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Purity: ≥98%
Entecavir hydrate (also known as SQ-34676 and BMS-200475), monohydrated form of entecavir and anti-hepatitis B virus (HBV) agent, is a novel deoxyguanine nucleoside analogue and a reverse transcriptase inhibitor. Entecavir potently and selectively inhibits HBV with an EC50 of 3.75 nM in HepG2 cells. Entecavir is an oral antiviral drug used in the treatment of hepatitis B virus (HBV) infection. It prevents the hepatitis B virus from multiplying and reduces the amount of virus in the body. Entecavir is a highly potent inhibitor of wild-type HBV Pol and is 100- to 300-fold more potent than lamivudine-triphosphate against 3TC-resistant HBV Pol. Entecavir inhibits the replication of 3TC-resistant HBV, but 20- to 30-fold higher concentrations are required.
| ln Vitro |
The EC50 value of entecavir monohydrate (also known as BMS200475 monohydrate or SQ34676 monohydrate) against HBV is 3.75 nM. It is incorporated into the HBV protein primer and then prevents reverse transcriptase from starting. The antiviral activity of BMS -200475 against other RNA and DNA viruses is notably lower [1]. Compared to Iamivudine and other deoxyguanosine analogs (Penciclovir, Ganciclovir, Lobucavir, and Aciclovir), entecavir monohydrate is phosphorylated to its active metabolite more easily. Entecavir has a 15-hour intracellular half-life [2].
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| ln Vivo |
In chronically infected woodchucks, daily oral treatment of Entecavir (monohydrate) at a dose range of 0.02-0.5 mg/kg for 1-3 months can effectively lower the levels of viremia caused by the woodchuck hepatitis virus (WHV) [3].
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| 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.
[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. [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 |
| Molecular Formula |
C12H15N5O3.H2O
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| Molecular Weight |
295.29
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| CAS # |
209216-23-9
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| Related CAS # |
Entecavir;142217-69-4
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| SMILES |
O=C1NC(N)=NC2=C1N=CN2[C@@H]3C([ C@H](CO)[C@@H](O)C3)=C.[H]O[H]
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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