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Synonyms:
JAK1-IN-20
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | JAK1-IN-20 (Compound 38) is a gut-restricted, orally active, selective JAK1 inhibitor with an IC50 of less than 0.5 nM. It inhibits the enzymatic activity of JAK1, reduces the production of pro-inflammatory cytokines (TNF-α, IL-6), and suppresses the phosphorylation of STAT3. JAK1-IN-20 shows potential in improving ulcerative colitis and is used in inflammatory bowel disease research. |
| Targets & IC50 | JAK1:<0.5 nM |
| In vitro | JAK1-IN-20 is a potent and selective inhibitor of JAK1 enzyme activity, with an IC50 of less than 0.5 nM. It demonstrates selectivity over JAK2, JAK3, and TYK2 by more than 312-fold, 20,000-fold, and 354-fold, respectively. JAK1-IN-20 (30 min) effectively inhibits the IL-6-induced JAK/STAT3 signaling pathway in HEK-Blue IL-6 cells, with an IC50 of 28.0 nM. |
| In vivo | JAK1-IN-20 (10-30 mg/kg; oral administration; once daily) significantly alleviates acute ulcerative colitis induced by DSS in female C57BL/6J mice, reducing disease activity, increasing colon length, inhibiting the production of pro-inflammatory cytokines, and improving the histopathological features of colon tissue. |
| Molecular Weight | 537.97 |
| Formula | C26H25ClFN7O3 |
| Cas No. | 3106963-85-0 |
| Smiles | O=C1NCC2=CC(=CC=C12)NC3=NC=C(Cl)C(=N3)NC4CCN(C(=O)NC5=CC=C(C=C5F)C(=O)C)CC4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 µL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
| Size | Quantity | Unit Price | Amount | Operation |
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