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Chemical Structure| 209216-23-9 Chemical Structure| 209216-23-9

Structure of Entecavir Monohydrate
CAS No.: 209216-23-9

Chemical Structure| 209216-23-9

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Entecavir, an analogue of guanosine, is reverse transcription inhibitor of HBV with EC50 of 3.75 nM in HepG2 cell.

Synonyms: BMS200475 monohydrate; SQ34676 monohydrate; SQ 34,676

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Product Details of Entecavir Monohydrate

CAS No. :209216-23-9
Formula : C12H17N5O4
M.W : 295.29
SMILES Code : O=C1NC(N)=NC2=C1N=CN2[C@@H]3C([C@H](CO)[C@@H](O)C3)=C.[H]O[H]
Synonyms :
BMS200475 monohydrate; SQ34676 monohydrate; SQ 34,676
MDL No. :MFCD09754448
InChI Key :YXPVEXCTPGULBZ-WQYNNSOESA-N
Pubchem ID :135526609

Safety of Entecavir Monohydrate

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H332-H335
Precautionary Statements:P261-P280-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HepG2.2.15 cells 10 µM 48 h To evaluate the inhibitory effect of entecavir on HBV replication J Virol. 2023 Oct 31;97(10):e0109023.
HepAD38 cells 1 μM To investigate the inhibitory effect of ETV on HBV DNA levels, results showed that Vpx-mediated knockdown of SAMHD1 significantly increased HBV DNA levels. Life Sci Alliance. 2019 Mar 27;2(2):e201900355.
HepG2-NTCP (K7) cells 1 μM 72 h To investigate the inhibitory effect of ETV on HBV DNA levels, results showed that Vpx-mediated degradation of SAMHD1 significantly increased extracellular HBV DNA levels. Life Sci Alliance. 2019 Mar 27;2(2):e201900355.
HepG2.2.15.7 cells 1-3 nM 6 days To investigate the effect of Entecavir on HBV-induced EV-miRNAs expression, it was found that the expression of five EV-miRNAs (miR-21, miR-192, miR-215, miR-221, miR-222) was up-regulated after Entecavir treatment. Sci Rep. 2017 Aug 10;7(1):7780.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice HBV-carrier mouse model Oral 0.3 mg/kg Once daily for 3 weeks To evaluate the therapeutic effect of Entecavir on HBV infection J Exp Med. 2020 Oct 5;217(10):e20200840
FRG mice Chronic HBV infection model Oral gavage 1 mg/kg Daily administration for 17 days Suppress HBV viral load to create conditions for AAV-SaCas9 therapy Mol Ther Methods Clin Dev. 2020 Nov 26;20:258-275
BALB/c Rag2-/-Il2rg-/-SirpaNODAlb-uPAtg/tg mice Mouse model with humanized immune system and hepatocytes Intraperitoneal injection or drinking water 0.3 mg/kg Once daily for 14 weeks Entecavir treatment effectively reduced viral loads and decreased liver inflammation Gastroenterology. 2017 Dec;153(6):1647-1661.e9
Mice HBV-carrier mouse model Gavage 0.1 mg/kg Daily for 6 weeks To evaluate the anti-HBV effect of ETV in combination with SPD, showing significant reduction in HBsAg and pgRNA levels Cell Rep Med. 2024 Nov 19;5(11):101822
Mice PAAV-HBV1.2 and rAAV8-HBV1.3-transduced HBV-carrier mouse models Oral gavage 50 μg/kg 15 consecutive days Evaluated the therapeutic efficacy of Entecavir in HBV-carrier mouse models, showing significant reduction in serum HBV DNA copies but inability to induce anti-HBs Abs or eliminate serum HBsAg. NPJ Vaccines. 2024 Feb 3;9(1):22
C57BL/6 mice Chronic unpredictable mild stress (CUMS) model Gastric administration 0.3 mg/kg Once daily for 2 weeks Entecavir significantly reversed chronic stress-induced negative emotional behaviors, including anxiety- and depressive-like behaviors, and improved microglial morphological activation and immuno-inflammatory responses in the BLA region. J Neuroinflammation. 2023 Feb 15;20(1):37
C57BL/6J mice HBV carrier mouse model Oral gavage 0.1 mg/kg Once daily for 15 days To evaluate the inhibitory effect of Entecavir on HBV-DNA levels Adv Sci (Weinh). 2022 May;9(16):e2103135

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.39mL

0.68mL

0.34mL

16.93mL

3.39mL

1.69mL

33.87mL

6.77mL

3.39mL

References

 

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