Molecular Formula | C19H18N4O3 |
Molar Mass | 350.37 |
Density | 1.302±0.06 g/cm3(Predicted) |
pKa | 10.26±0.50(Predicted) |
Storage Condition | 2-8°C |
In vitro study | Selective JAK3 inhibitor 1 is a potent JAK3 inhibitor with an IC50 of 0.15 nM, and is 4300 times more Selective for JAK3 than for JAK1 in enzyme activity experiments, it is 67 and 140 times more selective than erythropoietin and granulocyte-macrophage colony-stimulating factor. Selective JAK3 inhibitor 1 was also Selective in human peripheral blood mononuclear cell experiments. It inhibits cytokine signaling through JAK3, but not through other JAK family kinases. In T-cells, Selective JAK3 inhibitor 1 inhibits IL-7, IL-15, and IL-2 signaling, but not other cytokine signaling pathways. |
In vivo study | Dosing in a rat collagen-induced arthritis model, during the inflammatory phase, a dose that reaches or exceeds the dose required to completely suppress the phenotype during prophylaxis, selective JAK3 inhibitor 1 partially reversed the inflammatory response and osteoporosis. It inhibits the proliferation of white blood cells, but not red blood cell proliferation. Selective JAK3 inhibitor 1 completely inhibits the progression of the inflammatory response. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.854 ml | 14.271 ml | 28.541 ml |
5 mM | 0.571 ml | 2.854 ml | 5.708 ml |
10 mM | 0.285 ml | 1.427 ml | 2.854 ml |
5 mM | 0.057 ml | 0.285 ml | 0.571 ml |