2613434-12-9
2613434-12-9 structure
- Name: JAK2/TYK2-IN-1
- Chemical Name: JAK2/TYK2-IN-1
- CAS Number: 2613434-12-9
- Molecular Formula: C19H13F4N7O2S
- Molecular Weight: 479.41
- Create Date: 2022-05-20 11:42:58
- Modify Date: 2024-01-12 18:07:19
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JAK2/TYK2-IN-2 is a potent and selective TYK2 inhibitor with IC50 values of 9 and 157 nM for TYK2 and JAK2, respectively. JAK2/TYK2-IN-2 has anti-inflammatory activity[1].
| Name | JAK2/TYK2-IN-1 |
|---|
| Description | JAK2/TYK2-IN-2 is a potent and selective TYK2 inhibitor with IC50 values of 9 and 157 nM for TYK2 and JAK2, respectively. JAK2/TYK2-IN-2 has anti-inflammatory activity[1]. |
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| Related Catalog | |
| Target |
Tyk2:9 nM (IC50) JAK2:157 nM (IC50) |
| 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. |
| 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. |
| References |
| Molecular Formula | C19H13F4N7O2S |
|---|---|
| Molecular Weight | 479.41 |