2. Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt
  3. JAK
  4. Filgotinib maleate

Filgotinib maleate  (Synonyms: GLPG0634 maleate)

目录号: HY-18300A
产品使用指南

摩尔计算器

Filgotinib (maleate) 是一种选择性的，具有口服活性的 JAK1 抑制剂，能够有效抑制 JAK1，JAK2，JAK3 和 TYK2 的活性，IC50 值分别为 10 nM，28 nM，810 nM 和 116 nM。Filgotinib (maleate) 可用于类风湿性关节炎（RA）和克罗恩病的研究。

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Filgotinib maleate Chemical Structure

Filgotinib maleate Chemical Structure

CAS No. : 1802998-75-9

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Filgotinib maleate 的其他形式现货产品:

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Filgotinib maleate 相关抗体

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JAK1 JAK2 JAK3 Tyk2 JAK

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Filgotinib (maleate) is a selective and orally active JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM and 116 nM for JAK1, JAK2, JAK3 and TYK2, respectively. Filgotinib (maleate) can be used for rheumatoid arthritis (RA) and Crohn's disease research[1][2].

IC50 & Target[1]

JAK1

10 nM (IC50)

JAK2

28 nM (IC50)

JAK3

810 nM (IC50)

Tyk2

116 nM (IC50)

体外研究
(In Vitro)

Filgotinib (maleate) (1-10 μM) inhibits Th1 and Th2 differentiation in a dose-dependent manner[1].

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

Filgotinib maleate 相关抗体:
体内研究
(In Vivo)

Filgotinib (maleate) (1-10 mg/mL; p.o. and i.v.; Rat collagen-induced arthritis) exhibits good pharmacokinetic profiles and reduces paw swelling, bone and cartilage degradation and levels ofinflammatory cytokines[1].

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

Animal Model: Rat collagen-induced arthritis (CIA)[1]
Dosage: 1 and 10 mg/kg
Administration: Oral administration; for 4 days
Result: Reduced infiltration of inflammatory cells while protecting the articular cartilage and bone.
Animal Model: Rat collagen-induced arthritis (CIA)[1]
Dosage: 1 and 5 mg/kg
Administration: Oral administration and intravenous injection
Result: 1.19
Parameter (Unit) Mouse 1 mg/kg i.v. Mouse 5 mg/kg Orally Rat 1 mg/kg i.v. Rat 5 mg/kg Orally
Cmax or Co (ng/mL) 637 920 1407 (28) 310 (33)
Tmax (h) 0.5 22 (0.5-5)
Area under curve:0-24 h (ng/h/mL) 347 1893 739 (2) 1681 (8)
T1/2 (h) 2.5 1.7 1.6 3.9
Cl (L/h/kg) 2.9 1.4
Vss (L/kg) 6 1.8
F (%)
Clinical Trial
分子量

541.58

Formula

C25H27N5O7S
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

Filgotinib maleate 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

Filgotinib1802998-75-9GLPG0634GLPG 0634GLPG-0634JAKJanus kinaserheumatoid arthritisCrohn's diseaseInhibitorinhibitorinhibit

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