Entecavir monohydrate (Synonyms: 恩替卡韋 (1水合物); BMS200475 monohydrate; SQ34676 monohydrate)

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摩爾計(jì)算器

Entecavir monohydrate (BMS200475 monohydrate; SQ34676 monohydrate) 是有選擇且有效地HBV抑制劑。在HepG2細(xì)胞中的EC₅₀值為3.75 nM。

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Entecavir monohydrate Chemical Structure

CAS No. : 209216-23-9

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規(guī)格	價(jià)格	是否有貨
10 mM * 1 mL in DMSO	￥715	In-stock
1 mg	￥295	In-stock
5 mg	￥650	In-stock
10 mg	￥790	In-stock
50 mg	￥2200	In-stock
100 mg	￥3360	In-stock
200 mg	￥4800	In-stock
500 mg		詢價(jià)
1 g		詢價(jià)

or 大包裝詢價(jià)

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Customer Review

Other Forms of Entecavir monohydrate:

Entecavir In-stock
Entecavir monohydrate (Standard) 詢價(jià)

MCE 顧客使用本產(chǎn)品發(fā)表的 15 篇科研文獻(xiàn)

•Adv Sci (Weinh). 2022 May;9(16):e2103135. [Abstract]
•Emerg Microbes Infect. 2020 Dec 9;1-22. [Abstract]
•J Med Chem. 2023 Oct 15. [Abstract]
•Cell Mol Gastroenterol Hepatol. 2021 Dec 8;S2352-345X(21)00249-6. [Abstract]
•PLoS Pathog. 2021 Aug 9;17(8):e1009838. [Abstract]
•J Gastroenterol. 2021 Feb;56(2):168-180. [Abstract]
•Viruses. 2023 May 18, 15(5), 1195.
•J Glob Antimicrob Resist. 2022 Nov 14;S2213-7165(22)00250-8. [Abstract]
•Front Pharmacol. 26 September 2022.
•Biomedicines. 2022 Apr 14;10(4):900. [Abstract]
•Antiviral Res. 2020 Aug;180:104826. [Abstract]
•Virus Res. 2019 Oct 2;271:197677. [Abstract]

•Mol Pharm. 2018 Dec 3;15(12):5646-5652. [Abstract]
•J Pharmacol Sci. 2020 Sep;144(1):43-51. [Abstract]
•bioRxiv. 2020 May.

Entecavir monohydrate 相關(guān)產(chǎn)品

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生物活性
實(shí)驗(yàn)參考方法
純度 & 產(chǎn)品資料
參考文獻(xiàn)

生物活性

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]

細(xì)胞效力
(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]

體外研究
(In Vitro)

Entecavir monohydrate (BMS200475 monohydrate；SQ34676 monohydrate) 對(duì) HBV 的 EC₅₀ 為 3.75 nM。它被整合到 HBV 的蛋白質(zhì)引物中，隨后抑制逆轉(zhuǎn)錄酶的啟動(dòng)步驟。BMS -200475 對(duì)其他 RNA 和 DNA 病毒的抗病毒活性明顯較低^[1]。
與其他脫氧鳥苷類似物（Penciclovir, Ganciclovir, Lobucavir, 和 Aciclovir) 或 Iamivudine，Entecavir monohydrate 更容易磷酸化為其活性代謝物。Entecavir 的細(xì)胞內(nèi)半衰期為 15 小時(shí)^[2]。

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

體內(nèi)研究
(In Vivo)

每日口服 Entecavir (monohydrate)，劑量范圍為 0.02-0.5 mg/kg，持續(xù) 1-3 個(gè)月，可有效降低慢性感染土撥鼠的土撥鼠肝炎病毒 (WHV) 病毒血癥水平^[3]。

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

Clinical Trial

分子量

295.29

Formula

C₁₂H₁₇N₅O₄

CAS 號(hào)

209216-23-9

性狀

固體

顏色

White to off-white

中文名稱

恩替卡韋 (1水合物)

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

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

溶解性數(shù)據(jù)

細(xì)胞實(shí)驗(yàn)：

DMSO 中的溶解度 : ≥ 50 mg/mL (169.33 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

H₂O 中的溶解度 : 2.8 mg/mL (9.48 mM; 超聲加熱助溶)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液

濃度溶劑體積質(zhì)量	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

查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

* 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

摩爾計(jì)算器
稀釋計(jì)算器

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

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥方式選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

方案一

請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3 mg/mL (10.16 mM); 澄清溶液

此方案可獲得 ≥ 3 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 30.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水定容至 1 mL。
生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
方案二

請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3 mg/mL (10.16 mM); 澄清溶液

此方案可獲得 ≥ 3 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 30.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液中，混合均勻。
2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
方案三

請(qǐng)依序添加每種溶劑： 10% DMSO 90% Corn Oil
Solubility: ≥ 3 mg/mL (10.16 mM); 澄清溶液

此方案可獲得 ≥ 3 mg/mL（飽和度未知）的澄清溶液，此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。
以 1 mL 工作液為例，取 100 μL 30.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中，混合均勻。

動(dòng)物溶解方案計(jì)算器

請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只

由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量

請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：

DMSO +

Tween-80 +

Saline

如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。

方案所需 助溶劑 包括：DMSO，，均可在 MCE 網(wǎng)站選購(gòu)。，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。

計(jì)算結(jié)果

工作液所需濃度 : mg/mL

儲(chǔ)備液配制方法 : mg 藥物溶于 μL DMSO（母液濃度為 mg/mL）。

您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。

動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。

連續(xù)給藥周期超過(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。

請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱（超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。

純度 & 產(chǎn)品資料

純度: 99.85%

選擇批次：

Data Sheet (646 KB) SDS (393 KB)

COA (291 KB) HNMR (168 KB) LCMS (94 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻(xiàn)

[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.
參考文獻(xiàn)	[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.

參考文獻(xiàn)

[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]

Entecavir monohydrate 相關(guān)分類

完整儲(chǔ)備液配制表

可選溶劑	濃度溶劑體積質(zhì)量	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

* 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Entecavir209216-23-9BMS200475SQ34676恩替卡韋 (1水合物)BMS 200475BMS-200475SQ 34676SQ-34676HBVHepatitis B virusInhibitorinhibitorinhibit

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Entecavir monohydrate (Synonyms: 恩替卡韋 (1水合物); BMS200475 monohydrate; SQ34676 monohydrate)

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Other Forms of Entecavir monohydrate:

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生物活性

實(shí)驗(yàn)參考方法

純度 & 產(chǎn)品資料

參考文獻(xiàn)

摩爾計(jì)算器

稀釋計(jì)算器

Entecavir monohydrate 相關(guān)分類

完整儲(chǔ)備液配制表

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Entecavir monohydrate (Synonyms: 恩替卡韋 (1水合物); BMS200475 monohydrate; SQ34676 monohydrate)

Customer Review

Other Forms of Entecavir monohydrate:

Entecavir monohydrate 相關(guān)抗體

MCE 顧客使用本產(chǎn)品發(fā)表的 15 篇科研文獻(xiàn)

Entecavir monohydrate 相關(guān)產(chǎn)品

•相關(guān)化合物庫(kù):

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•同靶點(diǎn)蛋白產(chǎn)品:

生物活性

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純度 & 產(chǎn)品資料

參考文獻(xiàn)

Entecavir monohydrate 相關(guān)抗體:

摩爾計(jì)算器

稀釋計(jì)算器

Entecavir monohydrate 相關(guān)分類

完整儲(chǔ)備液配制表

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