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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Solubility

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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 57	In-stock	Estimated Time of Arrival: May 23
Solution
10 mM * 1 mL in DMSO	USD 60	In-stock	Estimated Time of Arrival: May 23
Solid
5 mg	USD 55	In-stock	Estimated Time of Arrival: May 23
10 mg	USD 99	In-stock	Estimated Time of Arrival: May 23
25 mg	USD 148	In-stock	Estimated Time of Arrival: May 23
50 mg	USD 209	In-stock	Estimated Time of Arrival: May 23
100 mg	USD 295	In-stock	Estimated Time of Arrival: May 23
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Customer Review

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

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%

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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

Keywords:

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

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Entecavir monohydrate (Synonyms: BMS200475 monohydrate; SQ34676 monohydrate)

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