HBV-IN-4

HBV-IN-4，是一种酞嗪酮衍生物，是一种有效的具有口服活性的 HBV DNA 复制抑制剂，IC50 为 14 nM。HBV-IN-4 可诱导无基因组衣壳的形成，并具有强大的抗 HBV 效力。

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库存: 现货

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5mg

￥3262.00

2610.00

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10mg

￥5175.00

4140.00

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25mg

￥10250.00

8200.00

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50mg

￥15487.00

12390.00

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100mg

￥24037.00

19230.00

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货号: ajcx33504
CAS: 2305897-84-9
别名:
分子式: C24H19ClFN5O3
分子量: 479.89
纯度: >98%
溶解度: DMSO : 100 mg/mL (208.38 mM; Need ultrasonic)
储存: Store at -20°C
库存: 现货

Background

HBV-IN-4, a phthalazinone derivative, is a potent and orally active HBV DNA replication inhibitor with an IC50 of 14 nM. HBV-IN-4 induces the formation of genome-free capsids and has potent anti-HBV potencies[1].

HBV-IN-4 (compound 19f; 0-1 μM; 8 days) treatment inhibits the various forms (relaxed circular [rc] and single-stranded [ss] HBV DNA) in a dose-dependent manner in HepG2.2.15 cells. HBV-IN-4 treatment could also reduce capsidassociated DNAs dose-dependently. HBV-IN-4 could induce the formation of genome-free capsids, including a phenotype of faster-migrating ones[1].

HBV-IN-4 (Compound 19f; 50-150 mg/kg; oral administration; twice a day; for 4 weeks; Balb/c male mice) treatment achieves 2.67 log viral load reduction in AAV-HBV/mouse model[1].HBV-IN-4 (compound 19f) exhibits favorable drug characteristics with low plasma clearance (CL=4.1 mL/min/kg), excellent drug exposure (AUC0-t=49 744 h?ng/L), T1/2 (2.15 hours) and oral bioavailability (F=60.4%) using 20 mg/kg oral administration in mice. HBV-IN-4 also shows good distribution in liver exposure[1].

[1]. Wuhong Chen, et al. Discovery of Phthalazinone Derivatives as Novel Hepatitis B Virus Capsid Inhibitors. J Med Chem. 2020 Jul 21.