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Filgotinib (GLPG0634)
| Product Name | Filgotinib (GLPG0634) |
| Price: | Inquiry |
| Catalog No.: | CN00156 |
| CAS No.: | 1206161-97-8 |
| Molecular Formula: | C21H23N5O3S |
| Molecular Weight: | 425.50 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | O=C(C1CC1)Nc1nc2n(n1)c(ccc2)c1ccc(cc1)CN1CCS(=O)(=O)CC1 |
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| Description | GLPG0634 is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. |
| Target | JAK1:10 nM (IC50) JAK2:28 nM (IC50) Tyk2:116 nM (IC50) JAK3:810 nM (IC50) |
| In Vitro | GLPG0634 dose-dependently inhibits the differentiation of Th2 cells mediated by IL-4, a cytokine that signals through JAK1 and JAK3. GLPG0634 also inhibits Th1 differentiation with similar potencies of 1 μM or lower[1]. GLPG0634 does not inhibit JAK2 homodimer-mediated signaling induced by EPO or PRL (IC50 > 10 μM)[2]. |
| In Vivo | GLPG0634 (3, 10, 30 mg/kg, p.o.) dose-dependently prevents disease progression in the therapeutic rat CIA model. GLPG0634 (50 mg/kg, o.p.) protects bone and cartilage from degradation, effectively reduces infiltration of T cells (CD3+ cells) and macrophages (F4/80+ cells) in the paw, and decreases the serum levels of all cytokines and chemokines measured, including IL-6, IP-10, XCL1, and MCP-1[1]. GLPG0634 (0.1 and 0.3 mg/kg) shows efficacy in the rat CIA model[2]. |
| Animal Admin | GLPG0634 is 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). In the rat study, each group consists of three rats and blood samples are collected via the jugular vein. In the mouse study, each group consists of 21 mice (n=3/time point) and blood samples are collected by intracardiac puncture under isoflurane anesthesia. Lithium heparin is used as anticoagulant and blood is taken at 0.05, 0.25, 0.5, 1, 3, 5, and 8 h (i.v. route) and 0.25, 0.5, 1, 3, 5, 8, and 24 h (by mouth). |
| Density | 1.5±0.1 g/cm3 |
| Exact Mass | 425.152161 |
| PSA | 108.28000 |
| LogP | 0.79 |
| Storage condition | 2-8°C |