Besifovir maleate (formerly known as ANA-380 maleate; LB-80380 maleate; PMCDG dipivoxil maleate; Korea Trade name: Besivo) is a reverse transcriptase inhibitor that has been approved in Korea to treat hepatitis B virus (HBV) infection. It is a novel and potent acyclic nucleotide phosphonate with a similar chemical structure to adefovir and tenofovir. Besifovir is a prodrug and an oral nucleotide analogue that inhibits viral replication by incorporation into the viral DNA. Antiviral activity against wild-type virus and virus with drug-resistant mutations was demonstrated in Phase II trials, with significant reduction of viral load in patients treated with LB80380. LB80380 was also shown to be safe and well tolerated.
理化性质和储存条件
| Molecular Weight (MW) | 627.58 |
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| Formula | C26H38N5O11P |
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| CAS No. | 1039623-01-2 (Besifovir maleate salt); |
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| Storage | -20℃ for 3 years in powder form |
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| -80℃ for 2 years in solvent |
| Solubility (In vitro) | DMSO: 10 mM |
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| Water: N/A |
| Ethanol: N/A |
| Chemical Name | ((((1-((2-amino-9H-purin-9-yl)methyl)cyclopropoxy)methyl)phosphanediyl)bis(oxy))bis(methylene) bis(2,2-dimethylpropanoate) maleate |
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| Synonyms | LB-80380 maleate; LB 80380; LB80380; ANA-380; AN-380; ANA 380; PMCDG dipivoxil maleate |
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| SMILES Code | NC1=NC=C2N=CN(CC3(OCP(OCOC(C(C)(C)C)=O)OCOC(C(C)(C)C)=O)CC3)C2=N1.O=C(O)/C=C\C(O)=O |
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