JAK2/TYK2-IN-2 是一种有效的选择性TYK2，JAK2抑制剂，IC50值分别为 9 和 157 nM。JAK2/TYK2-IN-2 还具有抗炎活性。
| 生物活性 | JAK2/TYK2-IN-2 is a potent and selectiveTYK2inhibitor withIC50values of 9 and 157 nM forTYK2andJAK2, respectively. JAK2/TYK2-IN-2 has anti-inflammatory activity[1]. |
| IC50& Target | Tyk2 9 nM (IC50) | JAK2 157 nM (IC50) |
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体外研究
(In Vitro) | JAK2/TYK2-IN-2 (compound 14l; 0-10000 nM) inhibits the phosphorylation of STAT in vitro[1].
Western Blot Analysis[1] | Cell Line: | TF-1, H9, TF-1, THP-1 cells | | Concentration: | 0-10000 nM | | Incubation Time: | | | Result: | After stimulation with IL-6 and IFN-α at a concentration of 100 to 5000 nM, JAK2/TYK2-IN-2 reduced JAK1/JAK2/TYK2 and JAK1/TYK2-dependent signal transduction in a dose-dependent manner and remarkably reduced IFN-α-induced phosphorylation at 10 000 nM. |
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体内研究
(In Vivo) | JAK2/TYK2-IN-2 (10 and 20 mg/kg; oral administration; twice a day for 6 consecutive days) exhibits anti-inflammatory activity in a dose-dependent manner[1].
JAK2/TYK2-IN-2 (5, 20 mg/kg; oral administration; twice a day for 12 days) leads to a low oral bioavailability[1].Pharmacokinetic Parameters of JAK1/TYK2-IN-2 in Male Sprague-Dawley rats[1]
| PK parameters | iv | PK parameters | p.o. | | AUC(0-t)(μg/L*h) | 29.00 | AUC(0-t)(μg/L*h) | 13.89 | | MRT(0-t)(h) | 4.98 | MRT(0-t)(h) | 2.76 | | t1/2(h) | 5.95 | t1/2(h) | 3.64 | | Cl (L/min/kg) | 1.58 | Cl (L/min/kg) | 20.55 | | Vss(L/kg) | 985.41 | Vss(L/kg) | 6564.28 | | Cmax(μg/L) | 48.55 | Cmax(μg/L) | 8.00 | | | Tmax(h) | 1.00 | | | F | 11.96% |
| Animal Model: | Six-eight week old male C57BL/6 mice, 20-22 g (acute mice colitis model)[1] | | Dosage: | 10, 20 mg/kg (dissolved in 5% EtOH, 1% Propylene glycol, 0.5% Tween 80 and 92.5% physiological saline) | | Administration: | Oral administration, twice a day 6 consecutive days | | Result: | Exhibited anti-inflammatory activity and have a good therapeutic effect on inflammatory bowel disease (IBD) in a dose-dependent manner. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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