产品
编 号：F754056
分子式：C19H13F4N7O2S
分子量：479.41
分子式：C19H13F4N7O2S
分子量：479.41
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CAS No: 2613434-12-9
产品详情
生物活性：
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.
体内研究：
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.JAK2/TYK2-IN-2 (5, 20 mg/kg; oral administration; twice a day for 12 days) leads to a low oral bioavailability.Pharmacokinetic Parameters of JAK1/TYK2-IN-2 in Male Sprague-Dawley ratsPK parametersiv PK parametersp.o.
AUC(0-t) (μg/L*h)29.00AUC(0-t) (μg/L*h)13.89
MRT(0-t) (h)4.98MRT(0-t) (h)2.76
t1/2 (h)5.95t1/2 (h)3.64
Cl (L/min/kg)1.58Cl (L/min/kg)20.55
Vss (L/kg)985.41Vss (L/kg)6564.28
Cmax (μg/L)48.55Cmax (μg/L)8.00
Tmax (h)1.00
F11.96%
Animal Model:Six-eight week old male C57BL/6 mice, 20-22 g (acute mice colitis model)
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.
体外研究：
JAK2/TYK2-IN-2 (compound 14l; 0-10000 nM) inhibits the phosphorylation of STAT in vitro.
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.
体内研究：
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.JAK2/TYK2-IN-2 (5, 20 mg/kg; oral administration; twice a day for 12 days) leads to a low oral bioavailability.Pharmacokinetic Parameters of JAK1/TYK2-IN-2 in Male Sprague-Dawley ratsPK parametersiv PK parametersp.o.
AUC(0-t) (μg/L*h)29.00AUC(0-t) (μg/L*h)13.89
MRT(0-t) (h)4.98MRT(0-t) (h)2.76
t1/2 (h)5.95t1/2 (h)3.64
Cl (L/min/kg)1.58Cl (L/min/kg)20.55
Vss (L/kg)985.41Vss (L/kg)6564.28
Cmax (μg/L)48.55Cmax (μg/L)8.00
Tmax (h)1.00
F11.96%
Animal Model:Six-eight week old male C57BL/6 mice, 20-22 g (acute mice colitis model)
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.
体外研究：
JAK2/TYK2-IN-2 (compound 14l; 0-10000 nM) inhibits the phosphorylation of STAT in vitro.
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