产品
编 号：F746580
分子式：C28H30FN7O2
分子量：515.58
分子式：C28H30FN7O2
分子量：515.58
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CAS No: 1654776-91-6
产品详情
生物活性：
JAK-IN-20 is a potent, pan and orally active JAK inhibitor with an IC50s of 7 nM, 5 nM, 14 nM for JAK1, JAK2, JAK3, respectively. JAK-IN-20 shows excellent pharmacokinetics and displays anti-inflammatory efficacy in vivo.
体内研究：
JAK-IN-20 (compound 32) (3 mg/kg for p.o.; 1 mg/kg for i.v.) shows excellent pharmacokinetics in rats.JAK-IN-20 (10 mg/kg; p.o.; once a day for 3 days) shows anti-inflammatory effect.Pharmacokinetic Parameters of JAK-IN-20 in female Sprague Dawley rats.parameter32
PO Dose (mg/kg)3
Tmax (h)0.63(0.25-6)
Cmax (μg/mL)7.82±3.68
AUC0-t (μg.h/mL)80.18±35.44
T1/2,po (h)4.77±1.84
MRT (h)7.54±2.52
IV Dose (mg/kg)1
C0 (μg/mL)4.70±2.50
AUC0-t (μg.h/mL)18.89±1.76
Vss (L/kg)0.32±0.14
CL (mL/min/kg)0.85±0.13
T1/2,iv (h)5.16±3.83
MRT (h)6.69±4.03
%F100
Wistar rats; 3 mg/kg; p.o. (1% Tween 80 + 99% (0.5%) methyl cellulose in water); 1 mg/kg; i.v. (5% NMP + 5% solutol + 90% normal saline)Animal Model:7-10 weeks, 250-300g, male wistar rats
Dosage:
Administration:3 mg/kg for p.o.; 1 mg/kg for i.v.
Result:Showed fast oral absorption, higher plasma exposure, extended oral half-life and excellent oral bioavailability of 100%.
Animal Model:Female Sprague Dawley rats ( PGPS rat model)
Dosage:10 mg/kg
Administration:P.o.; once a day; 3 days
Result:Showed anti-inflammatory effect.
JAK-IN-20 is a potent, pan and orally active JAK inhibitor with an IC50s of 7 nM, 5 nM, 14 nM for JAK1, JAK2, JAK3, respectively. JAK-IN-20 shows excellent pharmacokinetics and displays anti-inflammatory efficacy in vivo.
体内研究：
JAK-IN-20 (compound 32) (3 mg/kg for p.o.; 1 mg/kg for i.v.) shows excellent pharmacokinetics in rats.JAK-IN-20 (10 mg/kg; p.o.; once a day for 3 days) shows anti-inflammatory effect.Pharmacokinetic Parameters of JAK-IN-20 in female Sprague Dawley rats.parameter32
PO Dose (mg/kg)3
Tmax (h)0.63(0.25-6)
Cmax (μg/mL)7.82±3.68
AUC0-t (μg.h/mL)80.18±35.44
T1/2,po (h)4.77±1.84
MRT (h)7.54±2.52
IV Dose (mg/kg)1
C0 (μg/mL)4.70±2.50
AUC0-t (μg.h/mL)18.89±1.76
Vss (L/kg)0.32±0.14
CL (mL/min/kg)0.85±0.13
T1/2,iv (h)5.16±3.83
MRT (h)6.69±4.03
%F100
Wistar rats; 3 mg/kg; p.o. (1% Tween 80 + 99% (0.5%) methyl cellulose in water); 1 mg/kg; i.v. (5% NMP + 5% solutol + 90% normal saline)Animal Model:7-10 weeks, 250-300g, male wistar rats
Dosage:
Administration:3 mg/kg for p.o.; 1 mg/kg for i.v.
Result:Showed fast oral absorption, higher plasma exposure, extended oral half-life and excellent oral bioavailability of 100%.
Animal Model:Female Sprague Dawley rats ( PGPS rat model)
Dosage:10 mg/kg
Administration:P.o.; once a day; 3 days
Result:Showed anti-inflammatory effect.
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