PHOSPHONIC ACID, [[[1-[(2-AMINO-9H-PURIN-9-YL)METHYL]CYCLOPROPYL]OXY]METHYL]- (9CI)
PHOSPHONIC ACID, [[[1-[(2-AMINO-9H-PURIN-9-YL)METHYL]CYCLOPROPYL]OXY]METHYL]- (9CI) Basic information
- Product Name:
- PHOSPHONIC ACID, [[[1-[(2-AMINO-9H-PURIN-9-YL)METHYL]CYCLOPROPYL]OXY]METHYL]- (9CI)
- Synonyms:
-
- [1-[(2-amino-9-purinyl)methyl]cyclopropyl]oxymethylphosphonic acid
- PHOSPHONIC ACID, [[[1-[(2-AMINO-9H-PURIN-9-YL)METHYL]CYCLOPROPYL]OXY]METHYL]- (9CI)
- PHOSPHONIC ACID, [[[1-[(2-AMINO-9H-PURIN-9-YL)METHYL]CYCLOPROPYL]OXY]METHYL]-
- (1-((2-Amino-9H-purin-9-yl)methyl)cyclopropoxy)methylphosphonic acid
- P-[[[1-[(2-amino-9H-purin-9-yl)methyl]cyclopropyl]oxy]methyl]-Phosphonic acid
- [[[1-[(2-Amino-9H-purin-9-yl)methyl]cyclopropyl]oxy]methyl]phosphonic acid
- Besifovir
- [1-[(2-aminopurin-9-yl)methyl]cyclopropyl]oxymethylphosphonic acid
- CAS:
- 441785-25-7
- MF:
- C10H14N5O4P
- MW:
- 299.22
- Mol File:
- 441785-25-7.mol
PHOSPHONIC ACID, [[[1-[(2-AMINO-9H-PURIN-9-YL)METHYL]CYCLOPROPYL]OXY]METHYL]- (9CI) Chemical Properties
- Boiling point:
- 668.4±65.0 °C(Predicted)
- Density
- 1.94±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: 250 mg/mL (835.51 mM)
- form
- Solid
- pka
- 2.44±0.10(Predicted)
- color
- Light yellow to yellow
PHOSPHONIC ACID, [[[1-[(2-AMINO-9H-PURIN-9-YL)METHYL]CYCLOPROPYL]OXY]METHYL]- (9CI) Usage And Synthesis
Uses
Besifovir (LB80331), a parent agent converted by LB80380 (HY-19447A), further metabolizes to its active form, LB80317.html" class="link-product" target="_blank"> LB80317 (HY-106235). Besifovir is an orally active, novel antiviral agent against hepatitis B virus (HBV)[1][2].
in vivo
The prodrug, LB80380, is rapidly absorbed after oral administration (30, 60, 120, 240 mg) and is converted to its parent drug, Besifovir (LB80331) (LB80380 was not detected in plasma). The median Tmaxs of LB80331 ranged from 1.0 to 2.0 h postdosing. Thereafter, the plasma LB80331 concentration declined in a monoexponential manner, and the mean values of t1/2 ranged from 2.5 to 3.3 h[2].
References
[1] Jung JA, et al. Pharmacokinetic comparison of the maleate and free base formulations of LB80380, a novel nucleotide analog, in healthy male volunteers. Int J Clin Pharmacol Ther. 2012 Sep;50(9):657-64. DOI:10.5414/cp201716
[2] Yuen MF, et al. A randomized placebo-controlled, dose-finding study of oral LB80380 in HBeAg-positive patients with chronic hepatitis B. Antivir Ther. 2006;11(8):977-83. PMID:17302367
[3] Lung-Yi Mak, et al. Pharmacokinetic evaluation of besifovir for the treatment of HBV infection. Expert Opin Drug Metab Toxicol. 2018 Jan;14(1):101-106. DOI:10.1080/17425255.2018.1417983
PHOSPHONIC ACID, [[[1-[(2-AMINO-9H-PURIN-9-YL)METHYL]CYCLOPROPYL]OXY]METHYL]- (9CI)Supplier
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