GLPG0634 (Synonyms: GLPG0634) |
| Catalog No.GC12579 |
GLPG0634 (GLPG0634) 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.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1206161-97-8
Sample solution is provided at 25 µL, 10mM.
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GLPG0634 is a selective inhibitor of JAK1 with IC50 value of 10nM [1].
GLPG0634 is a small molecule inhibitor of JAK1. It shows potent inhibitory activity against both JAK1 and JAK2 with IC50 values of 10nM and 28nM, respectively. In cellular assays, GLPG0634 is most potent in inhibiting the JAK1/JAK3/γc signaling induced by IL-2– and IL-4 as well as the JAK1/TYK2 type II receptor signaling induced by IFN-αB2. However, it shows lower potent to inhibit JAK2 homodimer–mediated signaling induced by EPO or PRL. It demonstrates that GLPG0634 is specific to JAK1. In addition, GLPG0634 is found to inhibit the phosphorylation of STAT1 and STAT5 induced by cytokines. Moreover, GLPG0634 inhibits the differentiation of Th1 and Th2 cells with similar potencies. Th17 differentiation is also affected by GLPG0634 with a lower potency [1].
In the rat model of collagen-induced arthritis (CIA), oral administration of GLPG0634 shows a marked protection from bone damage at dose of 3 mg/kg. It reduces the infiltration of inflammatory cells significantly from 1 mg/kg onward [1].
References:
[1] Van Rompaey L, Galien R, van der Aar E M, et al. Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases. The Journal of Immunology, 2013, 191(7): 3568-3577.
| Cell experiment [1]: | |
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Cell lines |
THP-1 cells (ATCC TIB-202) |
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Preparation method |
The solubility of this compound in DMSO is >21.3mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
1 μM |
|
Applications |
In THP-1 cells, GLPG0634 preferentially inhibited JAK signaling complexes containing JAK1 and also inhibited Th1 differentiation with similar potencies of 1 μM or lower. |
| Animal experiment [2]: | |
|
Animal models |
Male Sprague Dawley rats (180–200 g) and CD1 mice (23–25 g) |
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Dosage form |
orally dosed as a single esophageal gavage at 5 mg/kg (dosing volume of 5 ml/kg) and i.v. dosed as a bolus via the caudal vein at 1 mg/kg (dosing volume of 5 ml/kg) |
|
Application |
GLPG0634 dose-dependently reduced inflammation, cartilage, and bone degradation in the CIA model in rats and mice with significant effect of 3 mg/kg. Protection from bone damage was evidenced by a dose-dependent reduction, with significant effect from GLPG0634 (3 mg/kg), showed a marked reduction of the infiltration of inflammatory cells while protecting the articular cartilage and bone from 1 mg/kg onward. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Van Rompaey L, Galien R, van der Aar E M., et al. Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases. The Journal of Immunology, 2013, 191(7): 3568-3577. | |
| Cas No. | 1206161-97-8 | SDF | |
| Synonyms | GLPG0634 | ||
| Chemical Name | N-[5-[4-[(1,1-dioxo-1,4-thiazinan-4-yl)methyl]phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide | ||
| Canonical SMILES | C1CC1C(=O)NC2=NN3C(=N2)C=CC=C3C4=CC=C(C=C4)CN5CCS(=O)(=O)CC5 | ||
| Formula | C21H23N5O3S | M.Wt | 425.5 |
| Solubility | ≥ 21.3mg/mL in DMSO | Storage | Store at -20°C |
| 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3502 mL | 11.7509 mL | 23.5018 mL |
| 5 mM | 0.47 mL | 2.3502 mL | 4.7004 mL |
| 10 mM | 0.235 mL | 1.1751 mL | 2.3502 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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