2. Anti-infection
  3. HBV
  4. GLPG3808

GLPG3808 是一种具有口服活性的 PAPD5/7 抑制剂。GLPG3808 抑制 HBV 感染的多种细胞中 HBcAg 的表达。GLPG3808 降低 HBV 感染动物模型中的乙型肝炎表面抗原水平。GLPG3808 可用于乙型肝炎病毒感染的研究。

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GLPG3808

GLPG3808 Chemical Structure

CAS No. : 2346450-55-1

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GLPG3808 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

GLPG3808 is an orally active PAPD5/7 inhibitor. GLPG3808 inhibits the expression of HBcAg in various cells infected with HBV. GLPG3808 reduces the hepatitis B surface antigen levels in HBV-infected animal models. GLPG3808 can be used for the research of hepatitis B virus infection[1].

体外研究
(In Vitro)

GLPG3808 (Compound 31) 抑制 HBV 感染的 HepG2-NTCP 细胞、iCell 肝细胞 2.0、原代人肝细胞中 HBcAg 的表达，其 IC50 分别为 0.12、5.18 nM、标准条件下 < 0.99 nM；延迟处理条件下 < 0.88 nM[1]。
GLPG3808 (0.25-20 μM): 在 yeast 三杂交竞争实验中可合 PAPD5 和 PAPD7 蛋白，在所有测试浓度完全抑制探针诱导的酵母生长[1]。

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

GLPG3808 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route CL CLunbound Vss T1/2 F AUC0-24
Mice[1] 0.1 mg/kg i.v. 0.86 L/h/kg 3.1 L/h/kg 2.4 L/kg 1.9 h / /
Mice[1] 5 mg/kg p.o. / / / 3.0 h 68 % /
Rat[1] 0.1 mg/kg i.v. 0.72 L/h/kg / 1.4 L/kg 1.3 h / /
Rat[1] 5 mg/kg p.o. / / / 4.6 h 87 % /
Dog[1] 0.5 mg/kg i.v. 0.22 L/h/kg 0.59 L/h/kg 1.27 L/kg 4.0 h / /
Dog[1] 5 mg/kg p.o. / / / 3.7 h 46 % /
Mice[1] 0.03 mg/kg p.o. / / / / / 6.94 ng·h/mL
Mice[1] 0.1 mg/kg p.o. / / / / / 23.5 ng·h/mL
Mice[1] 3 mg/kg p.o. / / / / / 748 ng·h/mL
体内研究
(In Vivo)

GLPG3808 (0.03-30 mg/kg; p.o.; QD; 28 days) 可在感染 HBV 的人源化 FRG 小鼠中使血清 HBsAg 水平降低约 1 个对数单位[1]。
GLPG3808 (0.3-20 mg/kg; p.o.; QD; 91 days) 会使 SD 大鼠的尾部神经传导速度呈剂量依赖性降低[1]。

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

Animal Model: HBV-infected FRG
humanized liver
mouse[1]
Dosage: 0.03, 0.1, 3 mg/kg
Administration: p.o; QD;
28 days
Result: Reduced serum HBsAg levels by
approximately 1 log unit.
Animal Model: SD rat (male and female, 10 weeks old, 262-474 g)[1]
Dosage: 0.3 , 1, 2, 3, 6, 20 mg/kg
Administration: p.o.; QD; 91 days
Result: Caused a dose-dependent decrease in tail nerve conduction velocity.
分子量

475.92

Formula

C24H26ClNO7
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

GLPG3808 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:

GLPG38082346450-55-1GLPG 3808GLPG-3808HBVHepatitis B virusPAPD7PAPD5HepG2-NTCP cellsSprague-Dawley ratsiCell Hepatocytes 2.0hepatitis B virus infectionInhibitorinhibitorinhibit

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