1. Anti-infection
  2. HBV
  3. CAB7-3

CAB7-3 是一种口服有效的 HBV 衣壳组装调节剂。CAB7-3 表现出卓越的抗病毒效力,其抑制 HBV DNA EC50 为 70 nM,CC50 为 32.3 μM。CAB7-3 在多种细胞模型中均显示出显著的抗 HBV 活性,其在 HBV 整合的 HepDES19 细胞、四环素诱导的 HepAD38 细胞以及 HBV 感染的 HLCZ01 细胞中的 EC50 值分别为 70 μM、1 nM 和 2 nM。CAB7-3 在体内能有效降低肝脏 HBV 核心蛋白水平并抑制病毒复制。CAB7-3 现出良好的类药性和安全性,可用于乙型肝炎病毒研究。

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CAB7-3

CAB7-3 Chemical Structure

CAS No. : 3014372-17-6

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CAB7-3 is an orally active HBV capsid assembly modulator (CAM). CAB7-3 exhibits an exceptional antiviral efficacy reducing HBV DNA with an EC50 = 70 nM, CC50 = 32.3 μM in HepDES19 cells. CAB7-3 exhibits significant anti-HBV activity in HBV-integrated HepDES19 (EC50 = 70 nM), HepAD38 (EC50 = 1 nM) and HBV-infected HLCZ01 cells (EC50 = 2 nM), respectively. CAB7-3 effectively reduces Hepatic HBV core protein levels and suppresses viral replication in vivo. CAB7-3 demonstrates a favorable drug-like and safety profile. CAB7-3 can be used for Hepatitis B Virus (HBV) research[1].

体外研究
(In Vitro)

CAB7-3 (0.001-1 μM,6 天) 在多种细胞模型中显示出抗病毒活性:在 HepAD38 细胞中,EC50 = 1 nM,CC50 = 26.54 μM,SI = 26540;在 HepDES19 细胞中,EC50 = 7 nM,CC50 = 32 μM,SI = 481;在 HBV 感染的 HLCZ01 细胞中,EC50 = 2 nM,CC50 = 30.73 μM,SI = 15365[1]
CAB7-3 (0.0003-1 μM,6 天) 在 HepAD38 和 HLCZ01 细胞中能够阻断新的 cccDNA 形成,同时不影响由已存在的 cccDNA 所产生的 HBsAg 分泌[1]
CAB7-3 (0.006-4 μM,3 天) 在 HepG2 细胞中能够诱导 HBV 核心蛋白降解并破坏衣壳组装[1]
CAB7-3 (1 μM,0-60 分钟) 在人肝微粒体中的代谢稳定性参数为:半衰期 (T1/2) = 169 分钟、微粒体固有清除率 (CLint(mic)) = 8.2 μL/min/mg、肝脏固有清除率 (CLint(liver)) = 7.4 mL/min/kg、60 分钟后剩余量 = 78.0%[1]
CAB7-3 (10 μM) 在人原代肝细胞中不诱导 CYP3A4表达[1]
CAB7-3 (0.3-100 μM) 在表达 hERG 通道的 HEK293 细胞中表现出显著较低的 hERG 通道抑制率:在0.3、1、3、10、30 和 100 μM 浓度下的抑制率分别为 3.52%、14.59%、31.84%、61.05%、83.05% 和 94.76%[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

ELISA Assay[1]

Cell Line: HepAD38 and HLCZ01 cells
Concentration: 0.0003, 0.001, 0.003, 0.1, 0.03, 0.1 and 0.3 μM
Incubation Time: 6 days
Result: Had minimal impact on the production of HBsAg in both HepAD38 cells and HLCZ01 cells.

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 0.06, 0.13, 0.25, 0.5, 1.0, 2.0, 4.0 μM
Incubation Time: 3 days
Result: Reduced intracellular Cp expression in a dose-dependent manner.
体内研究
(In Vivo)

CAB7-3 (口服给药,15 mg/kg,每日一次,持续 18 天) 在 HBV 携带小鼠模型中,通过抑制 HBV 衣壳组装,进而抑制含病毒 DNA 颗粒的分泌[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: pAAVHBV1.2 plasmid (6 μg, hydrodynamic injection ) induced-male C57BL/6J (6 weeks)[1]
Dosage: 15 mg/kg
Administration: p.o., once daily for 18 days
Result: Significantly reduced serum HBV DNA levels from the vehicle baseline of 1.02 × 105 IU/mL to 1.06 × 104 IU/mL.
Displayed enhanced anti-HBV activity, reducing hepatic HBcAg expression despite not noticeably affecting serum HBsAg expression.
Showed no significant change in the Serum ALT and AST levels, as well as HE staining of liver tissue.
分子量

656.33

Formula

C28H28BBrFN5O5S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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CAB7-3
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HY-180524
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