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GLPG0634 analogue

Catalog No.GC17222

GLPG0634 analogue (Compoun 176) is a broad spectrum JAK inhibitor with IC50 values of <100 nM against JAK1, JAK2 and JAK3.

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GLPG0634 analogue Chemical Structure

Cas No.: 1206101-20-3

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10mM (in 1mL DMSO)
$99.00
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5mg
$90.00
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10mg
$252.00
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50mg
$540.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

GLPG0634 is a potent and selective inhibitor of JAK1 with IC50 values of 10, 28, 810 and 116 nM for JAK1, JAK2, JAK3 and TYK2, respectively [1].

Janus kinase 1 (JAK1) is a member of the JAK family and is a non-receptor tyrosine kinase. JAKs play an important role in the immune system. JAK1 is a potential target for the treatment of immune-inflammatory diseases [1].

GLPG0634 is a potent and selective JAK1 inhibitor. GLPG0634 inhibited JAK1, JAK2, JAK3 and TYK2 with IC50 values of 10, 28, 810 and 116 nM, respectively. In CD4+ T cells, GLPG0634 significantly reduced IL-6-induced STAT1 phosphorylation with IC50 value of 629 nM, which suggested the inhibition of JAK1. In CD33+ T cells, GLPG0634 reduced GM-CSF-induced STAT5 phosphorylation with IC50 value of 17.5 µM, suggesting the inhibition of JAK2. GLPG0634 inhibited the differentiation of Th1 and Th2 cells mediated by IL-4 and IL-12, respectively. Also, GLPG0634 inhibited Th17 differentiation induced by TGF-β, IL-23, IL-6 and IL-1β [1].

In rats, GLPG0634 significantly reduced the mRNA levels of Mx2, which were modulated by IFN-α-JAK1/TYK2 signaling. In collagen-induced arthritis (CIA) rat model, GLPG0634 significantly reduced the infiltration of inflammatory cells and reduced the levels of IL-6, IP-10, XCL1 and MCP-1 [1].

Reference:
[1].  Van Rompaey L, Galien R, van der Aar EM, et al. Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases. J Immunol, 2013, 191(7): 3568-3577.

Chemical Properties

Cas No. 1206101-20-3 SDF
Chemical Name (E)-N-(5-(4-((6-cyanopyridin-3-yl)methoxy)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2(3H)-ylidene)cyclopropanecarboxamide
Canonical SMILES N#CC1=NC=C(COC2=CC=C(C3=CC=CC4=N/C(NN34)=N\C(C5CC5)=O)C=C2)C=C1
Formula C23H18N6O2 M.Wt 410.43
Solubility ≥ 31.67mg/mL in DMSO with gentle warming Storage 4°C, protect from light, stored under nitrogen
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.4365 mL 12.1823 mL 24.3647 mL
5 mM 0.4873 mL 2.4365 mL 4.8729 mL
10 mM 0.2436 mL 1.2182 mL 2.4365 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 32 reference(s) in Google Scholar.)

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