2. Anti-infection
  3. HBV
  4. HBV-IN-54

HBV-IN-54 是一种选择性的口服有效 HBV 抑制剂。HBV-IN-54 在 HepAD38 细胞 (EC50 = 0.020 μM，CC50 > 100 μM) 和 HLCZ01 细胞 (EC50 = 0.024 μM, CC50 > 100 μM) 中均表现出抗 HBV 活性，并能在体内抑制病毒复制。HBV-IN-54 展现出良好的理化性质与较高的血浆稳定性，适用于乙型肝炎 (HBV) 的相关研究。

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HBV-IN-54

HBV-IN-54 Chemical Structure

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HBV-IN-54 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HBV-IN-54 is a selective and orally active HBV inhibitor. HBV-IN-54 exhibits anti-HBV activity in both HepAD38 cells (EC50 = 0.020 μM, CC50 > 100 μM) and HLCZ01 cells (EC50 = 0.024 μM, CC50 > 100 μM). HBV-IN-54 inhibits viral replication in vivo. HBV-IN-54 displays favorable physicochemical properties and high plasma stability. HBV-IN-54 can be used for research on Hepatitis B (HBV)[1].

体外研究
(In Vitro)

HBV-IN-54 (compound 35a) 能够稳定地结合于 HBV 核心蛋白，保持与 Trp-102、Thr-128 和 Leu-140 的氢键相互作用，并与 Ser-106、Thr-142 和 Asn-136 形成相互作用[1]。
HBV-IN-54 (6 天) 在 HepAD38 细胞系中的 EC50 为 0.039 μM，CC50 为 53.11 μM，SI 为 1361.8[1]。
HBV-IN-54 (0.3-100 μM，6 天) 在 HLCZ01 细胞系中具有抗 HBV 活性，EC50 约为 0.024 μM[1]。
HBV-IN-54 (1 mg/mL，孵育 0-60 分钟) 在人肝微粒体中具有代谢稳定性，T1/2 = 30.8 min，C = 1 mg/mL，CLmint = 22.5 μL/min/mg protein，MPPGL = 48.8 mg protein/g tissue，OW = 25.7 g tissue/kg body weight，CLint,sce = 28.2 mL/min/kg[1]。

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

HBV-IN-54 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: HLCZ01 Cells
Concentration: 0.3 μM, 10 μM, 30 μM, and 100 μM
Incubation Time: 3 days
Result: Exhibited minimal cytotoxicity at a concentration of 100 μM (inhibition rate 8.02%) and suppressed HBV DNA replication in a dose-dependent manner.
体内研究
(In Vivo)

HBV-IN-54 (compound 35a) (25 mg/kg，口服给药，每日一次，连续 21 天) 在 pAAV-HBV1.2 质粒诱导的 HBV 小鼠模型中表现出体内抗病毒活性[1]。

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

Animal Model: pAAV-HBV1.2 plasmid (6 μg, i.v., once)-induced male C57BL/6J mice (6 week-old)[1]
Dosage: 25 mg/kg
Administration: i.g., once daily for 21 days , blood samples were collected every 3 days
Result: Reduced serum HBV DNA levels by 1.88 log10 IU/mL.
Reduced the number of HBcAg-positive cells by 40%.
Did not induce obvious drug-induced liver injury.
分子量

448.53

Formula

C22H26F2N4O2S
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

HBV-IN-54 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HBV-IN-54HBVHepatitis B virusanti-HBV activityHepAD38 cellsHepatitis BHLCZ01 cellsInhibitorinhibitorinhibit

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