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编 号：F746286
分子式：C20H15ClF4N4O
分子量：438.81
分子式：C20H15ClF4N4O
分子量：438.81
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CAS No: 1627900-41-7
产品详情
生物活性：
JNJ-54166060 is a potent and selective P2X7 receptor antagonist, with IC50s of 4/115/72 nM for human/rat/mouse P2X7 receptor, respectively.
体内研究：
JNJ-54166060 exhibits high oral bioavailability (rat 55%, dog >100%, monkey 54 %) and Cmax (rat 375, dog 1249, monkey 389 ng/mL) following oral administration (rat 5 and, dog 5 mg/kg, monkey 5 mg/kg).JNJ-54166060 exhibits terminal elimination half-lives (rat 1.7 and, dog 11.9 h, monkey 4.2 h) due to low-moderate clearance (30, 5.5, and 14 mL/min/kg respectively) following intravenous administration (rat 1.0 and, dog 1.0 mg/kg, monkey 1.0 mg/kg).Animal Model:Sprague-Dawley rats
Dosage:1 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis)
Administration:Intravenous administration and oral administration
Result:Oral bioavailability (55%), Cmax (375 ng/mL), T1/2 (1.7 h).
Animal Model:Beagle dogs
Dosage:1 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis)
Administration:Intravenous administration and oral administration
Result:Oral bioavailability (>100%), Cmax (1249 ng/mL), T1/2 (11.9 h).
Animal Model:Cynomolgus monkeys
Dosage:1 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis)
Administration:Intravenous administration and oral administration
Result:Oral bioavailability (54%), Cmax (389 ng/mL), T1/2 (4.2 h).
JNJ-54166060 is a potent and selective P2X7 receptor antagonist, with IC50s of 4/115/72 nM for human/rat/mouse P2X7 receptor, respectively.
体内研究：
JNJ-54166060 exhibits high oral bioavailability (rat 55%, dog >100%, monkey 54 %) and Cmax (rat 375, dog 1249, monkey 389 ng/mL) following oral administration (rat 5 and, dog 5 mg/kg, monkey 5 mg/kg).JNJ-54166060 exhibits terminal elimination half-lives (rat 1.7 and, dog 11.9 h, monkey 4.2 h) due to low-moderate clearance (30, 5.5, and 14 mL/min/kg respectively) following intravenous administration (rat 1.0 and, dog 1.0 mg/kg, monkey 1.0 mg/kg).Animal Model:Sprague-Dawley rats
Dosage:1 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis)
Administration:Intravenous administration and oral administration
Result:Oral bioavailability (55%), Cmax (375 ng/mL), T1/2 (1.7 h).
Animal Model:Beagle dogs
Dosage:1 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis)
Administration:Intravenous administration and oral administration
Result:Oral bioavailability (>100%), Cmax (1249 ng/mL), T1/2 (11.9 h).
Animal Model:Cynomolgus monkeys
Dosage:1 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis)
Administration:Intravenous administration and oral administration
Result:Oral bioavailability (54%), Cmax (389 ng/mL), T1/2 (4.2 h).
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