JNJ-54166060_product_DataBase

Bioactivity	JNJ-54166060 is a potent and selective P2X7 receptor antagonist, with IC50s of 4/115/72 nM for human/rat/mouse P2X7 receptor, respectively[1].
Target	IC50: 4/115/72 nM (human/rat/mouse P2X7 receptor)
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:
Name	JNJ-54166060
CAS	1627900-41-7
Formula	C20H15ClF4N4O
Molar Mass	438.81
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Devin M Swanson, et al. Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor. J Med Chem. 2016

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