[CAS NO. 1206101-20-3] GLPG0634 analogue
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PRODUCTS SPECIFICATIONS [1206101-20-3]
Catalog
SLK-S7137
Brand
Selleck
CAS
1206101-20-3
DESCRIPTION [1206101-20-3]
Overview
| MDL | MFCD26406012 |
|---|---|
| Molecular Weight | 410.43 |
| Molecular Formula | C23H18N6O2 |
| SMILES | O=C(C1CC1)NC2=NN3C(C4=CC=C(OCC5=CC=C(C#N)N=C5)C=C4)=CC=CC3=N2 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 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 |
| 50 mM | 0.0487 mL | 0.2436 mL | 0.4873 mL |
Description
GLPG0634 analogue is a selective inhibitor with of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. Phase 2.
Targets
| JAK [1] |
In vitro
In cell lines, GLPG0634 inhibits IL-2- and IL-4-induced JAK1/JAK3/γc signaling and IFN-αB2-induced JAK1/TYK2 type II receptor signaling with IC50 ranged from 150 to 760 nM. GLPG0634 shows higher selectivity for JAK/STAT signaling involving JAK1 than JAK2 kinase in a cellular context. Besides, GLPG0634 also inhibits the differentiation of Th1, Th2, and Th17 cells.
In vivo
Following oral administration, the absolute bioavailability was moderate in rats (45%) and high in mice (∼100%). GLPG0634 (30 mg/kg daily (Rats); 50 mg/kg twice daily (Mice)) dose-dependently reduces inflammation, cartilage, and bone degradation in the CIA model in rats and mice.
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