Interbiotech Entecavir

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FT-XLS250

Entecavir

Product Description

Catalog #:

XLS250, 5mg XLS251, 10mg XLS252, 50mg XLS253, 100mg

AXAIV0, 1ml 10mM in DMSO.

Catalog #: Name:

Entecavir, Monohydrate

Syn: BMS200475 monohydrate; SQ34676 monohydrate

CAS : 209216-23-9

MW :

295.29

Formula : Properties:

C₁₂H₁₇N₅O₄

DMSO : ≥ 50 mg/mL (169.33 mM)

H2O : 2.8 mg/mL (9.48 mM) >99.5%
Also available:

Storage:

Powder: -20°C (longterm; possible at +4°C (2 years)^(M)In solvent: -80°C (6 months) -20°C (1 month)

Entecavir free form #RO893P/Q/R

(Syn.:BMS200475;SQ34676)

CAS No. : 142217-69-4; MW: 277.2 For Research Use Only

Introduction

Entecavir monohydrate(BMS200475 monohydrate; SQ34676 monohydrate)is a potent andselective inhibitorof HBV, with an EC50 of 3.75 nM in HepG2 cell.

IC50 & Target EC50：3.75 nM (anti-HBV, HepG2 cell)[1]

In Vitro

*Solubility :

DMSO : ≥ 50 mg/mL (169.33 mM)

H₂O : 2.8 mg/mL (9.48 mM; Need ultrasonicandwarming)
*Preparation : 1mM = 1mg in 3.3865 mL

Entecavir monohydrate(BMS200475 monohydrate; SQ34676 monohydrate)has a EC50 of 3.75 nM againstHBV. It is incorporated intothe proteinprimer of HBV and subsequently inhibits theprimingstepof the reverse transcriptase. The antiviral activity of BMS-200475 is significantlyless against theother RNA and DNA viruses[1]. Entecavir monohydrateis more readilyphosphorylatedto its active metabolites than otherdeoxyguanosine analogs (penciclovir, ganciclovir, lobucavir, and aciclovir) or lamivudine. The intracellular half-life of entecavir is 15 h[2].

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InterBioTech

FT-XLS250

In Vivo

*Preparation : 1. Add each solventone by one: 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 3 mg/mL (10.16 mM); Clear solution

2. Add each solventone by one: 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 3 mg/mL (10.16 mM); Clear solution
3. Add each solventone by one: 10% DMSO 90% corn oil

Solubility: ≥ 3 mg/mL (10.16 mM); Clear solution

Daily oral treatmentwith Entecavir monohydrateat doses rangingfrom 0.02to 0.5 mg/kgof body weightfor 1 to 3 months effectively reduces thelevel of woodchuck hepatitisvirus (WHV) viremia in chronicallyinfected woodchucks [3].

References

[1 ]. Innaimo SF, et al. Identification of?BMS-200475?as a potent and selective inhibitor of hepatitisB 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(1 1):1845-56. [3 ]. Genovesi EV, et al. Efficacy of the carbocyclic 2'-deoxyguanosine nucleoside?BMS-200475?in the woodchuck modelof hepatitisB virus infection. Antimicrob Agents Chemother.?1998 Dec;42(12):3209-17.

More:
•Mol Pharm. 2018 Oct 30.

•Virus Res. 2019 Jul 31:197677.

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