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Submit ReviewEntecavir is a potent and selective hepatitis B virus reverse transcriptase inhibitor (EC50 = 3 nM); guanine analog. Inhibits hepatitis B virus replication in HepG2.2.15 cells. Displays selectively over HCMV, HSV-1, VZV, HIV and influenza (EC50 values are 15, 32, 30-60, >10 and >80 μM respectively). Orally bioavailable.
Entecavir is also offered as part of the Tocriscreen Epigenetics Library and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.
M. Wt | 277.28 |
Formula | C12H15N5O3 |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 142217-69-4 |
PubChem ID | 153941 |
InChI Key | QDGZDCVAUDNJFG-FXQIFTODSA-N |
Smiles | O=C1C2=C(N([C@H]3C[C@H](O)[C@@H](CO)C3=C)C=N2)NC(N)=N1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 27.73 | 100 |
The following data is based on the product molecular weight 277.28. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 3.61 mL | 18.03 mL | 36.06 mL |
5 mM | 0.72 mL | 3.61 mL | 7.21 mL |
10 mM | 0.36 mL | 1.8 mL | 3.61 mL |
50 mM | 0.07 mL | 0.36 mL | 0.72 mL |
References are publications that support the biological activity of the product.
Innaimo et al (1997) Identification of BMS-200475 as a potent and selective inhibitor of hepatitis B virus. Antimicrob. Agents Chemother. 41 1444 PMID: 9210663
Bisacchi et al (1997) BMS-200475, a novel carbocyclic 2'-deoxyguanosine analog with potent and selective anti-hepatitis B virus activity in vitro Bioorganic & Medicinal Chemistry Letters 7 127
If you know of a relevant reference for Entecavir, please let us know.
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.