2
NCT02555943	Humanity and Health Research Centre\|Beijing 302 Hospital\|Nanfang Hospital, Southern Medical University	Chronic Hepatitis C Infection\|HBV Coinfection\|Hepatitis B Reactivation	February 2015	Phase 2\|Phase 3
NCT00917761	National Taiwan University Hospital\|National Science Council, Taiwan	Hepatitis B, Chronic	February 2007	Phase 4
NCT01026610	LG Life Sciences	Chronic Hepatitis B	August 2009	Phase 2

Molecular Weight

295.29

Formula

C₁₂H₁₇N₅O₄

CAS No.

209216-23-9

Appearance

Solid

Color

White to off-white

SMILES

NC(N1)=NC(C2=C1N([C@@H](C[C@H](O)[C@H]3CO)C3=C)C=N2)=O.O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 50 mg/mL (169.33 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 2.8 mg/mL (9.48 mM; Need ultrasonic and warming)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.3865 mL	16.9325 mL	33.8650 mL
5 mM	0.6773 mL	3.3865 mL	6.7730 mL
10 mM	0.3387 mL	1.6933 mL	3.3865 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3 mg/mL (10.16 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3 mg/mL (10.16 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 3 mg/mL (10.16 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, PEG300/PEG400, Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Purity & Documentation

Purity: 99.85%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (253 KB)HNMR (168 KB)LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Innaimo SF, et al. Identification of?BMS-200475?as a potent and selective inhibitor of hepatitis B virus. Antimicrob Agents Chemother. 1997 Jul;41(7):1444-8. [Content Brief]

[2]. Rivkin A, et al. A review of entecavir in the treatment of chronic hepatitis B infection. Curr Med Res Opin.?2005 Nov;21(11):1845-56. [Content Brief]

[3]. Genovesi EV, et al. Efficacy of the carbocyclic 2'-deoxyguanosine nucleoside?BMS-200475?in the woodchuck model of hepatitis B virus infection. Antimicrob Agents Chemother.?1998 Dec;42(12):3209-17. [Content Brief]

Cell Assay
^[1]

BMS 200475 is prepared in phosphate-buffered saline (PBS) and diluted with appropriate medium containing 2% fetal bovine serum. HepG2 2.2.15 cells are plated at a density of 5×10⁵ cells per well on 12-well Biocoat collagen-coated plates and are maintained in a confluent state for 2 to 3 days before being overlaid with 1 mL of medium spiked with BMS 200475. Quantification of HBV was performed on day 10^[1].

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

References

[1]. Innaimo SF, et al. Identification of?BMS-200475?as a potent and selective inhibitor of hepatitis B virus. Antimicrob Agents Chemother. 1997 Jul;41(7):1444-8. [Content Brief]

[2]. Rivkin A, et al. A review of entecavir in the treatment of chronic hepatitis B infection. Curr Med Res Opin.?2005 Nov;21(11):1845-56. [Content Brief]

[3]. Genovesi EV, et al. Efficacy of the carbocyclic 2'-deoxyguanosine nucleoside?BMS-200475?in the woodchuck model of hepatitis B virus infection. Antimicrob Agents Chemother.?1998 Dec;42(12):3209-17. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	3.3865 mL	16.9325 mL	33.8650 mL	84.6625 mL
H₂O / DMSO	5 mM	0.6773 mL	3.3865 mL	6.7730 mL	16.9325 mL
DMSO	10 mM	0.3387 mL	1.6933 mL	3.3865 mL	8.4663 mL
	15 mM	0.2258 mL	1.1288 mL	2.2577 mL	5.6442 mL
	20 mM	0.1693 mL	0.8466 mL	1.6933 mL	4.2331 mL
	25 mM	0.1355 mL	0.6773 mL	1.3546 mL	3.3865 mL
	30 mM	0.1129 mL	0.5644 mL	1.1288 mL	2.8221 mL
	40 mM	0.0847 mL	0.4233 mL	0.8466 mL	2.1166 mL
	50 mM	0.0677 mL	0.3387 mL	0.6773 mL	1.6933 mL
	60 mM	0.0564 mL	0.2822 mL	0.5644 mL	1.4110 mL
	80 mM	0.0423 mL	0.2117 mL	0.4233 mL	1.0583 mL
	100 mM	0.0339 mL	0.1693 mL	0.3387 mL	0.8466 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Entecavir monohydrate Related Classifications

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Entecavir209216-23-9BMS200475SQ34676BMS 200475BMS-200475SQ 34676SQ-34676HBVHepatitis B virusInhibitorinhibitorinhibit

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Entecavir monohydrate (Synonyms: BMS200475 monohydrate; SQ34676 monohydrate)

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