JNJ-54166060 是一种 P2X7 受体 (P2X7 receptor) 拮抗剂，对人/大鼠/小鼠 P2X7 受体作用的IC50值分别为 4/115/72 nM。
| 生物活性 | JNJ-54166060 is a potent and selectiveP2X7 receptorantagonist, withIC50s of 4/115/72 nM for human/rat/mouseP2X7 receptor, respectively[1]. |
| IC50& Target | IC50: 4/115/72 nM (human/rat/mouse P2X7 receptor)[1] |
体内研究
(In Vivo) | 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)[1].
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)[1].
| Animal Model: | Sprague-Dawley rats[1] | | 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[1] | | 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[1] | | 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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
