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Entecavir (BMS200475) Sale

(Synonyms: 恩替卡韦; BMS200475; SQ34676) 目录号 : GC32093

An antiviral nucleoside analog

Entecavir (BMS200475) Chemical Structure

Cas No.:142217-69-4

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10mg
¥891.00
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50mg
¥1,881.00
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100mg
¥3,330.00
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Sample solution is provided at 25 µL, 10mM.

Description

Entecavir is an antiviral nucleoside analog of 2'-deoxyguanosine and inhibitor of hepatitis B virus (HBV) reverse transcriptase (IC50 = 0.5 nM).1,2 It undergoes phosphorylation by cellular kinases to its active form, entecavir triphosphate.3,2 Entecavir reduces virion DNA in the culture supernatant of HepG2 2.2.15 cells infected with hepatitis B virus (HBV; EC50 = 3.75 nM).1 It reduces serum and hepatic levels of viral DNA in a duckling model of HBV infection when administered at a dose of 1 mg/kg.4 Formulations containing entecavir have been used in the treatment of chronic HBV infection.

1.Innaimo, S.F., Seifer, M., Bisacchi, G.S., et al.Identification of BMS-200475 as a potent and selective inhibitor of hepatitis B virusAntimicrob. Agents Chemother.41(7)1444-1448(1997) 2.Langley, D.R., Walsh, A.W., Baldick, C.J., et al.Inhibition of hepatitis B virus polymerase by entecavirJ. Virol.81(8)3992-4001(2007) 3.Fung, J., Lai, C.-L., Seto, W.-K., et al.Nucleoside/nucleotide analogues in the treatment of chronic hepatitis BJ. Antimicrob. Chemother.66(12)2715-2725(2011) 4.Marion, P.L., Salazar, F.H., Winters, M.A., et al.Potent efficacy of entecavir (BMS-200475) in a duck model of hepatitis B virus replicationAntimicrob. Agents Chemother.46(1)82-88(2002)

实验参考方法

Cell experiment:

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].

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):1444-9.
[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):1845-57.
[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):3209-18.

化学性质

Cas No. 142217-69-4 SDF
别名 恩替卡韦; BMS200475; SQ34676
Canonical SMILES O=C1NC(N)=NC2=C1N=CN2[C@@H]3C([C@H](CO)[C@@H](O)C3)=C
分子式 C12H15N5O3 分子量 277.28
溶解度 DMSO : ≥ 44 mg/mL (158.68 mM) 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 3.6065 mL 18.0323 mL 36.0646 mL
5 mM 0.7213 mL 3.6065 mL 7.2129 mL
10 mM 0.3606 mL 1.8032 mL 3.6065 mL
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