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Synonyms: H018
RAI-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 | RAI-20 (H018) is an orally bioavailable dual inhibitor of JAK1 and JAK2, with IC50 values of 15.1 and 22.7 nM, respectively. It exhibits excellent pharmacokinetic properties, including plasma stability, systemic exposure, and a prolonged half-life. In a collagen-induced arthritis rat model, RAI-20 demonstrates significant anti-inflammatory and anti-arthritic activities, effectively reducing paw swelling volume and the arthritis index. RAI-20 serves as a useful compound for research into the pathogenesis of rheumatoid arthritis. |
| Targets & IC50 | JAK2:22.7 nM |
| In vitro | RAI-20 inhibits the proliferation of Ba/F3 cells with an IC50 of 1.21 μM and suppresses IL-6-induced pSTAT1 expression in human whole blood cells with an IC50 of 1.45 μM. It demonstrates excellent in vitro pharmacokinetic properties, including strong stability in human plasma, moderate metabolism in liver microsomes, high plasma protein binding, no significant CYP inhibition, and hERG inhibition activity with an IC50 of 11.5 μM. |
| In vivo | RAI-20 (2-10 mg/kg; oral administration; daily for 14 days) demonstrates strong, dose-dependent anti-arthritic activity in Lewis rats with collagen-induced arthritis, with the most significant reduction in paw volume and arthritis index observed at a daily dose of 10 mg/kg. |
| Synonyms | H018 |
| Molecular Weight | 448.53 |
| Formula | C20H21FN4O3S2 |
| Cas No. | 2549180-90-5 |
| Smiles | N(C(=O)[C@@H]1[C@@H](F)C1)C2=CN3C(=CC=CC3=N2)C=4SC(CN5CCS(=O)(=O)CC5)=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.
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