产品
编 号:F741597
分子式:C19H16N8O
分子量:372.38
产品类型
结构图
CAS No: 2445499-20-5
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产品详情
生物活性:
JAK-IN-21 (Example 4) is a selective and potent JAK inhibitor with IC50s of 1.73, 2.04, 109 and 62.9 nM against JAK1, JAK2, J2V617F and TYK2, respectively.
体内研究:
JAK-IN-21 (Example 4) shows low bioavailability (F=1.9%).Animal Model:SD rats
Dosage:10 mg/kg
Administration:Oral gavage (Pharmacokinetic Study)
Result:Rat Colon Pharmacokinetic StudyCompoundPlasma Cmax (ng/mL) Plasma AUC (h*ng/mL) t1/2 (h) Colon AUC (h*ng/g) Colon + Feces AUC (h*ng/g)
JAK-IN-2168.8961.66,623545,501
Animal Model:SD rats
Dosage:1 mg/kg or 2 mg/kg
Administration:Intravenous injection (1 mg/kg) or oral gavage (2 mg/kg) (Pharmacokinetic Study)
Result:Pharmacokinetic Parameters in Sprague-Dawley Rats by Intravenous Administration and Oral AdministrationCompoundDose (mg/kg) AUC (h*ng/mL) T1/2 (h) Cl (mL/min/kg) Vd (L/kg) Cmax (ng/mL) F (%)
JAK-IN-21 (iv)1854.80.2219.40.37
JAK-IN-21 (ig)229.80.3840.41.9
体外研究:
JAK-IN-21 (Example 4) doses not inhibit CYPs and shows good liver microsome stability.