2. Immunology/Inflammation Apoptosis
  3. IRAK TNF Receptor
  4. GLPG4471

GLPG4471 是一种选择性 IRAK4 抑制剂，IC50 为 1.7 nM。GLPG4471 在细胞和全血表型分析中表现出对细胞因子 (TNFα 和 IFNα) 分泌的强效抑制作用。GLPG4471 在胶原诱导性关节炎的小鼠模型中表现出显著的活性。GLPG4471 可用于研究关节炎。

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GLPG4471

GLPG4471 Chemical Structure

CAS No. : 2499855-36-4

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GLPG4471 相关抗体

Top Publications Citing Use of Products

查看 IRAK 亚型特异性产品:

查看所有亚型
IRAK1 IRAK4

查看 TNF Receptor 亚型特异性产品:

查看所有亚型
TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GLPG4471 is a selective IRAK4 inhibitor with an IC50 of 1.7 nM. GLPG4471 exhibits potent inhibition of cytokine (TNFα and IFNα) secretion in cellular and whole blood phenotypic assays. GLPG4471 displays significant activity in a mouse model of collagen-induced arthritis. GLPG4471 can be used for the study of arthritis[1].

IC50 & Target[1]

IRAK4

1.7 nM (IC50)

体外研究
(In Vitro)

GLPG4471 可有效抑制 CL097 (HY-128799) 刺激的人全血和外周血单个核细胞 (PBMC) 中 TNFα 和 IFNα 的分泌[1]。
GLPG4471 在小鼠、大鼠和人类的肝微粒体和肝细胞中表现出优异的代谢稳定性，预测的肝脏清除率为低至中等[1]。

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

GLPG4471 相关抗体:
药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Mice 1 mg/kg i.v. CL 0.89 L/h/kg
Mice 10 mg/kg p.o. F 75 %
Rat 0.5 mg/kg i.v. CL 0.365 L/h/kg
Rat 5 mg/kg p.o. F 87 %
Mice 1 mg/kg i.v. Vss 1.7 L/kg
Rat 0.5 mg/kg i.v. Vss 1.7 L/kg
Mice 1 mg/kg i.v. T1/2 1.4 h
Rat 0.5 mg/kg i.v. T1/2 3.1 h
体内研究
(In Vivo)

GLPG4471 (3-30 mg/kg，口服，每日两次，持续 17 天) 在 Collagen (HY-NP010) 诱发的关节炎小鼠模型中表现出剂量依赖性活性[1]。

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

Animal Model: Collagen-induced arthritis (CIA) model established in mice[1]
Dosage: 3, 10, 30 mg/kg
Administration: Oral administration (p.o.), twice daily for 17 days
Result: Exhibited a dose-dependent manner of significantly inhibiting the progression of arthritis.
Was above mouse whole blood IC50 for 15, 19 and 24 h at 3, 10 and 30 mg/kg twice-daily, respectively.
分子量

410.47

Formula

C22H26N4O4
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

GLPG4471 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 *
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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)
× = ×
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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:

GLPG44712499855-36-4GLPG 4471GLPG-4471IRAKTNF ReceptorInterleukin-1 receptor associated kinaseIL-1R associated kinaseTumor Necrosis Factor ReceptorTNFRIRAK4Kinase inhibitorInflammationCollagen-induced arthritisInhibitorinhibitorinhibit

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产品名称：
GLPG4471
目录号：
HY-178012
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